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1.
Arch Pharm (Weinheim) ; 357(2): e2300528, 2024 Feb.
Article En | MEDLINE | ID: mdl-37974540

The genus Stachys L., one of the largest genera of the Lamiaceae family, is highly represented in Turkey. This study was conducted to determine the bio-pharmaceutical potential and phenolic contents of six different extracts from aerial parts of Stachys tundjeliensis. The obtained results showed that the ethanol extract exhibited the highest antioxidant activity in the antioxidant assays. Meanwhile, the ethanol extract displayed strong inhibitory activity against α-tyrosinase, the dichloromethane extract exhibited potent inhibition against butyrylcholinesterase, and the n-hexane extract against α-amylase. Based on ultra-high performance liquid chromatography coupled to high-resolution mass spectrometry analysis, more than 90 secondary metabolites, including hydroxybenzoic acid, hydroxycinnamic acid, and their glycosides, acylquinic acids, phenylethanoid glycosides, and various flavonoids were identified or tentatively annotated in the studied S. tundjeliensis extracts. It was observed that the application of S. tundjeliensis eliminated H2 O2 -induced oxidative stress. It was determined that protein levels of phospho-nuclear factor kappa B (NF-κB), receptor for advanced glycation endproducts, and activator protein-1, which are activated in the nucleus, decreased, and the synthesis of matrix metalloproteinase (MMP)-2 and MMP-9 also decreased to basal levels. Overall, these findings suggest that S. tundjeliensis contains diverse bioactive compounds for the development of nutraceuticals or functional foods with potent biological properties.


Stachys , Stachys/chemistry , Plant Extracts/chemistry , Butyrylcholinesterase , Receptor for Advanced Glycation End Products , Structure-Activity Relationship , Antioxidants/pharmacology , Antioxidants/chemistry , Glycosides , Ethanol
2.
Curr Med Chem ; 2023 05 24.
Article En | MEDLINE | ID: mdl-37226794

Background: Zingiber officinale Roscoe (Ginger) belongs to the Zingiberaceae family, which is renowned for its rich nutritional and phytochemical composition, and has been validated for its anti-diabetic and anti-inflammatory properties via in vitro, in vivo, and clinical studies. Nonetheless, a comprehensive review of these pharmacological studies, especially clinical studies, together with an analysis of the mechanism of action of the bioactive compounds is still lacking. This review provided a comprehensive and updated analysis of the anti-diabetic efficacy of Z. officinale and its compounds ginger enone, gingerol, paradol, shogaol, and zingerone. Methods: The present systematic review was conducted using the PRISMA guidelines. Scopus, ScienceDirect, Google Scholar, and PubMed were the main databases used for retrieving information from inception to March 2022. Results: From the findings obtained, Z. officinale can be regarded as a therapeutic species showing significant improvement in clinical studies on glycemic parameters (Fasting blood glucose (FBG), hemoglobin A1C (HbA1c), and insulin resistance). In addition, the bioactive compounds of Z. officinale act via several mechanisms as revealed by in vitro and in vivo studies. Overall, these mechanisms were by increasing glucose-stimulated insulin secretion, sensitising insulin receptors and raising glucose uptake, translocation of GLUT4, inhibition of advanced glycation end product-induced increase of reactive oxygen species, regulation of hepatic gene expression of enzymes associated with glucose metabolism, regulation of the level of pro-inflammatory cytokines, amelioration of the pathological injuries of kidneys, protective effect on the morphology of ß-cells as well as its antioxidant mechanisms, among others. Conclusion: Z. officinale and its bioactive compounds displayed promising results in in vitro and in vivo systems, nevertheless, it is highly recommended that human trials be conducted on these compounds since clinical studies are the core of medical research and considered the final stages of the drug development process.

3.
Int J Mol Sci ; 23(20)2022 Oct 11.
Article En | MEDLINE | ID: mdl-36292966

Despite existing conventional hypoglycemic drugs to manage diabetes, their non-availability and cost in low-income countries coupled with the associated side effects remain a major concern. Consequently, exploring for alternative treatments to manage diabetes has been a continuous priority. Nigella sativa L. (NS) (Family: Ranunculaceae) is regarded as a valuable traditional remedy in diabetes management and extensively studied for its biological properties. This systematic review provides a comprehensive and critical analysis of clinical studies on the efficacy, safety, and mechanism of action of NS and its compound thymoquinone (TQ) in diabetes management. The main scientific databases which were scrutinised were Scopus, PubMed, Google Scholar, and Web of Science. Data search was conducted from inception to January 2022. A total of 17 clinical studies were obtained; 16 studies on Nigella sativa L. and 1 study on its compound TQ. N. sativa was found to be highly potent in terms of its hypoglycemic activity when compared to placebo based on improvement in parameters including fasting blood glucose (FBG), postprandial blood glucose (PPBG), Hemoglobin A1C (HbA1c), homeostatic model assessment for insulin resistance (HOMA-IR), and homeostatic model assessment for assessment of beta-cell functionality (HOMA-ß). The compound TQ in combination with a daily dose of metformin demonstrated a greater reduction in the levels of HbA1c and blood glucose compared to metformin alone. The bioavailability of TQ can be enhanced by using nanoparticulate drug delivery systems. Considering the findings of the clinical studies along with negligible adverse effects, NS has strong potential application in bioproduct development for the management of diabetes. Further investigations should explore the detailed mechanism of actions by which TQ exerts its therapeutic antidiabetic effects to provide more insights into its clinical use in the management of diabetes.


