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1.
Fitoterapia ; : 106026, 2024 May 18.
Artículo en Inglés | MEDLINE | ID: mdl-38768794

RESUMEN

Rydingia michauxii and R. persica, respectively, known as Kase Gol and Goldar in Persian, belong to the family Lamiaceae and they are well known herbal medicine in Iran for the treatment of various diseases, particularly diabetes. This review aims to appraise the phytochemistry, ethnopharmacology, and pharmacological activities of Rydingia species growing in Iran and assess their potential in clinical applications. Besides, it critically evaluates existing literature and looks into the perspective for further research and utilization. All available scientific literature was consulted using the database searches involving Google Scholar, PubMed, and Web of Science applying the keyword Rydingia and its Syn; Otostegia. Only the search results that are associated with the Iranian species R. michauxii and R. persica are included in this review. α-pinene, carvacrol, caryophyllene oxide, diisooctyl phthalate, dillapiole, eugenol, hexadecanoic acid, and pentacosane are the major constituents of the essential oils of the Rydingia species. Additionally, these species produce bioactive flavonoids, phenolic acids, steroids, and terpenoids. Extracts and active compounds from Rydingia species have been reported to possess various pharmacological activities including antidiabetic, anti-inflammatory, antimalarial, antimicrobial, antioxidant, cytotoxic, and lipid-lowering properties. Based on the information available to date on the Iranian Rydingia species, it will be worth subjecting these species to further developmental work involving preclinical and clinical trials.

2.
Fitoterapia ; 176: 105979, 2024 Apr 29.
Artículo en Inglés | MEDLINE | ID: mdl-38692415

RESUMEN

Anogeissus leiocarpus (DC.) Guill. & Perr. belongs to the family Combretaceae and is used both by African traditional medical practitioners and livestock rearers to treat diseases such as African trypanosomiasis, animal diarrhoea, asthma, cancer, cough, diabetes, dysentery, erectile dysfunction, fever, giardiasis, helminthiases, meningitis, menstrual disorders, monkeypox, oral infections, poliomyelitis, sickle cell anaemia, snake bites, toothache, urinary schistosomiasis, and yellow fever. Some of these activities have been associated with the presence of polyphenols in the plant which include ellagic acid derivatives, flavonoids, stilbenes, tannins, and triterpenes. Several bioactive molecules have been identified from A. leiocarpus. These include the main active constituents, ellagitannins, ellagic acid derivates, flavonoids and triterpenes. Pharmacological studies have confirmed its antibacterial, antifungal, antihyperglycemic, antihypertensive, antimalarial, antioxidative, antiparasitic, antitumour and anti-ulcer effects. The stem bark has been investigated mainly for biological activities and phytochemistry, and it is the most mentioned plant part highlighted by the traditional users in ethnomedicinal surveys. In vitro and in vivo models, which revealed a wide range of pharmacological actions against parasites causing helminthiasis, leishmaniasis, malaria and trypanosomiasis, have been used to study compounds from A. leiocarpus. Because of its uses in African traditional medicine and veterinary practices, A. leiocarpus has received considerable attention from researchers. The current review provides a comprehensive overview and critical appraisal of scientific reports on A. leiocarpus, covering its traditional uses, pharmacological activities and phytochemistry.

3.
J Pharm Sci ; 2024 Apr 16.
Artículo en Inglés | MEDLINE | ID: mdl-38621439

RESUMEN

Oral thrush and throat infections can occur in a wide range of patients. Treatments are available; however, resistance to drugs is a major problem for treating oral and throat infections. Three-dimensional printing (3DP) of fast dissolving oral films (FDFs) of linalool oil may provide an alternative solution. Linalool oil FDFs were printed by fused deposition modelling across 1-18 % w/w linalool content range with nozzle diameters of 0.4 or 1 mm at the temperature range of 150 °C-185 °C. The FDFs were evaluated for physicochemical and mechanical properties. Increasing the printer nozzle diameter to 1 mm allowed reducing the printing temperature from 185 °C to 150 °C; consequently, more linalool was quantified in the films with improved content uniformity. The higher linalool content in the films increased the film disintegration time and mechanical strength. FDFs containing 10% w/w linalool showed clear antifungal activity against Candida albicans. Raman spectroscopy suggested linalool separation from excipients at higher temperature printing. Viscoelastic measurements indicated that to achieve printing; the elastic modulus of molten filament needed to be higher than the loss modulus at low angular frequencies. In conclusion, increasing the printing nozzle diameter may avoid loss of the active ingredient by reducing the temperature of the 3DP process.

