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1.
Oxid Med Cell Longev ; 2022: 5288698, 2022.
Article in English | MEDLINE | ID: mdl-35237381

ABSTRACT

Neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson's disease (PD), and Huntington's disease (HD), are characterized by the progressive degeneration of neurons. Although the etiology and pathogenesis of neurodegenerative diseases have been studied intensively, the mechanism is still in its infancy. In general, most neurodegenerative diseases share common molecular mechanisms, and multiple risks interact and promote the pathologic process of neurogenerative diseases. At present, most of the approved drugs only alleviate the clinical symptoms but fail to cure neurodegenerative diseases. Numerous studies indicate that dietary plant polyphenols are safe and exhibit potent neuroprotective effects in various neurodegenerative diseases. However, low bioavailability is the biggest obstacle for polyphenol that largely limits its adoption from evidence into clinical practice. In this review, we summarized the widely recognized mechanisms associated with neurodegenerative diseases, such as misfolded proteins, mitochondrial dysfunction, oxidative damage, and neuroinflammatory responses. In addition, we summarized the research advances about the neuroprotective effect of the most widely reported dietary plant polyphenols. Moreover, we discussed the current clinical study and application of polyphenols and the factors that result in low bioavailability, such as poor stability and low permeability across the blood-brain barrier (BBB). In the future, the improvement of absorption and stability, modification of structure and formulation, and the combination therapy will provide more opportunities from the laboratory into the clinic for polyphenols. Lastly, we hope that the present review will encourage further researches on natural dietary polyphenols in the treatment of neurodegenerative diseases.


Subject(s)
Antioxidants/therapeutic use , Neurodegenerative Diseases/drug therapy , Neuroprotective Agents/therapeutic use , Phytochemicals/therapeutic use , Phytotherapy/methods , Plant Extracts/therapeutic use , Polyphenols/therapeutic use , Animals , Antioxidants/classification , Biological Availability , Biological Transport , Blood-Brain Barrier/metabolism , Disease Models, Animal , Humans , Neurodegenerative Diseases/metabolism , Neuroprotective Agents/classification , Neuroprotective Agents/metabolism , Oxidative Stress/drug effects , Phytochemicals/classification , Phytochemicals/metabolism , Plant Extracts/classification , Polyphenols/classification , Polyphenols/metabolism , Treatment Outcome
2.
Molecules ; 27(3)2022 Jan 20.
Article in English | MEDLINE | ID: mdl-35163946

ABSTRACT

Asian lotus has long been consumed as a food and herbal drug that provides several health benefits. The number of studies on its biological activity is significant, but research at the population level to investigate the variation in phytochemicals and biological activity of each population which is useful for a more efficient phytopharmaceutical application strategy remains needed. This present study provided the frontier results to fill-in this necessary gap to investigating the phytopharmaceutical potential of perianth and stamen, which represent an important part for Asian traditional medicines, from 18 natural populations throughout Thailand by (1) determining their phytochemical profiles, such as total contents of phenolic, flavonoid, and anthocyanin, and (2) determining the antioxidant activity of these natural populations using various antioxidant assays to examine different mechanisms. The result showed that Central is the most abundant floristic region. The stamen was higher in total phenolic and flavonoid contents, whereas perianth was higher in monomeric anthocyanin content. This study provided the first description of the significant correlation between phytochemical contents in perianth compared with stamen extracts, and indicated that flavonoids are the main phytochemical class. This analysis indicated that the stamen is a richer source of flavonoids than perianth, and provided the first report to quantify different flavonoids accumulated in stamen and perianth extracts under their native glycosidic forms at the population level. Various antioxidant assays revealed that major flavonoids from N. nucifera prefer the hydrogen atom transfer mechanism when quenching free radicals. The significant correlations between various phytochemical classes and the different antioxidant tests were noted by Pearson correlation coefficients and emphasized that the antioxidant capability of an extract is generally the result of complex phytochemical combinations as opposed to a single molecule. These current findings offer the alternative starting materials to assess the phytochemical diversity and antioxidant potential of N. nucifera for phytopharmaceutical sectors.


Subject(s)
Antioxidants/pharmacology , Nelumbo/chemistry , Phytochemicals/classification , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Plant Leaves/chemistry , Thailand
3.
Biomed Pharmacother ; 146: 112242, 2022 Feb.
Article in English | MEDLINE | ID: mdl-34953630

ABSTRACT

Myocarditis is an inflammatory disease of the myocardium that mostly affects young adults. The disease is commonly caused by viral infection, medications, autoimmune disorders, and inflammatory conditions. Nearly 50% of the cases of myocarditis are due to post-viral immune response in a setting of an identifiable or non-identifiable infection. The clinical manifestation is nonspecific ranging from asymptomatic courses to sudden death in infants and young patients. This review describes the properties of phytochemicals as plant-derived active ingredients which can be used in the prevention and treatment of myocarditis and its associated risk factors. Meanwhile, it has illustrated epidemiological analyses, mechanism of action, and the metabolism of phytochemicals in animal and human clinical trials. We also mentioned the precise mechanism of action by which phytochemicals elicit their anti-viral, anti-inflammatory, antioxidant, and immunomodulatory effects and how they regulate signal transduction pathways. Nevertheless, comprehensive clinical trials are required to study the properties of phytochemicals in vivo, in vitro, and in silico for a proper management of myocarditis. Our findings indicate that phytochemicals function as potent adjunctive therapeutic drugs in myocarditis and its related complications.