Diabetes Mellitus , Metformin , Nigella sativa , Humans , Glycated Hemoglobin , Blood Glucose , Benzoquinones/pharmacology , Benzoquinones/therapeutic use , Diabetes Mellitus/drug therapy , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Metformin/therapeutic use
4.
Front Pharmacol ; 13: 1046523, 2022.
Article En | MEDLINE | ID: mdl-36588685

Sepsis is a severe inflammatory response to systemic infection and is a threatening cause of death in intensive care units. In recent years, a number of studies have been conducted on the protective effect of natural products against sepsis-induced organ injury. However, a comprehensive review of these studies indicating the mechanisms of action of the bioactive compounds is still lacking. In this context, this review aimed to provide an updated analysis of the mechanism of action of plants' secondary metabolites in the management of sepsis. Scopus, Science Direct, Google Scholar, and PubMed were searched from inception to July 2022. A variety of secondary metabolites were found to be effective in sepsis management including allicin, aloin, cepharanthine, chrysin, curcumin, cyanidin, gallic acid, gingerol, ginsenoside, glycyrrhizin, hesperidin, kaempferol, narciclasine, naringenin, naringin, piperine, quercetin, resveratrol, rosmarinic acid, shogaol, silymarin, sulforaphane, thymoquinone, umbelliferone, and zingerone. The protective effects exerted by these compounds can be ascribed to their antioxidant properties as well as induction of endogenous antioxidant mechanisms, and also via the downregulation of inflammatory response and reduction of biochemical and inflammatory markers of sepsis. These findings suggest that these secondary metabolites could be of potential therapeutic value in the management of sepsis, but human studies must be performed to provide strength to their potential clinical relevance in sepsis-related morbidity and mortality reduction.

5.
Curr Med Chem ; 28(23): 4670-4693, 2021.
Article En | MEDLINE | ID: mdl-33475054

BACKGROUND: The increasing incidence of diabetes worldwide has urged researchers to explore novel antidiabetic agents from natural products. Ethnomedicinal field studies on diabetes have expanded across the globe, documenting large numbers of folk medicinal plants against diabetes. Nonetheless, a systematic review of these surveys has not been conducted so far. This study documents the medicinal plants traditionally used globally for managing diabetes. METHODS: Key databases including Sciencedirect, Medline/PubMed, and Google Scholar were scrutinized. The Plant List and The International Plant Names Index (IPNI) were used to validate the scientific plant names. RESULTS: 2004 traditionally used plants belonging to 1112 genera and 197 families were reported across 92 countries for the management of diabetes. Leguminosae (105 genera and 193 species), Compositae (97 genera and 188 species), and Lamiaceae (47 genera and 121 species) were the main plant families reported. Momordica charantia L., Syzygium cumini (L.) Skeels, Allium sativum L., Azadirachta indica A.Juss., Catharanthus roseus (L.) G.Don, Olea europaea L., Trigonella foenum-graecum L., Gymnema sylvestre (Retz.) R.Br. ex Sm., Aloe vera (L.) Burm.f., and Allium cepa L were the species mostly reported. Indeed, the antidiabetic properties of these main species have been evidenced by experimental studies. Several antidiabetic compounds acting via different mechanisms have been identified, including momordicoside, karaviloside, cucurbitacin, charantin, and charantoside from M. charantia, cuminoside from S. cumini, S-allyl cysteine sulfoxide from A. sativum, limonoids from A. indica, alkaloids including vindoline, vindolidine, vindolicine and vindolinine from C. roseus, oleuropein and oleanolic acid from O. europaea, flavone C-glycosides such as vicenin-1, isoschaftoside, and schaftoside from T. foenum-graecum seeds, gymnemosides, gymnemagenin, and pregnane glycosides from G. sylvestre, chysalodin from A. vera, and quercetin from A. cepa. CONCLUSION: This review is the first to provide a compiled list of traditional medicinal plants used worldwide against diabetes.


Diabetes Mellitus , Plants, Medicinal , Diabetes Mellitus/drug therapy , Humans , Hypoglycemic Agents/therapeutic use , Medicine, Traditional , Phytotherapy
6.
Food Chem Toxicol ; 135: 111013, 2020 Jan.
Article En | MEDLINE | ID: mdl-31794803

Seaweeds are among the significant currently exploited marine plant resources which are gaining full applications in culinary, cosmetic, pharmaceutical, and biotechnological processes. Much attention has been devoted to seaweeds based on their proven health benefits and is considered as a rich source of structurally different bioactive metabolites for the discovery of novel functional food-based pharmacophores/drugs. Nonetheless, there is still a dearth of updated compilation and analysis of the in-depth pharmacological activities of these compounds. This review, therefore, aims to provide a piece of up-to-date detailed information on the major compounds isolated from various seaweed species together with their in-vitro and in-vivo biological properties. These compounds were found to possess broad pharmacological properties and inhibitory enzyme activities against critical enzymes involved in the aetiology of noncommunicable diseases. However, their toxicity, clinical efficacy, mechanisms of action, and interaction with conventional foods, are still less explored and require more attention in future studies.