4.
Heliyon ; 10(1): e23335, 2024 Jan 15.
Artículo en Inglés | MEDLINE | ID: mdl-38332887

RESUMEN

Ceiba pentandra (L.) Gaertn. (Bombacaceae) is popular for the quality of its wood. However, its leaf, stem bark and root bark have been popular in ethnomedicine and, apart from the inflorescence, have been subject of extensive phytochemical investigations. In this study, two compounds were isolated from the crude methanol extract of the inflorescence. Through data from UV, NMR, MS, electrochemical studies, differential scanning calorimetry, and thermogravimetric analysis, the structures were elucidated as 3-C-ß-d-glucopyranosyl-1,3,6,7-tetrahydroxyxanthone (1) and 2-C-ß-d-glucopyranosyl-1,3,6,7-tetrahydroxyxanthone (mangiferin, 2). They were assessed for antioxidant efficacy (DCFDA assay) and for anti-inflammatory efficacy using the lipopolysaccharide (LPS)-induced inflammation model in the RAW 264.7 macrophages (nitrite levels quantified, using Griess Assay, as surrogate for nitric oxide (NO)). Compound 1 (named ceibinin) was established as a novel positional isomer of mangiferin (2). While both 1 and 2 were antioxidant against basal and hydrogen peroxide (100 µM)-induced oxidative stress (6.25 µg/ml abrogated peroxide-induced oxidative stress), ceibinin (1) demonstrated no anti-inflammatory potential, unlike mangiferin (2) which, as previously reported, showed anti-inflammatory effect. Our work reports a positional isomer of mangiferin for the first time in C. pentandra and demonstrates how such isomerism could underlie differences in biological activities and thus the potential for development into therapeutics.

5.
Toxicon ; 238: 107603, 2024 Feb 01.
Artículo en Inglés | MEDLINE | ID: mdl-38184283

RESUMEN

Arsenic toxicity is a major problem across the world due to geogenic activity and has been supposed to generate free radicals and genotoxicity among the arsenic-poisoned population. There is a need to find suitable free radical quenching compounds for the arsenic-induced free radical-affected population. In the present study, Na3AsO3- induced oxidative stress and genotoxicity were evaluated in Oryctolagus cuniculus L, and quenching competency of Ocimum species was examined by applying enzymatic and non-enzymatic in vitro tests, comet assay, and Random Amplified Polymorphic Deoxyribonucleic acid - Polymerase Chain Reaction (RAPD-PCR) methods. In the present study, oxidative damage due to Na3AsO3 intoxication in O. cuniculus L has been confirmed followed by substantive genotoxicity, and in a further study, it has also been reported that the extract of O. gratissimum L lowers the oxidative stress in experimental animals confirmed by a decrease in Malondialdehyde (MDA) 4.78 ± 0.05 (nmol/mg protein), and an increase in Glutathione (GSH) 2.87 ± 0.50 (µmoles/mg proteins), Superoxide Dismutase (SOD) 1.78 ± 0.03(Units/mg protein), Catalase (CAT) 2.72 ± 0.02 (µmoles of H2O2 consumed/min/mg proteins) and Glutathione peroxidase (GPX) 7.43 ± 0.01 (µg of glutathione utilized/min/mg protein). A positive impact of extract of O. gratissimum L on protection of genotoxicity has been also confirmed by Random Amplified Polymorphic DNA (RAPD) based reduction in polymorphic bands of Deoxyribonucleic acid (DNA) from 6.5 to 3.16 and comet assay-based increase in head DNA % (87.86 ± 1.58), tail moment (1.07 ± 0.27) and decrease in tail DNA % (12.13 ± 1.58) & tail length (8.2 ± 1.46) at 5% P in lymphocytes. A significant level reduction in free radicals and reduction in DNA polymorphism has proved the competency of test material for the development of suitable antidotes against arsenicosis.