Subject(s)
Dietary Supplements , Myocarditis/prevention & control , Phytochemicals/therapeutic use , Protective Agents/therapeutic use , Animals , Dietary Supplements/adverse effects , Humans , Phytochemicals/adverse effects , Phytochemicals/classification , Protective Agents/adverse effects
4.
Molecules ; 26(15)2021 Jul 28.
Article in English | MEDLINE | ID: mdl-34361712

ABSTRACT

The genus Maytenus is a member of the Celastraceae family, of which several species have long been used in traditional medicine. Between 1976 and 2021, nearly 270 new compounds have been isolated and elucidated from the genus Maytenus. Among these, maytansine and its homologues are extremely rare in nature. Owing to its unique skeleton and remarkable bioactivities, maytansine has attracted many synthetic endeavors in order to construct its core structure. In this paper, the current status of the past 45 years of research on Maytenus, with respect to its chemical and biological activities are discussed. The chemical research includes its structural classification into triterpenoids, sesquiterpenes and alkaloids, along with several chemical synthesis methods of maytansine or maytansine fragments. The biological activity research includes activities, such as anti-tumor, anti-bacterial and anti-inflammatory activities, as well as HIV inhibition, which can provide a theoretical basis for the better development and utilization of the Maytenus.


Subject(s)
Alkaloids/chemistry , Maytansine/analogs & derivatives , Maytenus/chemistry , Phytochemicals/chemistry , Sesquiterpenes/chemistry , Triterpenes/chemistry , Alkaloids/classification , Alkaloids/isolation & purification , Alkaloids/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Anti-Bacterial Agents/pharmacology , Anti-HIV Agents/chemistry , Anti-HIV Agents/isolation & purification , Anti-HIV Agents/pharmacology , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Humans , Maytansine/isolation & purification , Maytansine/pharmacology , Maytenus/metabolism , Molecular Structure , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plants, Medicinal , Sesquiterpenes/classification , Sesquiterpenes/isolation & purification , Sesquiterpenes/pharmacology , Structure-Activity Relationship , Triterpenes/classification , Triterpenes/isolation & purification , Triterpenes/pharmacology
5.
Int J Mol Sci ; 22(14)2021 Jul 12.
Article in English | MEDLINE | ID: mdl-34299094

ABSTRACT

The root bark of Cudrania tricuspidata has been reported to have anti-sclerotic, anti-inflammatory, antioxidant, neuroprotective, hepatoprotective, and cytotoxic activities. In the present study, the effect of 16 compounds from C. tricuspidata on tumor necrosis factor-α+interferon-γ-treated HaCaT cells were investigated. Among these 16 compounds, 11 decreased IL-6 production and 15 decreased IL-8 production. The six most effective compounds, namely, steppogenin (2), cudraflavone C (6), macluraxanthone B (12), 1,6,7-trihydroxy-2-(1,1-dimethyl-2-propenyl)-3- methoxyxanthone (13), cudraflavanone B (4), and cudratricusxanthone L (14), were selected for further experiments. These six compounds decreased the expression levels of chemokines, such as regulated on activation, normal T cell expressed and secreted (RANTES) and thymus and activation-regulated chemokine (TARC), and downregulated the protein expression levels of intercellular adhesion molecule-1. Compounds 2, 6, 12, 4, and 14 inhibited nuclear factor-kappa B p65 translocation to the nucleus; however, compound 13 showed no significant effects. In addition, extracellular signal regulatory kinase-1/2 phosphorylation was only inhibited by compound 14, whereas p38 phosphorylation was inhibited by compounds 13 and 4. Taken together, the compounds from C. tricuspidata showed potential to be further developed as therapeutic agents to suppress inflammation in skin cells.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Inflammation/drug therapy , Keratinocytes/drug effects , Moraceae/chemistry , Phytochemicals/chemistry , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Chemokines/metabolism , Cytokines/metabolism , Humans , Inflammation/metabolism , Inflammation/pathology , Interferon-gamma/metabolism , Keratinocytes/metabolism , NF-kappa B/metabolism , Phosphorylation , Phytochemicals/classification , Signal Transduction , Tumor Necrosis Factor-alpha/pharmacology
6.
ScientificWorldJournal ; 2021: 6623609, 2021.
Article in English | MEDLINE | ID: mdl-33986636

ABSTRACT

BACKGROUND: Nigella sativa L (NS) is a powerful antioxidant and medicinal plant with many therapeutic applications particularly in traditional medicine for respiratory, gastrointestinal, rheumatic, and inflammatory disorders, as well as cancer. OBJECTIVE: The aim of this study is to extract the active ingredients from the Moroccan Nigella sativa L and determine its antioxidant properties. We hypothesize that the separation of the compounds from Nigella sativa L has either a positive or negative effect on antioxidants. To study this, we explored different methods to simultaneously extract and separate compounds from Nigella sativa L and performed antioxidant tests (ß-carotene and DPPH) for all collected fractions. METHODS: Nigella sativa L was hot-extracted by Soxhlet and mother extracts and was separated using silica column chromatography with adequate eluents. Qualitative phytochemical tests to determine the chemical families in Nigella sativa L seeds were performed on the fractions. They were also identified and characterized by GC-MS and HPLC-DAD. Then, antioxidant activity was examined by ß-carotene bleaching and DPPH radical scavenger tests. Results and Conclusion. The mother extract hexane FH generated eight different fractions (SH1-8) and the acetone extract FA generated 11 fractions (SA1-11). The FH fractions had a high percentage of fatty acids, and the FA fractions had some interesting polyphenols derivative compounds. Phytochemical screening revealed secondary metabolites such as polyphenols flavonoids, alkaloids, steroids, terpenes coumarins, tannins, and saponins. We found that only two solvents (hexane, acetone) of different polarities could easily extract and simultaneously separate the components of Nigella sativa L. The antioxidant fractions that we collected had close activity to reference compounds but were more active than the corresponding mother extracts. Moreover, several IC50 values of fractions from acetone extract were better than those from hexane. Therefore, the antioxidant activity of Nigella sativa L is more attributed to flavonoids and polyphenols than fatty acids. In summary, the separation of hexane extract presents a more pronounced positive effect for antioxidant tests than acetone extract.