Biological Products/pharmacology , Seaweed/chemistry , Animals , Humans , Polysaccharides/pharmacology , Tannins/pharmacology
7.
J Food Biochem ; 43(11): e13003, 2019 11.
Article En | MEDLINE | ID: mdl-31393014

The phytochemical, antiradical, and enzyme inhibition profile of three solvent extracts (ethyl acetate, methanol, water) of Origanum sipyleum were assessed. We also performed a pharmacological study in order to explore protective effects induced by extracts in inflamed colon. LC-MS analysis revealed that the extracts contained different classes of phenolics. The aqueous extract showed the highest antioxidant and acetylcholinesterase (AChE) inhibitory effects. Total phenol and flavonoid contents were highest in aqueous and ethyl acetate extract, respectively. All extracts were effective in reducing colon pro-oxidant and pro-inflammatory biomarkers. The extracts revealed also able to inhibit fungal and bacterial species involved in ulcerative colitis, including Candida albicans, Candida tropicalis, Staphylococcus aureus, and Staphylococcus thyphimurium. Finally, we also showed the antiproliferative effects exerted by the EA extracts on human colon cancer HCT116 cell line. Concluding, our results indicated that O. sipyleum extracts displayed promising therapeutic properties which warrants further validation. PRACTICAL APPLICATIONS: The present phytochemical and biological studies, including antioxidant, anti-inflammatory, and antimicrobic assessments, showed significant protective effects exerted by O. sipyleum extracts in an experimental model of ulcerative colitis. The results are intriguing and suggest potential applications O. sipyleum extracts as sources of natural agents for the management of clinical symptoms related to ulcerative colitis, characterized by increased burden of oxidative stress and microbiome dysbiosis.


Acetylcholinesterase/pharmacology , Anti-Inflammatory Agents/pharmacology , Origanum/chemistry , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Acetates , Acetylcholinesterase/chemistry , Acetylcholinesterase/drug effects , Anti-Inflammatory Agents/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Cholinesterase Inhibitors , Flavonoids/chemistry , Flavonoids/pharmacology , Methanol/chemistry , Phenols/chemistry , Phenols/pharmacology , Phytochemicals/chemistry , Plant Extracts/chemistry , Plant Extracts/toxicity , Solvents
8.
Food Res Int ; 123: 414-424, 2019 09.
Article En | MEDLINE | ID: mdl-31284993

Bunium species have been reported to be used both as food and in traditional medicines. The scientific community has attempted to probe into the pharmacological and chemical profiles of this genus. Nonetheless, many species have not been investigated fully to date. In this study, we determined the phenolic components, antimicrobial, antioxidant, and enzyme inhibitory activities of aerial parts of four Bunium species (B. sayai, B. pinnatifolium, B. brachyactis and B. macrocarpum). Results showed that B. microcarpum and B. pinnatifolium were strong antioxidants as evidenced in the DPPH, ABTS, CUPRAC, and FRAP assays. B. brachyactis was the most effective metal chelator, and displayed high enzyme inhibition against cholinesterase, tyrosinase, amylase, glucosidase, and lipase. The four species showed varied antimicrobial activity against each microorganism. Overall, they showed high activity against P. mirabilis and E. coli (MIC and MBC <1 mg mL-1). B. brachyactis was more effective against Aspergillus versicolor compared to the standard drug ketoconazole. B. brachyactis was also more effective than both ketoconazole and bifonazole against Trichoderma viride. B. sayai was more effective than ketoconazole in inhibiting A. fumigatus. B. sayai was most non-toxic to HEK 293 (cellular viability = 117%) and HepG2 (cellular viability = 104%). The highest level of TPC was observed in B. pinnatifolium (35.94 mg GAE g-1) while B. microcarpum possessed the highest TFC (39.21 mg RE g-1). Seventy four compounds were detected in B. microcarpum, 70 in B. brachyactis, 66 in B. sayai, and 51 in B. pinnatifolium. Quinic acid, chlorogenic acid, pantothenic acid, esculin, isoquercitrin, rutin, apigenin, and scopoletin were present in all the four species. This study showed that the four Bunium species are good sources of biologically active compounds with pharmaceutical and nutraceutical potential.