Asunto(s)
Intoxicación por Arsénico , Arsénico , Ocimum , Animales , Conejos , Antioxidantes/farmacología , Arsénico/toxicidad , Ocimum/metabolismo , Peróxido de Hidrógeno , Técnica del ADN Polimorfo Amplificado Aleatorio , Estrés Oxidativo , Glutatión/metabolismo , Daño del ADN , ADN/metabolismo , Superóxido Dismutasa/metabolismo
6.
Phytochem Anal ; 34(8): 903-924, 2023 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-37963411

RESUMEN

INTRODUCTION: Cannabinoids are a group of compounds that bind to cannabinoid receptors. They possess pharmacological properties like that of the plant Cannabis sativa. Gas chromatography (GC) is one of the popular chromatographic techniques that has been routinely used in the analysis of cannabinoids in different matrices. OBJECTIVE: The article aims to review the literature on the application of GC-based analytical methods for the analysis of phytocannabinoids published during the period from January 2020 to August 2023. METHODOLOGY: A thorough literature search was conducted using different databases, like Web of Knowledge, PubMed, Google Scholar, and other relevant published materials including published books. The keywords used, in various combinations, with cannabinoids being present in all combinations, in the search were cannabinoids, Cannabis sativa, marijuana, analysis, GC, quantitative, qualitative, and quality control. From the search results, only the publications that incorporate the GC analysis of phytocannabinoids were reviewed, and papers on synthetic cannabinoids were excluded. RESULTS: Since the publication of the review article on GC analysis of phytocannabinoids in early 2020, several GC-based methods for the analysis of phytocannabinoids have appeared in the literature. While simple 1D GC-mass spectrometry (MS) and GC-flame ionisation detector (FID) methods are still quite common in phytocannabinoids analysis, 2D GC-MS and GC-MS/MS are increasingly becoming popular, as these techniques offer more useful data for identification and quantification of phytocannabinoids in various matrices. The use of automation in sample preparation and the utilisation of mathematical and computational models for optimisation of different protocols have become a norm in phytocannabinoids analysis. Pre-analyses have been found to incorporate different derivatisation techniques and environmentally friendly extraction protocols. CONCLUSIONS: GC-based analysis of phytocannabinoids, especially using GC-MS, remains one of the most preferred methods for the analysis of these compounds. New derivatisation methods, ionisation techniques, mathematical models, and computational approaches for method optimisation have been introduced.


Asunto(s)
Cannabinoides , Cannabis , Alucinógenos , Espectrometría de Masas en Tándem/métodos , Cromatografía de Gases y Espectrometría de Masas/métodos , Cannabinoides/análisis , Cannabis/química
7.
Phytochemistry ; 215: 113853, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37689382

RESUMEN

Bioactivity-guided phytochemical fractionation of the methanol extract of Olax subscorpioidea root has led to the isolation of six triterpenes. Three of these compounds are previously undescribed triterpenoid saponins: oleanolic acid 3-O-[α-L-rhamnopyranosyl-(1→3)-ß-D-glucopyranosyl-(1 â†’ 2)-6-O-methyl-ß-D-glucuronopyranoside]-28-O-ß-D-glucopyranosyl ester (2), oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-ß-D-glucopyranosyl-(1 â†’ 3)-ß-D-glucopyranoside] (3), and oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-6-O-methyl-ß-D-glucuronopyranoside] ester (5). Other reported known compounds include two triterpene glycosides: oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-6-O-methyl-ß-D-glucuronopyranoside]-28-O-ß-D-glucopyranosyl ester (1) and oleanolic acid 3-O-[ß-D-glucopyranosyl-(1 â†’ 4)-ß-D-glucuronopyranoside] (4); and a triterpene acid, oleanolic acid (6). The structures of these compounds were elucidated by spectroscopic means. The isolated compounds were tested against human cervical cancer (HeLa), colorectal cancer (Caco-2) and breast cancer (MCF-7) cell lines using the in vitro 3-[4,5-dimethylthiazole-2-yl] 3,5-diphenyltetrazolium bromide (MTT) assay, with vincristine as positive control. The cytotoxicity assay showed that compounds 3 and 5 exhibited significant inhibitory effects on the HeLa cell line, with IC50 values of 7.42 ± 0.34 µM and 10.27 ± 1.26 µM; and moderate effects on MCF-7 (IC50 values, 36.67 ± 1.23 µM and 43.83 ± 0.65 µM) and Caco-2 (IC50 values, 35.83 ± 0.55 µM and 39.03 ± 4.38 µM, respectively) cell lines. They were also more selectively cytotoxic than vincristine against the cancer cell lines, when compared with cytotoxicity against the normal lung cell line MRC5.