Subject(s)
Antioxidants/isolation & purification , Flavonoids/isolation & purification , Liquid-Liquid Extraction/methods , Nigella sativa/chemistry , Phytochemicals/isolation & purification , Polyphenols/isolation & purification , Seeds/chemistry , Acetone/chemistry , Alkaloids/chemistry , Alkaloids/classification , Alkaloids/isolation & purification , Antioxidants/chemistry , Antioxidants/classification , Biphenyl Compounds/antagonists & inhibitors , Chromatography, High Pressure Liquid , Coumarins/chemistry , Coumarins/classification , Coumarins/isolation & purification , Flavonoids/chemistry , Flavonoids/classification , Hexanes/chemistry , Humans , Morocco , Phytochemicals/chemistry , Phytochemicals/classification , Picrates/antagonists & inhibitors , Plant Extracts/chemistry , Plants, Medicinal , Polyphenols/chemistry , Polyphenols/classification , Saponins/chemistry , Saponins/classification , Saponins/isolation & purification , Solvents/chemistry , Steroids/chemistry , Steroids/classification , Steroids/isolation & purification , Tannins/chemistry , Tannins/classification , Tannins/isolation & purification , Terpenes/chemistry , Terpenes/classification , Terpenes/isolation & purification , beta Carotene/agonists
7.
Biophys Chem ; 275: 106608, 2021 Aug.
Article in English | MEDLINE | ID: mdl-33962341

ABSTRACT

This paper proposes natural drug candidate compounds for the treatment of coronavirus disease 2019 (COVID-19). We investigated the binding properties between the compounds in the Moringa oleifera plant and the main protease (Mpro) of severe acute respiratory syndrome coronavirus 2 using molecular docking and ab initio fragment molecular orbital calculations. Among the 12 compounds, niaziminin was found to bind the strongest to Mpro. We furthermore proposed novel compounds based on niaziminin and investigated their binding properties to Mpro. The results reveal that the introduction of a hydroxyl group into niaziminin enhances its binding affinity to Mpro. These niaziminin derivatives can be promising candidate drugs for the treatment of COVID-19.


Subject(s)
Antiviral Agents/chemistry , Coronavirus 3C Proteases/antagonists & inhibitors , Moringa oleifera/chemistry , Phytochemicals/chemistry , Protease Inhibitors/chemistry , SARS-CoV-2/chemistry , Thiocarbamates/chemistry , Antiviral Agents/classification , Antiviral Agents/isolation & purification , Antiviral Agents/pharmacology , Catalytic Domain , Coronavirus 3C Proteases/chemistry , Coronavirus 3C Proteases/genetics , Coronavirus 3C Proteases/metabolism , Drug Design , Drug Discovery , Gene Expression , Humans , Molecular Docking Simulation , Molecular Dynamics Simulation , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Protease Inhibitors/classification , Protease Inhibitors/isolation & purification , Protease Inhibitors/pharmacology , Protein Binding , Protein Interaction Domains and Motifs , Protein Structure, Secondary , Quantum Theory , SARS-CoV-2/drug effects , SARS-CoV-2/enzymology , Structure-Activity Relationship , Thermodynamics , Thiocarbamates/classification , Thiocarbamates/isolation & purification , Thiocarbamates/pharmacology , COVID-19 Drug Treatment
8.
Int J Mol Sci ; 22(6)2021 Mar 23.
Article in English | MEDLINE | ID: mdl-33806786

ABSTRACT

In plant ecology, biochemical analyses of bryophytes and vascular plants are often conducted on dried herbarium specimen as species typically grow in distant and inaccessible locations. Here, we present an automated in silico compound classification framework to annotate metabolites using an untargeted data independent acquisition (DIA)-LC/MS-QToF-sequential windowed acquisition of all theoretical fragment ion mass spectra (SWATH) ecometabolomics analytical method. We perform a comparative investigation of the chemical diversity at the global level and the composition of metabolite families in ten different species of bryophytes using fresh samples collected on-site and dried specimen stored in a herbarium for half a year. Shannon and Pielou's diversity indices, hierarchical clustering analysis (HCA), sparse partial least squares discriminant analysis (sPLS-DA), distance-based redundancy analysis (dbRDA), ANOVA with post-hoc Tukey honestly significant difference (HSD) test, and the Fisher's exact test were used to determine differences in the richness and composition of metabolite families, with regard to herbarium conditions, ecological characteristics, and species. We functionally annotated metabolite families to biochemical processes related to the structural integrity of membranes and cell walls (proto-lignin, glycerophospholipids, carbohydrates), chemical defense (polyphenols, steroids), reactive oxygen species (ROS) protection (alkaloids, amino acids, flavonoids), nutrition (nitrogen- and phosphate-containing glycerophospholipids), and photosynthesis. Changes in the composition of metabolite families also explained variance related to ecological functioning like physiological adaptations of bryophytes to dry environments (proteins, peptides, flavonoids, terpenes), light availability (flavonoids, terpenes, carbohydrates), temperature (flavonoids), and biotic interactions (steroids, terpenes). The results from this study allow to construct chemical traits that can be attributed to biogeochemistry, habitat conditions, environmental changes and biotic interactions. Our classification framework accelerates the complex annotation process in metabolomics and can be used to simplify biochemical patterns. We show that compound classification is a powerful tool that allows to explore relationships in both molecular biology by "zooming in" and in ecology by "zooming out". The insights revealed by our framework allow to construct new research hypotheses and to enable detailed follow-up studies.