Apiaceae/chemistry , Apiaceae/classification , Amylases/antagonists & inhibitors , Amylases/metabolism , Animals , Anti-Infective Agents/analysis , Anti-Infective Agents/pharmacology , Antioxidants/analysis , Antioxidants/pharmacology , Apigenin/analysis , Apigenin/metabolism , Chlorogenic Acid/analysis , Chlorogenic Acid/pharmacology , Cholinesterase Inhibitors/analysis , Cholinesterase Inhibitors/pharmacology , Enterobacter cloacae/drug effects , Enterobacter cloacae/metabolism , Enzyme Inhibitors/analysis , Enzyme Inhibitors/pharmacology , Escherichia coli/drug effects , Escherichia coli/metabolism , Esculin/analysis , Esculin/pharmacology , Glucosidases/antagonists & inhibitors , Glucosidases/metabolism , HEK293 Cells , Hep G2 Cells , Humans , Lipase/antagonists & inhibitors , Lipase/metabolism , Mice , Microbial Sensitivity Tests , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Pantothenic Acid/analysis , Pantothenic Acid/pharmacology , Phenols/analysis , Phenols/pharmacology , Plant Extracts/analysis , Plant Extracts/pharmacology , Proteus mirabilis/drug effects , Proteus mirabilis/metabolism , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/metabolism , Quercetin/analogs & derivatives , Quercetin/analysis , Quercetin/pharmacology , Quinic Acid/analysis , Quinic Acid/pharmacology , RAW 264.7 Cells , Rutin/analysis , Rutin/pharmacology
9.
J Food Biochem ; 43(3): e12766, 2019 03.
Article En | MEDLINE | ID: mdl-31353569

The present study evaluated the biological potential of methanol and aqueous extracts of the twigs and fruits of Cotoneaster integerrimus Medik. Lethality bioassays performed on Artemia salina showed that aqueous and methanol C. integerrimus extracts were non-toxic in the concentration range (0.1-20 mg/ml), with a LC50 ≥ 2.5 mg/ml, for each single extract. The protective effect of the extracts was assessed in vitro against hydrogen peroxide-induced lactate dehydrogenase (LDH) activity and tumor necrosis factor (TNF)α gene expression in colon cancer HCT116 cell line. All the extracts downregulated (H2 O2 )-induced TNFα gene expression, in HCT116. By contrast, it was observed that the lipopolysaccharide (LPS)-induced increase in colon nitrite, prostaglandin E2 , and 8-iso-PGF2α levels were counteracted mostly by the methanol twig extract. The present study showed protective effects induced by C. integerrimus in vitro and ex vivo, thus supporting potential application in the management of chronic inflammatory diseases. PRACTICAL APPLICATIONS: In the present study, protective effects of C. integerrimus are highlighted using in vitro and ex-vivo models of hydrogen peroxide-induced LDH activity in HCT116 cell and on LPS-induced inflammation in rat colon. Based on our results, this edible and traditionally used species could be considered as a valuable source of natural agents to combat inflammatory diseases, particularly ulcerative colitis. Results amassed herein advocates for further bioprospection of this species that could open new avenues for the development of nutraceuticals and functional foods geared toward the management of chronic inflammatory diseases.


Colon/immunology , Hydrogen Peroxide/toxicity , L-Lactate Dehydrogenase/metabolism , Plant Extracts/pharmacology , Protective Agents/pharmacology , Rosaceae/chemistry , Animals , Colon/drug effects , Dinoprostone/immunology , Fruit/chemistry , HCT116 Cells , Humans , In Vitro Techniques , L-Lactate Dehydrogenase/genetics , Lipopolysaccharides/adverse effects , Male , Rats , Rats, Sprague-Dawley , Tumor Necrosis Factor-alpha/genetics , Tumor Necrosis Factor-alpha/immunology
10.
J Pharm Biomed Anal ; 168: 217-224, 2019 May 10.
Article En | MEDLINE | ID: mdl-30831505

The practice of traditional medicine, especially herbal medicine, is still prevalent across the African continent. Yet, their in-depth pharmacological and chemical exploitation by the scientific community remain a necessity. The aim of the present study was to investigate into the phenolic components, antioxidant, and enzyme-inhibitory activities of three solvent extracts (ethyl acetate, methanol, and water) of the stem bark of four African plant species (Senna siamea, Distemonanthus benthamianus, Harrisonia abyssinica, and Pycnanthus angolensis). It was found that D. benthamianus followed by P. angolensis, displayed the highest DPPH and ABTS scavenging, ferric and cupric reducing, and total antioxidant capacity in the phosphomolybdenum assay. A similar result was observed for AChE, BChE, and tyrosinase inhibition. The two plants also showed comparable α-amylase inhibitory effect. On the other hand, H. abyssinica showed high metal chelating and α-glucosidase inhibition. Among the solvents used, the methanol extract seemed to be the most bioactive. In addition, TPC was highest in D. benthamianus (135.33-192.29 mg GAE/g) while P. angolensis was richest in TFC (7.68-12.48 mg RE/g). A range of bioactive compounds were identified in the extracts, with variations observed among the plants. Senna siamea stem bark showed the presence of nine compounds; where flavonoids (e.g. naringenin, kaempferol, dihydroquercetin) were recorded. Genistein (m/z 271.06), procyanidin B (m/z 577.13) and C (m/z 865.19) isomers were common in stem barks extracts of D. benthamianus and P. Angolensis. To conclude, D. benthamianus and P. angolensis can be considered as potential pharmaceutical agents or functional food components that could reduce the risks of oxidative stress-related disorders.