Asunto(s)
Antineoplásicos , Olacaceae , Ácido Oleanólico , Saponinas , Triterpenos , Humanos , Células HeLa , Vincristina , Células CACO-2 , Saponinas/farmacología , Saponinas/química , Triterpenos/farmacología , Triterpenos/química
8.
Fitoterapia ; 170: 105647, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37562490

RESUMEN

Oliveria decumbens Vent., an annual herb resistant to harsh environmental conditions, is an aromatic medicinal plant of the Apiaceae family. O. decumbens has numerous pharmacological, food and feed, and cosmetic applications. This species is endemic to Iran, Iraq, and Turkey. Published literature, available until 30 November 2022 on the morphology, phytochemistry, and bioactivity of O. decumbens, has been reviewed, and appraised for the potential therapeutic potential of this species, utilizing the databases, Web of Science, Google Scholar, PubMed, and Dictionary of Natural Products. The search term used was O. decumbens. Some manuscripts were issued on the chemical components of O. decumbens essential oil (EO) and various extracts. The EO of O. decumbens was evaluated for its chemical composition and medicinal potential against various diseases. Thymol and carvacrol constituted the primary oxygenated monoterpenes detected in substantial amounts within the EO. Additionally, diverse metabolites of O. decumbens were examined for their bactericidal, antioxidant, larvicidal, and immunomodulatory effects. This review article discusses morphology, phenology, and geographical distribution of O. decumbens and presents a critical appraisal of its phytochemistry and therapeutic potential as documented in the published literature.


Asunto(s)
Apiaceae , Aceites Volátiles , Plantas Medicinales , Apiaceae/química , Estructura Molecular , Aceites Volátiles/farmacología , Aceites Volátiles/química , Timol , Plantas Medicinales/química , Extractos Vegetales/farmacología , Extractos Vegetales/química , Fitoquímicos/farmacología , Etnofarmacología
9.
Phytochem Anal ; 34(7): 709-728, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37392081

RESUMEN

INTRODUCTION: In recent decades, quantitative structure-activity relationship (QSAR) analysis has become an important method for drug design and natural product research. With the availability of bioinformatic and cheminformatic tools, a vast number of descriptors have been generated, making it challenging to select potential independent variables that are accurately related to the dependent response variable. OBJECTIVE: The objective of this study is to demonstrate various descriptor selection procedures, such as the Boruta approach, all subsets regression, the ANOVA approach, the AIC method, stepwise regression, and genetic algorithm, that can be used in QSAR studies. Additionally, we performed regression diagnostics using R software to test parameters such as normality, linearity, residual histograms, PP plots, multicollinearity, and homoscedasticity. RESULTS: The workflow designed in this study highlights the different descriptor selection procedures and regression diagnostics that can be used in QSAR studies. The results showed that the Boruta approach and genetic algorithm performed better than other methods in selecting potential independent variables. The regression diagnostics parameters tested using R software, such as normality, linearity, residual histograms, PP plots, multicollinearity, and homoscedasticity, helped in identifying and diagnosing model errors, ensuring the reliability of the QSAR model. CONCLUSION: QSAR analysis is vital in drug design and natural product research. To develop a reliable QSAR model, it is essential to choose suitable descriptors and perform regression diagnostics. This study offers an accessible, customizable approach for researchers to select appropriate descriptors and diagnose errors in QSAR studies.

10.
Life Sci ; 327: 121856, 2023 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-37307966

RESUMEN

BACKGROUND: Arjunolic acid (AA) is a potent phytochemical with multiple therapeutics effects. In this study, AA is evaluated on type 2 diabetic (T2DM) rats to understand the mechanism of ß-cell linkage with Toll-like receptor 4 (TLR-4) and canonical Wnt signaling. However, its role in modulating TLR-4 and canonical Wnt/ß-catenin crosstalk on insulin signaling remains unclear during T2DM. Aim The current study is aimed to examine the potential role of AA on insulin signaling and TLR-4-Wnt crosstalk in the pancreas of type 2 diabetic rats. METHOD: Multiple methods were used to determine molecular cognizance of AA in T2DM rats, when treated with different dosage levels. Histopathological and histomorphometry analysis was conducted using masson trichrome and H&E stains. While, protein and mRNA expressions of TLR-4/Wnt and insulin signaling were assessed using automated Western blotting (jess), immunohistochemistry, and RT-PCR. RESULTS: Histopathological findings revealed that AA had reversed back the T2DM-induced apoptosis and necrosis caused to rats pancreas. Molecular findings exhibited prominent effects of AA in downregulating the elevated level of TLR-4, MyD88, NF-κB, p-JNK, and Wnt/ß-catenin by blocking TLR-4/MyD88 and canonical Wnt signaling in diabetic pancreas, while IRS-1, PI3K, and pAkt were all upregulated by altering the NF-κB and ß-catenin crosstalk during T2DM. CONCLUSION: Overall results, indicate that AA has potential to develop as an effective therapeutic in the treatment of T2DM associated meta-inflammation. However, future preclinical research at multiple dose level in a long-term chronic T2DM disease model is warranted to understand its clinical relevance in cardiometabolic disease.