Subject(s)
Bryophyta/chemistry , Computational Biology , Metabolomics , Phytochemicals/chemistry , Phytochemicals/classification , Biodiversity , Bryophyta/classification , Bryophyta/genetics , Cluster Analysis , Computational Biology/methods , Metabolome , Metabolomics/methods , Phylogeny
9.
Molecules ; 26(8)2021 Apr 10.
Article in English | MEDLINE | ID: mdl-33920081

ABSTRACT

The metabolite profiling of saffron (Crocus sativus L.) from several countries was measured by using ultra-performance liquid chromatography combined with high resolution mass spectrometry (UPLC-HR MS). Multivariate statistical analysis was employed to distinguish among the several samples of C. sativus L. from Greece, Italy, Morocco, Iran, India, Afghanistan and Kashmir. The results of this study showed that the phytochemical content in the samples of C. sativus L. were obviously diverse in the different countries of origin. The metabolomics approach was deemed to be the most suitable in order to evaluate the enormous array of putative metabolites among the saffron samples studied, and was able to provide a comparative phytochemical screening of these samples. Several markers have been identified that aided the differentiation of a group from its counterparts. This can be important for the selection of the appropriate saffron sample, in view of its health-promoting effect which occurs through the modulation of various biological and physiological processes.


Subject(s)
Crocus/metabolism , Metabolome/genetics , Phytochemicals/metabolism , Plant Extracts/chemistry , Biomarkers , Crocus/chemistry , Crocus/classification , Crocus/genetics , Gas Chromatography-Mass Spectrometry , Greece , Humans , India , Iran , Italy , Metabolomics/methods , Morocco , Phytochemicals/chemistry , Phytochemicals/classification , Plant Extracts/classification , Plant Extracts/metabolism
10.
Molecules ; 26(7)2021 Mar 28.
Article in English | MEDLINE | ID: mdl-33800622

ABSTRACT

Croton hirtus L'Hér methanol extract was studied by NMR and two different LC-DAD-MSn using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol-O-[arabinosil(1-6) glucoside] (133 mg/g), dihydro ß ionol-O-[arabinosil(1-6) glucoside] (80 mg/g), ß-sitosterol (49 mg/g), and isorhamnetin-3-O-rutinoside (26 mg/g). C. hirtus was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. The methanolic extracts presented the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), and ferric reducing antioxidant power (FRAP) values. All the tested extracts exhibited inhibitory effects on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with a higher activity observed for dichloromethane (AChE: 5.03 and BChE: 16.41 mgGALAE/g), while the methanolic extract showed highest impact against tyrosinase (49.83 mgKAE/g). Taken together, these findings suggest C. hirtus as a novel source of bioactive phytochemicals with potential for commercial development.


Subject(s)
Antioxidants/chemistry , Cholinesterase Inhibitors/chemistry , Croton/chemistry , Glucosides/chemistry , Phytochemicals/chemistry , Phytosterols/chemistry , Terpenes/chemistry , Acetates/chemistry , Acetylcholinesterase/chemistry , Acetylcholinesterase/metabolism , Antioxidants/classification , Antioxidants/isolation & purification , Benzothiazoles/antagonists & inhibitors , Benzothiazoles/chemistry , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , Butyrylcholinesterase/chemistry , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/isolation & purification , Croton/metabolism , Glucosides/classification , Glucosides/isolation & purification , Humans , Methanol/chemistry , Methylene Chloride/chemistry , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytosterols/classification , Phytosterols/isolation & purification , Picrates/antagonists & inhibitors , Picrates/chemistry , Plant Extracts/chemistry , Solvents/chemistry , Structure-Activity Relationship , Sulfonic Acids/antagonists & inhibitors , Sulfonic Acids/chemistry , Terpenes/classification , Terpenes/isolation & purification , Water/chemistry
11.
Sci Rep ; 11(1): 5019, 2021 03 03.
Article in English | MEDLINE | ID: mdl-33658577

ABSTRACT

In the present research, inter and intra genetic variability of 77 accessions belonging to 11 Thymus species were assessed using eight SRAP primer combinations. High polymorphism (98.3%) was observed in the studied species. The cluster analysis classified Thymus species into five main groups. According to molecular variance (AMOVA) analysis, 63.14% of total genetic variation was obtained within the species, while 36.86% of variation was observed among species. STRUCTURE analysis was also performed to estimate the admixture of species. For instance, T. carmanicus and T. transcaspicus revealed high admixtures. HPLC analysis also demonstrated the presence of rosmarinic acid (32.3-150.7 mg/100 g DW), salvianolic acid (8-90 mg/100 g DW), and cinnamic acid (1.7-32.3 mg/100 g DW) as major phenolic acids, as well as apigenin, epicatechin, and naringenin as the major flavonoids. The highest phenolic and flavonoid contents were detected in T. transcaspicus (37.62 mg gallic acid equivalents (GAE) g-1 DW) and T. vulgaris (8.72 mg quercetin equivalents (QE) g-1 DW), respectively. The antioxidant properties and total phenolic of Thymus species were examined using DPPH and ß-carotene-linoleic acid model systems and consequently T. vulgaris and T. pubescens were detected with the highest and the lowest antioxidant activities respectively. Cluster and principal Components Analysis (PCA) of the components classified the species in to three groups. Finally, similarity within some species was observed comparing molecular and phytochemical markers. For instance, T. vulgaris separated from other species according to major polyphenolic profiles and molecular analyses, as well as T. transcaspicus, T. carmanicus, and T. fedtschenkoi that were clustered in the same groups.