Chromatography, High Pressure Liquid/methods , Plant Extracts/analysis , Plants, Medicinal/chemistry , Tandem Mass Spectrometry/methods , Africa , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/pharmacology , Plant Bark , Plant Extracts/chemistry , Plant Extracts/pharmacology , Solvents/chemistry
11.
J Pharm Biomed Anal ; 168: 174-180, 2019 May 10.
Article En | MEDLINE | ID: mdl-30807922

The present investigation attempts to compare the pharmacological properties and phytochemical profile of four extracts (ethyl acetate, dichloromethane, methanol, and water) of Asphodeline taurica (Pall.) Endl. roots from Bulgaria and Turkey. The Bulgarian ethyl acetate extract displayed the highest antioxidant activity in the DPPH, CUPRAC, and phosphomolybdenum assay, and strongest inhibition against α-amylase and α-glucosidase. The Turkish aqueous extract exhibited the strongest ABTS scavenging and ferric reducing power while its methanol extract was the most effective acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor. On the other hand, the Turkish dichloromethane extract showed the highest lipase inhibition. UHPLC/Orbitrap MS analysis showed a wide array of individual phenolics; six free anthraquinones, two bianthraquinones, three bianthracenes, three anthraquinone glycosides and one bianthracen glycoside were identified. The present data suggest that A. taurica roots can be considered as a valuable source of biologically active phytocompounds with functional properties for the cosmetic and pharmaceutical industries.


Asphodelaceae/chemistry , Cholinesterase Inhibitors/pharmacology , Chromatography, High Pressure Liquid/methods , Plant Extracts/pharmacology , Acetylcholinesterase/drug effects , Bulgaria , Butyrylcholinesterase/drug effects , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/isolation & purification , Metabolomics/methods , Plant Extracts/chemistry , Plant Roots , Turkey
12.
J Ethnopharmacol ; 234: 245-289, 2019 Apr 24.
Article En | MEDLINE | ID: mdl-30658182

ETHNOPHARMACOLOGICAL RELEVANCE: Mauritius is famous for its floricultural diversity and traditions practiced across the island by various ethnic groups. During the British rule in the 1835s, Indian indentured labourers migrated to Mauritius and played a very important role in shaping the Mauritian culture. They brought along their high heritage of traditional knowledge of certain medicinal herbs and spices. Nonetheless, there has been no comparative study to investigate whether these past traditional knowledge are still preserved in Mauritius and India. AIM OF THE STUDY: To document and compare the traditional uses of medicinal herbs and spices brought by Indian indentured labourers with their current uses in Mauritius and India, and to review pharmacological studies of such plants. MATERIALS AND METHODS: Locally published textbooks, research dissertations, and relevant records from the 'Mauritiana' section of the University of Mauritius library were scrutinised for possible early records of such herbs and spices brought by Indian indentured immigrants. Field trips and site visits to Mauritius Herbarium and The National Folk Museum were conducted to gather data on their traditional uses as practiced by the Indian indentured immigrants. A literature search was performed to gather the current ethnomedicinal uses of these plants in Mauritius and India using key databases such as ScienceDirect and PubMed, as well as thesis from local university website. Pharmacological studies on these plants were also reviewed in an attempt to compare the ethnomedicinal uses against reported ailments. RESULTS: Indian labourers brought 18 medicinal plants for medicinal purposes as documented at the folk museum of Indian Immigration. Piper betle L., Azadirachta indica A. Juss., and Curcuma longa L. were common plants used by Indian indentured immigrants against a wide range of ailments. Data obtained from recent ethnomedicinal surveys revealed that A. indica and C. longa were the most traditionally used plants in India, while in Mauritius, C. longa was the most popular plant followed by Allium sativum L. and Ocimum tenuiflorum L. It was also found that all these plants are currently being used against a wide range of diseases in both countries. In addition, several studies have highlighted the pharmacological properties such as analgesic, anti-inflammatory, anti-microbial, anti-pyretic, and anti-diabetic for some plants. CONCLUSION: This investigation can be considered as a first attempt to document and compare traditional knowledge of medicinal plants brought by Indian immigrants. We observed that some of these knowledge are preserved and still practiced in Mauritius. It is anticipated that this study will revive the interest in safeguarding and promoting the ancestral knowledge on the uses of such plants.


Phytotherapy/history , Plant Preparations/history , Plants, Medicinal/chemistry , Emigrants and Immigrants/history , Ethnopharmacology/history , Health Knowledge, Attitudes, Practice , History, 19th Century , Humans , India , Mauritius , Medicine, Traditional/history , Plant Preparations/chemistry
13.
Food Res Int ; 115: 425-438, 2019 01.
Article En | MEDLINE | ID: mdl-30599961