Asunto(s)
Diabetes Mellitus Experimental , Diabetes Mellitus Tipo 2 , Ratas , Animales , Vía de Señalización Wnt , FN-kappa B/metabolismo , beta Catenina/metabolismo , Receptor Toll-Like 4/metabolismo , Diabetes Mellitus Experimental/metabolismo , Factor 88 de Diferenciación Mieloide/metabolismo , Páncreas/metabolismo , Insulina/metabolismo , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Diabetes Mellitus Tipo 2/metabolismo
11.
Phytochem Anal ; 34(7): 855-868, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-37337376

RESUMEN

INTRODUCTION: Azadirachta indica A. Juss. is a well-known medicinal plant that has been used traditionally to cure various ailments in every corner of the globe. There are many in vitro and in vivo experimental evidences in connection with the bioactivity of the extracts of this plant. Lung cancer is the deadliest form of cancer and contributes to the most cancer related deaths. The mode of action of anticancer components of this plant is still to be established explicitly. OBJECTIVE: The objective of this study is to identify druggable targets of active constituents of A. indica A. Juss. for non-small cell lung cancer (NSCLC) using network pharmacology and validation of activity through molecular docking analysis. METHODOLOGY: Targets of all the active phytochemicals from A. indica were predicted and genes related to NSCLC were retrieved. A protein-protein interaction (PPI) network of the overlapping genes were prepared. Various databases and servers were employed to analyse the disease pathway enrichment analysis of the clustered genes. Validation of the gene/protein activity was achieved by performing molecular docking, and ADMET profiling of selected phytocompounds was performed. RESULT: Gene networking revealed three key target genes as EGFR, BRAF and PIK3CA against NSCLC by the active components of A. indica. Molecular docking and ADMET analysis further validated that desacetylnimbin, nimbandiol, nimbin, nimbinene, nimbolide, salannin and vepinin are the best suited anti- NSCLC among all the phytocompounds present in this plant. CONCLUSION: The present study has provided a better understanding of the pharmacological effects of active components from A. indica and its potential therapeutic effect on NSCLC.


Asunto(s)
Azadirachta , Carcinoma de Pulmón de Células no Pequeñas , Neoplasias Pulmonares , Simulación del Acoplamiento Molecular , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/genética , Azadirachta/química , Farmacología en Red , Neoplasias Pulmonares/tratamiento farmacológico , Neoplasias Pulmonares/genética
12.
Molecules ; 28(3)2023 Jan 30.
Artículo en Inglés | MEDLINE | ID: mdl-36770987

RESUMEN

Skimmianine is a furoquinoline alkaloid which is found in the Zanthoxylum genus and also in other plants of the Rutaceae family. This study evaluated the effects of skimmianine on the production of pro-inflammatory mediators in LPS-activated BV-2 microglia. Cultured BV-2 cells were treated with skimmianine (10, 20 and 30 µM), followed by stimulation with LPS (100 ng/mL). Levels of TNFα and IL-6 in cell supernatants were measured using ELISA, while NO and PGE2 levels were evaluated with Griess assay and EIA, respectively. Western blotting was used to determine the protein expression of iNOS, COX-2, phospho-p65 and phospho-IκBα. Results showed that Skimmianine reduced LPS-induced elevated the secretion of TNFα, IL-6, NO, and PGE2, as well as the increased protein expression of iNOS and COX-2. Experiments to elucidate the mechanisms of the anti-neuroinflammatory activity of skimmianine revealed the significant inhibition of LPS-induced increased NF-κB-mediated luciferase activity. Pre-treatment with skimmianine also reduced LPS-induced the increased phosphorylation of NF-κB/p65 and IκBα proteins. Furthermore, skimmianine interfered with the binding capacity of NF-κB to consensus sites. Skimmianine pre-treatment protected HT-22 cells from toxicity induced by microglia-conditioned media, as well as increasing MAP-2 expression. The results of this study suggest that skimmianine inhibits neuroinflammation in LPS-activated microglia by targeting the NF-κB activation pathway. Skimmianine also produced neuroprotection against neurotoxicity induced by microglia-conditioned media.