Subject(s)
Flavonoids/classification , Genetic Variation/physiology , Liquid-Liquid Extraction/methods , Phenols/classification , Phytochemicals/classification , Thymus Plant/chemistry , Antioxidants/chemistry , Antioxidants/isolation & purification , Biphenyl Compounds/antagonists & inhibitors , Biphenyl Compounds/chemistry , Chromatography, High Pressure Liquid , Cluster Analysis , Flavonoids/chemistry , Flavonoids/isolation & purification , Humans , Iran , Phenols/chemistry , Phenols/isolation & purification , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Picrates/antagonists & inhibitors , Picrates/chemistry , Plant Breeding/methods , Plant Extracts/chemistry , Principal Component Analysis , Thymus Plant/classification , Thymus Plant/genetics , Thymus Plant/metabolism
12.
Int J Mol Sci ; 22(3)2021 Jan 26.
Article in English | MEDLINE | ID: mdl-33530651

ABSTRACT

Gynecological cancer confers an enormous burden among women worldwide. Accumulating evidence points to the role of phytochemicals in preventing cervical, endometrial, and ovarian cancer. Experimental studies emphasize the chemopreventive and therapeutic potential of plant-derived substances by inhibiting the early stages of carcinogenesis or improving the efficacy of traditional chemotherapeutic agents. Moreover, a number of epidemiological studies have investigated associations between a plant-based diet and cancer risk. This literature review summarizes the current knowledge on the phytochemicals with proven antitumor activity, emphasizing their effectiveness and mechanism of action in gynecological cancer.


Subject(s)
Chemoprevention , Genital Neoplasms, Female/prevention & control , Phytochemicals/pharmacology , Animals , Chemoprevention/methods , Female , Genital Neoplasms, Female/drug therapy , Humans , Phytochemicals/chemistry , Phytochemicals/classification , Phytochemicals/therapeutic use , Polyphenols/chemistry , Polyphenols/pharmacology , Polyphenols/therapeutic use , Structure-Activity Relationship , Sulfhydryl Compounds/chemistry , Sulfhydryl Compounds/pharmacology , Sulfhydryl Compounds/therapeutic use , Terpenes/chemistry , Terpenes/pharmacology , Terpenes/therapeutic use
13.
Proc Natl Acad Sci U S A ; 118(3)2021 01 19.
Article in English | MEDLINE | ID: mdl-33431671

ABSTRACT

To cope with environmental challenges, plants produce a wide diversity of phytochemicals, which are also the source of numerous medicines. Despite decades of research in chemical ecology, we still lack an understanding of the organization of plant chemical diversity across species and ecosystems. To address this challenge, we hypothesized that molecular diversity is not only related to species diversity, but also constrained by trophic, climatic, and topographical factors. We screened the metabolome of 416 vascular plant species encompassing the entire alpine elevation range and four alpine bioclimatic regions in order to characterize their phytochemical diversity. We show that by coupling phylogenetic information, topographic, edaphic, and climatic variables, we predict phytochemical diversity, and its inherent composition, of plant communities throughout landscape. Spatial mapping of phytochemical diversity further revealed that plant assemblages found in low to midelevation habitats, with more alkaline soils, possessed greater phytochemical diversity, whereas alpine habitats possessed higher phytochemical endemism. Altogether, we present a general tool that can be used for predicting hotspots of phytochemical diversity in the landscape, independently of plant species taxonomic identity. Such an approach offers promising perspectives in both drug discovery programs and conservation efforts worldwide.


Subject(s)
Metabolome , Phytochemicals/classification , Plants/chemistry , Plants/classification , Altitude , Biodiversity , Climate , Conservation of Natural Resources/methods , Drug Discovery/methods , Ecosystem , Europe , Hydrogen-Ion Concentration , Phylogeny , Phytochemicals/biosynthesis , Phytochemicals/chemistry , Phytochemicals/isolation & purification , Plants/genetics , Plants/metabolism , Soil/chemistry , Temperature
14.
Curr Drug Discov Technol ; 18(2): 244-271, 2021.
Article in English | MEDLINE | ID: mdl-32178613

ABSTRACT

Osteoarthritis (OA) is known to be the leading cause of pain and disability in the elderly. The prevalence of this disease in adults over 60 years was 9.6% in men and 18% in women. The therapeutic goals of this disease generally include pain relief with the least side effects, improvement of articular function and improvement of life, in which pharmacological and nonpharmacological treatments are performed in different protocols. Due to the common side effects of pain relievers and complaints after invasive joint surgeries, there is a growing interest in the use of Traditional and Complementary protocols in OA treatment. In this paper, different sources of Traditional Persian Medicine (TPM) were searched to obtain any evidence evaluating any medicinal plants in the management of OA. Over 250 effective medicinal plants for the treatment of OA have been introduced in these sources, and by searching electronic databases including PubMed and Scopus, we have found that of these plants, 39 have direct or indirect evidence in the treatment of this complication by different mechanism of actions such as effect on Body mass index (BMI), obesity and dyslipidemia, anti-inflammatory, anti-nociceptive and antioxidant activity. The most important medicinal plants with direct evidence in the management of OA are Allium sativum, Commiphora mukul, Linum usitatissimum, Matricaria chamomilla, Nigella sativa, Zingiber officinale, and Piper nigrum. Medicinal plants seem to be a valuable source for discovering and identifying new drugs for treatment of OA; however, since most of the studies are preclinical, further clinical trials are required to achieve more conclusive results.