Phyllanthus phillyreifolius var. commersonii Müll. Arg is an endemic plant of Mauritius. To date, no study has been performed concerning its polyphenolic profile and pharmacological properties. In this study, a decoction (water), ethyl acetate and methanol extracts of the aerial parts of P. phillyreifolius, obtained from different extraction procedures (maceration and Soxhlet), were studied for antibacterial, antioxidant, anticancer, and enzyme inhibitory properties along with their polyphenolic profile. The ethyl acetate macerated extract showed high antibacterial activity against B. cereus (MIC = 0.293 mg/mL) and E. coli (MIC = 0.417 mg/mL) while S. epidermidis was most susceptible to the ethyl acetate-Soxhlet extract (MIC = 0.521 mg/mL). The methanol-Soxhlet extract displayed the most potent cupric and ferric reducing power, and metal chelating effect, while the macerated methanolic extract was the most effective DPPH and ABTS scavenger, and BChE inhibitor. Only the ethyl acetate-Soxhlet extract exhibited α-glucosidase inhibition. All extracts exhibited a strong anti-tyrosinase activity, which was further investigated by molecular docking and molecular dynamic. After 48 h exposure to the extracts for HeLa cell lines, the ethyl acetate-Soxhlet extract showed the highest inhibition (IC50 = 533.1 µg/mL) while the decoction extract was more cytotoxic to MDA-MB-231 cells (IC50 = 337.4 µg/mL). Treatment of cancer cell lines with all P. phillyreifolius extracts resulted in a time-dependent reduction of cell viability for HeLa and dose-and time-dependent reduction for MDA-MB-231. Gene expression ratio of Bcl-2 to Bax was higher for all Soxhlet-extracts. Total phenolics (TPC) and flavonoids (TFC) content were highest in the decoction and methanol-Soxhlet extract, respectively (122.43 mg GAE/g extract and 31.28 mg RE/g extract, respectively). The extracts were abundant in ellagitannins, although phenolic acids and flavonoids were also detected. Granatin B was detected for the first time in Phyllanthus species. Overall, the aerial parts of P. phillyreifolius exemplify a potent reservoir of bioactive phytochemicals for therapeutic applications.


Phenols/analysis , Phenols/pharmacology , Phyllanthus/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Anti-Bacterial Agents/analysis , Antineoplastic Agents/analysis , Antioxidants/analysis , Bacteria/drug effects , Cell Survival/drug effects , Enzyme Inhibitors/analysis , Flavonoids/analysis , HeLa Cells , Humans , Hydrolyzable Tannins/analysis , Mauritius , Microbial Sensitivity Tests , Molecular Docking Simulation , Molecular Dynamics Simulation , Monophenol Monooxygenase/drug effects , Phytochemicals/analysis , Phytochemicals/pharmacology
14.
J Pharm Biomed Anal ; 162: 225-233, 2019 Jan 05.
Article En | MEDLINE | ID: mdl-30268023

The genus Scrophularia has received much interest with regards to its traditional uses against eczema, psoriasis, and mastitis. Yet, the medicinal properties of some species still need to be scientifically validated. The present study was designed to investigate into the biological properties of various solvent extracts (ethyl acetate, methanol, and aqueous) of the roots and aerial parts of Scrophularia lucida based on its antioxidant, anti-inflammatory, and enzyme inhibitory activities together with phytochemical screening. Our results revealed that the solvent extracts differed in their biological effectiveness. The root ethyl acetate extract showed the highest ABTS scavenging, FRAP, CUPRAC, and inhibitory activity against AChE and α-glucosidase. The ethyl acetate extract of the aerial parts displayed the highest BChE and α-amylase inhibition and antioxidant effect in the phosphomolybdenum assay, while the methanol extracts of both parts were the most effective DPPH• scavengers and tyrosinase inhibitors. The methanol extracts of the root and aerial parts also inhibited NO production in lipopolysaccharide (LPS)-stimulated murine leukemic monocyte-macrophage cell (4.99% and 10.77%, respectively), at 31.25 µg/mL concentration. The highest TPC (34.98 mg GAE/g extract) and TFC (48.33 mg RE/g extract) were observed in the ethyl acetate extract of the root and aerial parts, respectively. The most abundant compounds in the root ethyl acetate extract were luteolin (852 µg/g extract), rosmarinic acid (522 µg/g extract), and hesperidin (394 µg/g extract) while kaempferol was most abundant in the ethyl acetate extract of the aerial parts (628 µg/g extract). In silico experiments were conducted on tyrosinase and the higher docking values were observed for rosmarinic acid and hesperidin. The present findings provide base line information which tend to support the potential use of S. lucida in the management of several chronic diseases, including Alzheimer's disease and diabetes mellitus.


Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Chromatography, High Pressure Liquid , Computer Simulation , Enzyme Inhibitors/pharmacology , Plant Extracts/pharmacology , Scrophularia/chemistry , Acetates/chemistry , Amylases/antagonists & inhibitors , Amylases/metabolism , Animals , Anti-Inflammatory Agents/isolation & purification , Antioxidants/chemistry , Antioxidants/isolation & purification , Cholinesterase Inhibitors/isolation & purification , Cholinesterase Inhibitors/pharmacology , Cinnamates/isolation & purification , Cinnamates/pharmacology , Depsides/isolation & purification , Depsides/pharmacology , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors/pharmacology , Hesperidin/isolation & purification , Hesperidin/pharmacology , Kaempferols/isolation & purification , Kaempferols/pharmacology , Luteolin/isolation & purification , Luteolin/pharmacology , Macrophages/drug effects , Macrophages/metabolism , Methanol/chemistry , Mice , Molecular Docking Simulation , Molecular Dynamics Simulation , Molecular Structure , Monophenol Monooxygenase/antagonists & inhibitors , Monophenol Monooxygenase/metabolism , Nitric Oxide/metabolism , Plant Components, Aerial/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Roots/chemistry , RAW 264.7 Cells , Scrophularia/classification , Solvents/chemistry , Structure-Activity Relationship , Rosmarinic Acid
15.
J Pharm Biomed Anal ; 165: 1-11, 2019 Feb 20.
Article En | MEDLINE | ID: mdl-30481579