Asunto(s)
Neuroprotección , Quinolinas , Línea Celular , Medios de Cultivo Condicionados/farmacología , Ciclooxigenasa 2/metabolismo , Interleucina-6/metabolismo , Lipopolisacáridos/farmacología , Microglía , FN-kappa B/metabolismo , Inhibidor NF-kappaB alfa/metabolismo , Factor de Necrosis Tumoral alfa/metabolismo , Animales , Ratones , Quinolinas/farmacología
13.
Pharmaceuticals (Basel) ; 16(1)2023 Jan 05.
Artículo en Inglés | MEDLINE | ID: mdl-36678576

RESUMEN

Three-dimensional printing (3DP) allows production of novel fast dissolving oral films (FDFs). However, mechanical properties of the films may not be desirable when certain excipients are used. This work investigated whether adding chitosan micro-ribbons or cellulose microfibres will achieve desired FDFs by fused deposition modelling 3DP. Filaments containing polyvinyl alcohol (PVA) and paracetamol as model drug were manufactured at 170 °C. At 130 °C, filaments containing polyvinylpyrrolidone (PVP) and paracetamol were also created. FDFs were printed with plain or mesh patterns at temperatures of 200 °C (PVA) or 180 °C (PVP). Both chitosan micro-ribbons and cellulose micro-fibres improved filament mechanical properties at 1% w/w concentration in terms of flexibility and stiffness. The filaments were not suitable for printing at higher concentrations of chitosan micro-ribbons and cellulose micro-fibres. Furthermore, mesh FDFs containing only 1% chitosan micro-ribbons disintegrated in distilled water within 40.33 ± 4.64 s, while mesh FDFs containing only 7% croscarmellose disintegrated in 55.33 ± 2.86 s, and croscarmellose containing films showed signs of excipient scorching for PVA polymer. Cellulose micro-fibres delayed disintegration of PVA mesh films to 108.66 ± 3.68 s at 1% w/w. In conclusion, only chitosan micro-ribbons created a network of hydrophilic channels within the films, which allowed faster disintegration time at considerably lower concentrations.

14.
Explor Target Antitumor Ther ; 4(6): 1328-1344, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38213537

RESUMEN

Aim: While the traditional use of Cola rostrata in treating illnesses and diseases has not been reported, the presence of cytotoxic principles has been reported in phylogenetically and biogeographically related species within the Cola genus. This study, therefore, evaluated the cytotoxic potential of extracts of the plant, and the associated cellular and molecular mechanisms. Methods: Activity-based fractionation of the extracts was carried out and cytotoxicity was assessed in the human cervical cancer cell line, HeLa, and the transformed human lung cell line, MRC5-SV2, using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay complemented with brightfield imaging. The 2',7'-dichlorofluorescein diacetate (DCFDA) assay was used to assess induction of cellular reactive oxygen species (ROS), while flow cytometry of 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethyl-imidacarbocyanine iodide (JC-1)-stained cells assessed the loss of mitochondrial membrane potential (∆ΨM). Gas chromatography-mass spectrometry (GC-MS) analysis was carried out on an active fraction. Results: Extracts of the fruit epicarp and leaf were cytotoxic against the cell lines. Half-maximal inhibitory concentration (IC50) values for the 48 h cytotoxicity of the ethanol extract of the epicarp against HeLa and MRC5-SV2 cells were 48.0 µg/mL ± 12.1 µg/mL and 40.4 µg/mL ± 7.2 µg/mL, respectively, while fractions from second-level partitioning of the hexane fraction of the leaf extract elicited cytotoxicity with IC50 values ranging from 12.8 µg/mL ± 1.0 µg/mL to 39.6 µg/mL ± 7.2 µg/mL in both cell lines, following 48 h treatment. GC-MS revealed the presence of seventeen compounds in a hexane fraction of the leaf extract, including even- and odd-chain fatty acids, the most abundant of which were n-hexadecanoic acid, decanoic acid 10-(2-hexylcyclopropyl); and octadecanoic acid. The mechanisms of cytotoxicity of most active fractions involved generation of ROS and mitochondrial membrane depolarisation. Conclusions: The findings show that C. rostrata is rich in cytotoxic phytochemicals which could be isolated for developing new anti-cancer agents.