Subject(s)
Drug Evaluation, Preclinical , Osteoarthritis/drug therapy , Phytochemicals , Plants, Medicinal/classification , Drug Discovery , Evidence-Based Medicine , Humans , Medicine, Persian/methods , Phytochemicals/classification , Phytochemicals/pharmacology , Phytotherapy/methods
15.
Curr Top Med Chem ; 21(6): 442-460, 2021.
Article in English | MEDLINE | ID: mdl-33292134

ABSTRACT

[Coronaviruses (CoVs) are enveloped positive-stranded RNA viruses with spike (S) protein projections that allow the virus to enter and infect host cells. The S protein is a key virulence factor determining viral pathogenesis, host tropism, and disease pathogenesis. There are currently diverse corona viruses that are known to cause disease in humans. The occurrence of Middle East respiratory syndrome coronavirus (MERS-CoV) and Severe Acute Respiratory Syndrome coronavirus (SARS-CoV), as fatal human CoV diseases, has induced significant interest in the medical field. The novel coronavirus disease (COVID-19) is an infectious disease caused by a novel strain of coronavirus (SAR-CoV-2). The SARS-CoV2 outbreak has been evolved in Wuhan, China, in December 2019, and identified as a pandemic in March 2020, resulting in 53.24 M cases and 1.20M deaths worldwide. SARS-CoV-2 main proteinase (MPro), a key protease of CoV-2, mediates viral replication and transcription. SARS-CoV-2 MPro has been emerged as an attractive target for SARS-CoV-2 drug design and development. Diverse scaffolds have been released targeting SARS-CoV-2 MPro. In this review, we culminate the latest published information about SARS-CoV-2 main proteinase (MPro) and reported inhibitors.


Subject(s)
Antiviral Agents/chemistry , Coronavirus 3C Proteases/antagonists & inhibitors , Phytochemicals/chemistry , Protease Inhibitors/chemistry , SARS-CoV-2/chemistry , Amino Acid Sequence , Antiviral Agents/classification , Antiviral Agents/pharmacology , Catalytic Domain , Coronavirus 3C Proteases/chemistry , Coronavirus 3C Proteases/genetics , Coronavirus 3C Proteases/metabolism , Drug Discovery , Gene Expression , High-Throughput Screening Assays , Humans , Molecular Docking Simulation , Phytochemicals/classification , Phytochemicals/pharmacology , Protease Inhibitors/classification , Protease Inhibitors/pharmacology , Protein Binding , Protein Interaction Domains and Motifs , Protein Structure, Secondary , SARS-CoV-2/drug effects , SARS-CoV-2/enzymology , Structure-Activity Relationship , COVID-19 Drug Treatment
16.
Molecules ; 25(21)2020 Oct 22.
Article in English | MEDLINE | ID: mdl-33105694

ABSTRACT

Viral infections and associated diseases are responsible for a substantial number of mortality and public health problems around the world. Each year, infectious diseases kill 3.5 million people worldwide. The current pandemic caused by COVID-19 has become the greatest health hazard to people in their lifetime. There are many antiviral drugs and vaccines available against viruses, but they have many disadvantages, too. There are numerous side effects for conventional drugs, and active mutation also creates drug resistance against various viruses. This has led scientists to search herbs as a source for the discovery of more efficient new antivirals. According to the World Health Organization (WHO), 65% of the world population is in the practice of using plants and herbs as part of treatment modality. Additionally, plants have an advantage in drug discovery based on their long-term use by humans, and a reduced toxicity and abundance of bioactive compounds can be expected as a result. In this review, we have highlighted the important viruses, their drug targets, and their replication cycle. We provide in-depth and insightful information about the most favorable plant extracts and their derived phytochemicals against viral targets. Our major conclusion is that plant extracts and their isolated pure compounds are essential sources for the current viral infections and useful for future challenges.


Subject(s)
Antiviral Agents/therapeutic use , Coronavirus Infections/drug therapy , HIV Infections/drug therapy , Hepatitis C, Chronic/drug therapy , Herpes Simplex/drug therapy , Influenza, Human/drug therapy , Phytochemicals/therapeutic use , Pneumonia, Viral/drug therapy , Antiviral Agents/chemistry , Antiviral Agents/classification , Antiviral Agents/isolation & purification , Betacoronavirus/drug effects , Betacoronavirus/pathogenicity , Betacoronavirus/physiology , COVID-19 , Coronavirus Infections/pathology , Coronavirus Infections/virology , Drug Discovery , HIV/drug effects , HIV/pathogenicity , HIV/physiology , HIV Infections/pathology , HIV Infections/virology , Hepacivirus/drug effects , Hepacivirus/pathogenicity , Hepacivirus/physiology , Hepatitis C, Chronic/pathology , Hepatitis C, Chronic/virology , Herpes Simplex/pathology , Herpes Simplex/virology , Humans , Influenza, Human/pathology , Influenza, Human/virology , Orthomyxoviridae/drug effects , Orthomyxoviridae/pathogenicity , Orthomyxoviridae/physiology , Pandemics , Phytochemicals/chemistry , Phytochemicals/classification , Phytochemicals/isolation & purification , Plants, Medicinal , Pneumonia, Viral/pathology , Pneumonia, Viral/virology , SARS-CoV-2 , Simplexvirus/drug effects , Simplexvirus/pathogenicity , Simplexvirus/physiology , Virus Internalization/drug effects , Virus Replication/drug effects
17.
Molecules ; 25(17)2020 Aug 28.
Article in English | MEDLINE | ID: mdl-32872217