Paeonia species have been valued for their ethnomedicinal uses in various countries and received much interest among the scientific community for their therapeutic properties, including anti-microbial, anti-inflammatory, anti-cancer, nephroprotective and hepatoprotective effects. The multiple phytotherapeutical applications of Paeonia species inspired us to establish the phytochemical fingerprint and to evaluate the biological properties of ethyl acetate, methanol, and aqueous extracts from the roots and aerial parts of two Paeonia species (P. arietina G. Anderson and P. kesrounansis Thiébaut). Phytoconstituents of P. arietina and P. kesrounansis extracts were analyzed using 1D and 2D NMR and LC-DAD-ESI-MS. The total content of phenolics (TPC) and flavonoids (TFC) in the extracts was also evaluated. The antioxidant activity was profiled using DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelation assays. Enzyme inhibitory properties were evaluated against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase. Phytochemical analysis of P. arietina and P. kesrounansis extracts showed the presence of galloyl esters of sugars, galloyl monoterpenes, and glycosylated flavonoids. The three solvent extracts presented different behavior in the bioassays. The highest antioxidant activity, tyrosinase and AChE inhibition were observed for the methanolic extract of the aerial parts of P. kesrounansis. In addition, the ethyl acetate extracts of the aerial parts of both plants were the most effective inhibitors of α-amylase. The highest BChE inhibition was observed for root methanolic extract of P. kesrounansis while the root ethyl acetate extract of P. arietina exerted the strongest inhibition of α-glucosidase. Methanol extract of P. kesrounansis aerial parts presented the highest TPC, while TFC was greatest in the corresponding extract of P. arietina. Our findings can be considered as a starting point for future studies to further validate the effectiveness and safety profiles of these plants in folk medicine.


Antioxidants/isolation & purification , Enzyme Inhibitors/isolation & purification , Paeonia/chemistry , Plant Extracts/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Chromatography, Liquid/methods , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Flavonoids/analysis , Flavonoids/isolation & purification , Phenols/analysis , Phenols/isolation & purification , Plant Components, Aerial , Plant Extracts/chemistry , Plant Roots , Solvents/chemistry , Spectrometry, Mass, Electrospray Ionization/methods
16.
Int J Environ Health Res ; 29(6): 607-621, 2019 Dec.
Article En | MEDLINE | ID: mdl-30569760

This study investigated into the phytochemical profile and biological properties of extracts (methanol and aqueous) of Origanum onites based on the antioxidant, enzyme inhibitory, and antibacterial activities. The aqueous extract exhibited higher antioxidant activities in the 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), ferric reducing antioxidant power, cupric reducing antioxidant capacity, phosphomolybdenum, and metal chelating assays, compared to the methanol extract. In contrast, the methanol extract was the most effective inhibitor of acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-amylase, and α-glucosidase. The methanol extract also showed higher antibacterial activity with highest inhibition against Escherichia coli (MIC = 6.25 mg/mL). The total phenolic content was higher in the aqueous extract while the methanol extract possessed higher total flavonoid content. A total of 28 and 18 compounds (belonging to polyphenols, flavonoids, terpenoids, and ester classes) were identified from the methanol and water extracts, respectively. These findings suggest that O. onites could be helpful in the management of oxidative stress-associated diseases including diabetes and neurodegenerative complications. Abbreviations: ABTS: 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid; ACAE: acarbose equivalent; AChE: acetylcholinesterase; AD: Alzheimer's disease; BChE: butyrylcholinesterase; CUPRAC: cupric reducing antioxidant capacity; DPPH: 1,1-diphenyl-2-picrylhydrazyl; EDTAE: EDTA equivalent; FRAP: ferric reducing antioxidant power; GAE: gallic acid equivalent; GALAE: galatamine equivalent; HPLC: high performance liquid chromatography; KAE: kojic acid equivalent; RE: rutin equivalents; TE: trolox equivalent; TPC: total phenolic content; TFC: total flavonoid content.