15.
Molecules ; 27(24)2022 Dec 11.
Artículo en Inglés | MEDLINE | ID: mdl-36557918

RESUMEN

Arbutin, a hydroquinone glucoside, has been detected in ca. 50 plant families, especially in the plants of the Asteraceae, Ericaceae, Proteaceae and Rosaceae families. It is one of the most widely used natural skin-whitening agents. In addition to its skin whitening property, arbutin possesses other therapeutically relevant biological properties, e.g., antioxidant, antimicrobial and anti-inflammatory, as well as anticancer potential. This review presents, for the first time, a comprehensive overview of the distribution of arbutin in the plant kingdom and critically appraises its therapeutic potential as an anticancer agent based on the literature published until the end of August 2022, accessed via several databases, e.g., Web of Science, Science Direct, Dictionary of Natural Products, PubMed and Google Scholar. The keywords used in the search were arbutin, cancer, anticancer, distribution and hydroquinone. Published outputs suggest that arbutin has potential anticancer properties against bladder, bone, brain, breast, cervix, colon, liver, prostate and skin cancers and a low level of acute or chronic toxicity.


Asunto(s)
Antineoplásicos , Arbutina , Femenino , Humanos , Arbutina/farmacología , Arbutina/uso terapéutico , Hidroquinonas , Glucósidos , Antineoplásicos/farmacología , Antineoplásicos/uso terapéutico
16.
Artículo en Inglés | MEDLINE | ID: mdl-35497914

RESUMEN

The Sundarbans, a UNESCO world heritage site, is one of the largest mangrove forests in one stretch. Mangrove plants from this forest are little studied for their endophytic fungi. In this study, we isolated fourteen endophytic fungi from the plants Ceriops decandra and Avicennia officinalis collected from the Sundarbans. Five of them were identified as Aspergillus sp. and one as Penicillium sp. by macroscopic and microscopic observation. Antibacterial activity of the crude extracts obtained from these endophytes was determined against Staphylococcus aureus, Micrococcus luteus, Escherichia coli, and Pseudomonas aeruginosa using resazurin-based microtiter assay. The isolated endophytes showed varying degrees of antibacterial activity with MICs ranging between 5 and 0.078 mg/mL. Molecular identification of the most active endophyte revealed its identity as Aspergillus fumigatus obtained from the leaves of C. decandra. Acute toxicity study of the ethyl acetate extract of A. fumigatus in mice revealed no mortality even at the highest dose of 2000 mg/kg bodyweight, though some opposing results are found in the subacute toxicity study. The extract was subjected to silica gel and Sephadex column chromatography resulting in the isolation of three pure compounds. LC-MS analysis of these pure compounds revealed their identity as fumigaclavine C, azaspirofuran B, and fraxetin. This is the first report of fraxetin from A. fumigatus. All three identified compounds were previously reported for their antibacterial activity against different strains of both Gram-positive and Gram-negative bacteria. Therefore, the observed antibacterial activity of the ethyl acetate (EtOAc) extract of A. fumigatus could be due to the presence of these compounds. These results support the notion of investigating fungal endophytes from the Sundarbans for new antimicrobial compounds.

17.
Biomolecules ; 12(4)2022 04 14.
Artículo en Inglés | MEDLINE | ID: mdl-35454170

RESUMEN

Alternanthera philoxeroides (Mart.) Griseb., commonly known as "Alligator weed" in English, and "Malancha" in Bengali, is a leafy vegetable from the family Amaranthaceae A. L. de Jussieu. This species is native to China, particularly to the provinces around the Yangtze River, other Far East and South-East Asian countries, and countries from other continents (e.g., South America). This plant also grows in certain areas in Australia, New Zealand, and the USA. While in Bangladesh the leaves of this plant are consumed as a vegetable, in China, this plant has been used widely as a traditional remedy for the treatment of various viral diseases (e.g., measles, influenza, and haemorrhagic fever). Flavonoids and saponins are the two largest groups of phytochemicals produced by this plant, and the antiviral property of this plant and its compounds has been studied extensively. This review article reviews all published literature on this plant and critically appraises its phytochemical profile linking to biomolecular interactions and therapeutic potential, particularly, against viral diseases.