ABSTRACT

A pandemic caused by the novel coronavirus (SARS-CoV-2 or COVID-19) began in December 2019 in Wuhan, China, and the number of newly reported cases continues to increase. More than 19.7 million cases have been reported globally and about 728,000 have died as of this writing (10 August 2020). Recently, it has been confirmed that the SARS-CoV-2 main protease (Mpro) enzyme is responsible not only for viral reproduction but also impedes host immune responses. The Mpro provides a highly favorable pharmacological target for the discovery and design of inhibitors. Currently, no specific therapies are available, and investigations into the treatment of COVID-19 are lacking. Therefore, herein, we analyzed the bioactive phytocompounds isolated by gas chromatography-mass spectroscopy (GC-MS) from Tinospora crispa as potential COVID-19 Mpro inhibitors, using molecular docking study. Our analyses unveiled that the top nine hits might serve as potential anti-SARS-CoV-2 lead molecules, with three of them exerting biological activity and warranting further optimization and drug development to combat COVID-19.


Subject(s)
Antiviral Agents/chemistry , Betacoronavirus/chemistry , Phytochemicals/chemistry , Protease Inhibitors/chemistry , Tinospora/chemistry , Viral Nonstructural Proteins/antagonists & inhibitors , Antiviral Agents/classification , Antiviral Agents/isolation & purification , Antiviral Agents/pharmacology , Betacoronavirus/drug effects , Betacoronavirus/enzymology , COVID-19 , Catalytic Domain , Coronavirus 3C Proteases , Coronavirus Infections/drug therapy , Cysteine Endopeptidases/chemistry , Cysteine Endopeptidases/genetics , Cysteine Endopeptidases/metabolism , Drug Discovery , Gas Chromatography-Mass Spectrometry , Gene Expression , Humans , Kinetics , Molecular Docking Simulation , Pandemics , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Pneumonia, Viral/drug therapy , Protease Inhibitors/classification , Protease Inhibitors/isolation & purification , Protease Inhibitors/pharmacology , Protein Binding , Protein Interaction Domains and Motifs , Protein Structure, Secondary , SARS-CoV-2 , Substrate Specificity , Thermodynamics , Viral Nonstructural Proteins/chemistry , Viral Nonstructural Proteins/genetics , Viral Nonstructural Proteins/metabolism
18.
Molecules ; 25(14)2020 Jul 17.
Article in English | MEDLINE | ID: mdl-32708908

ABSTRACT

Herbs derived from Taraxacum genus have been used as traditional medicines and food supplements in China for hundreds of years. Taraxacum mongolicum is a famous traditional Chinese medicine derived from Taraxacum genus for the treatment of inflammatory disorders and viral infectious diseases. In the present study, the bioactive phenolic chemical profiles and antioxidant activities of flowers, leaves, and roots of Taraxacum mongolicum were investigated. Firstly, a high performance liquid chromatography method combined with segmental monitoring strategy was employed to simultaneously determine six bioactive phenolic compounds in Taraxacum mongolicum samples. Moreover, multivariate statistical analysis, including hierarchical clustering analysis, principal component analysis, and partial least squares discriminant analysis were performed to compare and discriminate different parts of Taraxacum mongolicum based on the quantitative data. The results showed that three phenolic compounds, caftaric acid, caffeic acid, and luteolin, could be regarded as chemical markers for the differences of flowers, leaves, and roots of Taraxacum mongolicum. In parallel, total phenolic contents, total flavonoid contents and antioxidant activities of different parts of Taraxacum mongolicum were also evaluated and compared. It is clear that Taraxacum mongolicum had antioxidant properties, and the antioxidant capacities of different parts of Taraxacum mongolicum in three antioxidant assays showed a similar tendency: Flowers ≈ leaves > roots, which revealed a positive relationship with their total phenolic and flavonoid contents. Furthermore, to find the potential antioxidant components of Taraxacum mongolicum, the latent relationships of the six bioactive phenolic compounds and antioxidant activities of Taraxacum mongolicum were investigated by Pearson correlation analysis. The results indicated caftaric acid and caffeic acid could be the potential antioxidant ingredients of Taraxacum mongolicum. The present work may facilitate better understanding of differences of bioactive phenolic constituents and antioxidant activities of different parts of Taraxacum mongolicum and provide useful information for utilization of this herbal medicine.