Asunto(s)
Amaranthaceae , Saponinas , Virosis , Amaranthaceae/química , Antivirales/farmacología , Antivirales/uso terapéutico , Hojas de la Planta/química , Saponinas/química
18.
Daru ; 30(1): 191-210, 2022 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-35476297

RESUMEN

OBJECTIVES: The recent emergence of the COVID-19 pandemic (caused by SARS-CoV-2) and the experience of its unprecedented alarming toll on humanity have shone a fresh spotlight on the weakness of global preparedness for pandemics, significant health inequalities, and the fragility of healthcare systems in certain regions of the world. It is imperative to identify effective drug treatments for COVID-19. Therefore, the objective of this review is to present a unique and contextualised collection of antiviral natural plants or remedies from the West African sub-region as existing or potential treatments for viral infections, including COVID-19, with emphasis on their mechanisms of action. EVIDENCE ACQUISITION: Evidence was synthesised from the literature using appropriate keywords as search terms within scientific databases such as Scopus, PubMed, Web of Science and Google Scholar. RESULTS: While some vaccines and small-molecule drugs are now available to combat COVID-19, access to these therapeutic entities in many countries is still quite limited. In addition, significant aspects of the symptomatology, pathophysiology and long-term prognosis of the infection yet remain unknown. The existing therapeutic armamentarium, therefore, requires significant expansion. There is evidence that natural products with antiviral effects have been used in successfully managing COVID-19 symptoms and could be developed as anti-COVID-19 agents which act through host- and virus-based molecular targets. CONCLUSION: Natural products could be successfully exploited for treating viral infections/diseases, including COVID-19. Strengthening natural products research capacity in developing countries is, therefore, a key strategy for reducing health inequalities, improving global health, and enhancing preparedness for future pandemics.


Asunto(s)
Productos Biológicos , Tratamiento Farmacológico de COVID-19 , Plantas Medicinales , Antivirales/uso terapéutico , Humanos , Pandemias , SARS-CoV-2
19.
Eur J Cancer Prev ; 31(1): 50-53, 2022 01 01.
Artículo en Inglés | MEDLINE | ID: mdl-34871198

RESUMEN

The cancer chemopreventive potential of various solvent extracts from six medicinal plants was evaluated by their ability to activate the transcription factor Nrf2 using AREc32 cells, which contain a luciferase gene under the control of antioxidant responsive element promoters. Nrf2 regulates the expression of many detoxification enzymes, making it an ideal target for cancer prevention. The present research revealed Zanthoxylum zanthoxyloides extracts as promising sources of cancer chemopreventive compounds. Bioassay-guided isolation of the Z. Zanthoxyloides methanol extract resulted in the isolation of N-methylatanine, N-methylplatydesminecation, sesamin and skimmianine. Among these compounds, skimmianine was identified as the most active compound, causing a 2.8-fold increase in luciferase activity. Skimmianine and other related quinolone alkaloids could represent an appropriate starting scaffold for the development of new chemopreventive cancer drugs.


Asunto(s)
Anticarcinógenos , Neoplasias de la Mama , Plantas Medicinales , Anticarcinógenos/farmacología , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/prevención & control , Femenino , Humanos , Plomo , Luciferasas , Factor 2 Relacionado con NF-E2/genética , Factor 2 Relacionado con NF-E2/metabolismo , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Plantas Medicinales/metabolismo
20.
Antioxidants (Basel) ; 10(10)2021 Sep 29.
Artículo en Inglés | MEDLINE | ID: mdl-34679692

RESUMEN

Xylaria species associated with termite nests or soil have been considered rare species in nature and the few which have been reported upon have been found to act as a rich source of bioactive metabolites. This study evaluated 10 ethyl acetate extracts of five new Xylaria species associated with termite nests or soil for their antioxidant activity, and cytotoxicity against different cancer and normal cell lines. DPPH and ABTS radical scavenging activities of the extracts demonstrated strong capacity with low IC50 values. The highest observed activities belonged to X. vinacea SWUF18-2.3 having IC50 values of 0.194 ± 0.031 mg/mL for DPPH assay and 0.020 ± 0.004 mg/mL for ABTS assay. Total phenolic content ranged from 0.826 ± 0.123 to 3.629 ± 0.381 g GAE/g crude extract which correlated with antioxidant activities. The high total phenolic content could contribute to the high antioxidant activities. Cytotoxicity was recorded against A549, HepG2, HeLa and PNT2 and resulted in broad spectrum to specific activity depending on the cell lines. The highest activities were observed with X. subintraflava SWUF16-11.1 which resulted in 11.15 ± 0.32 to 13.17 ± 2.37% cell viability at a concentration of 100 µg/mL. Moreover, LC-MS fingerprints indicated over 61 peaks from all isolates. There were 18 identified and 43 unidentified compounds compared to mass databases. The identified compounds were from various groups of diterpenoids, diterpenes, cytochalasin, flavones, flavonoids, polyphenols, steroids and derivatives, triterpenoids and tropones. These results indicate that Xylaria spp. has abundant secondary metabolites that could be further explored for their therapeutic properties.

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