Subject(s)
Antioxidants/chemistry , Phenols/chemistry , Phytochemicals/chemistry , Taraxacum/chemistry , Antioxidants/classification , Antioxidants/isolation & purification , Caffeic Acids/chemistry , Chromatography, High Pressure Liquid , Flowers/chemistry , Luteolin/chemistry , Phenols/classification , Phenols/isolation & purification , Phytochemicals/classification , Phytochemicals/isolation & purification , Plant Leaves/chemistry , Plant Roots/chemistry
19.
Molecules ; 25(4)2020 Feb 14.
Article in English | MEDLINE | ID: mdl-32075048

ABSTRACT

In this work a comparative study on phytochemical profiles of comfrey root extracts obtained by different extraction approaches has been carried out. Chemical profiles of extracts obtained by supercritical fluid (SFE), pressurized liquid (PLE), and conventional solid/liquid extraction were compared and discussed. Phytochemical composition was assessed by high-performance liquid chromatography coupled with electrospray time-of-flight mass spectrometry (HPLC-ESI-QTOF-MS/MS) identifying 39 compounds reported for the first time in comfrey root, mainly phenolic acids and fatty acids. The influence of different extraction parameters on phytochemical profiles of S. officinale root was investigated for all applied techniques. PLE and maceration, using alcohol-based solvents (aqueous methanol or ethanol), were shown to be more efficient in the recovery of more polar compounds. Greater numbers of phenolics were best extracted by PLE using 85% EtOH at 63 °C. The use of SFE and 100% acetone for 30 min enabled good recoveries of nonpolar compounds. SFE using 15% EtOH as a cosolvent at 150 bar produced the best recoveries of a significant number of fatty acids. The main compositional differences between extracts obtained by different extraction techniques were assigned to the solvent type. Hence, these results provided comprehensive approaches for treating comfrey root enriched in different phytochemicals, thereby enhancing its bioaccessibility.


Subject(s)
Comfrey/chemistry , Phenols/isolation & purification , Phytochemicals/isolation & purification , Plant Extracts/chemistry , Antioxidants/chemistry , Antioxidants/isolation & purification , Chromatography, High Pressure Liquid , Liquid-Liquid Extraction , Phenols/chemistry , Phenols/classification , Phytochemicals/chemistry , Phytochemicals/classification , Plant Roots/chemistry , Solvents/chemistry , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry
20.
Recent Pat Biotechnol ; 14(3): 203-228, 2020.
Article in English | MEDLINE | ID: mdl-31987028

ABSTRACT

BACKGROUND: Gracilaria has been shown to be an important source of marine bioactive natural biomaterials and compounds. Although there are no enough patents used Gracilaria worldwide, the current study tries to put the Gracilaria on the spot for further important patents in the future. OBJECTIVE: The current study investigates the pharmaceuticals and biochemical activity of Gracilaria because no previous studies have been carried out to examine the biochemical and pharmaceutical activates of Gracilaria from the Suez Canal of Egypt as an excellent source for bioactive compounds. METHODS: Different advanced experimental models and analytical techniques, such as cytotoxicity, total antioxidant capacity, anticancer, and anti-inflammatory profiling were applied. The phytochemical analysis of different constituents was also carried out. RESULTS: The mineral analysis revealed the presence of copper (188.3 ppm) and iron (10.07 ppm) in addition to a remarkable wealth of selenium and sulfur contents giving up to 36% of its dry mass. The elemental analysis showed high contents of sulfur and nitrogen compounds. The GCMS profiling showed varieties of different bioactive compounds, such as fatty acids, different types of carotenoids in addition to pigments, alkaloids, steroids. Many other compounds, such as carbohydrates and amino acids having antioxidant, anti-inflammatory, and antiviral activities, etc. were identified. The cytotoxicity activity of Gracilaria marine extract was very effective against cancerous cell lines and showed high ability as a potent antitumor due to their bioactive constituents. Specialized screening assays using two anticancer experimental models, i.e., PTK and SKH1 revealed 77.88% and 84.50% inhibition anticancer activity; respectively. The anti-inflammatory activities investigated using four different experimental models, i.e., COX1, COX2, IL6, and TNF resulted in 68%, 81.76%, 56.02% and 78.43% inhibition; respectively. Moreover, Gracilaria extracts showed potent anti-Alzheimer with all concentrations. CONCLUSION: Gracilaria proved to be a multi-product source of marine natural products for different biotechnological applications. Our recommendation is to investigate the Gracilaria bioactive secondary metabolites in order to create and innovate in more patents from current important seaweeds (Gracilaria).


Subject(s)
Anti-Inflammatory Agents/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Antioxidants/chemistry , Biological Products/chemistry , Cytotoxins/chemistry , Gracilaria/chemistry , Phytochemicals/chemistry , Alkaloids/chemistry , Alkaloids/classification , Alkaloids/isolation & purification , Alkaloids/pharmacology , Anti-Inflammatory Agents/classification , Anti-Inflammatory Agents/isolation & purification , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/classification , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/pharmacology , Antioxidants/classification , Antioxidants/isolation & purification , Antioxidants/pharmacology , Aquatic Organisms , Biological Products/classification , Biological Products/isolation & purification , Biological Products/pharmacology , Carotenoids/chemistry , Carotenoids/classification , Carotenoids/isolation & purification , Carotenoids/pharmacology , Cell Line, Tumor , Cell Survival/drug effects , Copper/chemistry , Copper/isolation & purification , Cytotoxins/classification , Cytotoxins/isolation & purification , Cytotoxins/pharmacology , Fatty Acids/chemistry , Fatty Acids/classification , Fatty Acids/isolation & purification , Fatty Acids/pharmacology , Gracilaria/metabolism , High-Throughput Screening Assays , Humans , Iron/chemistry , Iron/isolation & purification , Nootropic Agents/chemistry , Nootropic Agents/classification , Nootropic Agents/isolation & purification , Nootropic Agents/pharmacology , Patents as Topic , Phytochemicals/classification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Pigments, Biological/chemistry , Pigments, Biological/classification , Pigments, Biological/isolation & purification , Pigments, Biological/pharmacology , Selenium Compounds/chemistry
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