Origanum/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Anti-Bacterial Agents/analysis , Anti-Bacterial Agents/pharmacology , Antioxidants/analysis , Antioxidants/pharmacology , Chromatography, High Pressure Liquid , Enzyme Inhibitors/analysis , Enzyme Inhibitors/pharmacology , Flavonoids/analysis , Phenols/analysis , Tandem Mass Spectrometry
17.
J Pharm Biomed Anal ; 164: 581-589, 2019 Feb 05.
Article En | MEDLINE | ID: mdl-30466026

In the quest for new drugs of herbal origin, the ethyl acetate (EAE), methanol (ME), and water (WE) extracts of Crocus chrysanthus (Herb.) Herb. flowers were analyzed for their polyphenolic composition, antioxidant, and enzyme inhibitory potential. WE showed the highest antioxidant activities in all assays including metal chelating, phosphomolybdenum, FRAP, CUPRAC, ABTS and DPPH. EAE was the most effective enzyme inhibitor, exhibiting the highest inhibition against some enzymes linked to Alzheimer's disease (cholinesterases), diabetes mellitus (α-glucosidase and α-amylase) and hyperpigmentation problems (tyrosinase). The highest total phenolics (34.99 mg GAE/g) and flavonoids content (77.58 mg RE/g) were observed in WE and ME, respectively. Eight compounds were identified in EAE, 24 in ME, and 15 in WE. Kaempferol 3-O glucoside was found in all extracts. In conclusion, C. chrysanthus flowers can be suggested as a source of bioactive components with potential use against chronic disorders caused by oxidative stress. Future in-depth studies are recommended to determine the biological effects of isolated compounds from C. chrysanthus to identify the main compounds modulating the observed activities.


Antioxidants/pharmacology , Crocus/chemistry , Enzyme Inhibitors/pharmacology , Plant Extracts/pharmacology , Polyphenols/pharmacology , Antioxidants/chemistry , Antioxidants/isolation & purification , Chromatography, High Pressure Liquid/methods , Enzyme Assays/methods , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Flowers/chemistry , Oxidative Stress/drug effects , Plant Extracts/chemistry , Polyphenols/chemistry , Polyphenols/isolation & purification , Solvents/chemistry , Tandem Mass Spectrometry/methods
18.
J Pharm Pharmacol ; 71(2): 270-280, 2019 Feb.
Article En | MEDLINE | ID: mdl-30306560

OBJECTIVES: This study investigates into the biological effects of solvent extracts (ethyl acetate, methanol, and water) of Scutellaria orientalis L. and Scutellaria salviifolia Benth. based on its enzyme inhibitory activity and antioxidant ability together with the screening of bioactive compounds. METHODS: Total and individual bioactive components were determined using spectrophotometric and HPLC-ESI-MS methods. Six antioxidant assays were conducted and enzyme inhibition was tested against key enzymes linked to the pathology of common chronic disorders. KEY FINDINGS: Results revealed that the aqueous extracts of both plants exerted better 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid scavenging, reducing power, metal chelating, and α-glucosidase inhibitory activities. The methanol extracts showed highest tyrosinase inhibition and antioxidant activity in phosphomolybdenum assay while the less polar ethyl acetate extracts showed better acetylcholinesterase, butyrylcholinesterase, and α-amylase inhibition. Phytochemical evaluation by HPLC-ESI-MS revealed the presence of high amounts of flavones. CONCLUSIONS: Scutellaria orientalis and S. salviifolia are important sources of bioactive agents that warrants further studies.


Antioxidants/pharmacology , Enzyme Inhibitors/pharmacology , Plant Extracts/pharmacology , Scutellaria/chemistry , Antioxidants/isolation & purification , Chromatography, High Pressure Liquid/methods , Enzyme Inhibitors/isolation & purification , Solvents/chemistry , Species Specificity , Spectrometry, Mass, Electrospray Ionization/methods , Spectrophotometry/methods
19.
Int J Environ Health Res ; 29(5): 520-530, 2019 Oct.
Article En | MEDLINE | ID: mdl-30514101

This study explored the efficacy of the methanolic extract of three Asphodeline species (A. damascena subsp. rugosa, A. tenuior subsp. tenuiflora var. tenuiflora, and A. cilicica) to protect against hydrogen peroxide (H2O2)-induced lactate dehydrogenase (LDH) activity in HCT116 cells, and also any protective effects against lipopolysaccharides (LPS)-induced nitrite levels, prostaglandin E2 (PGE2) and 8-iso-prostaglandin F2α (8-iso-PGF2α) levels, 5HIAA/5-HT ratio, tumor necrosis factor (TNF)-α and interleukin (IL)-6 gene expression in rat colon specimens. Interestingly, A. tenuior extract was most effective in improving the tested biomarkers, by reducing LDH activity and nitrite level. On the other hand, A. damascena was the only species able to blunt LPS-induced TNF-α gene expression in rat colon specimens. The present findings highlighted the protective effects of Asphodeline extracts via in vitro and ex vivo models of inflammation and oxidative stress, adding new insights to the pharmacological actions of these medicinal plant species. Abbreviations: IBD: inflammatory bowel disease; LPS: lipopolysaccharide; LDH: lactate dehydrogenase; 5HIAA: 5-hydroxyindoleacetic acid; 5-HT: 5-hydroxytryptamine.


Asphodelaceae/chemistry , Colon/drug effects , Inflammation/metabolism , Oxidative Stress/drug effects , Plant Extracts/pharmacology , Protective Agents/pharmacology , Animals , Colon/metabolism , Gene Expression/drug effects , HCT116 Cells , Humans , Hydrogen Peroxide/toxicity , Inflammation/chemically induced , L-Lactate Dehydrogenase/metabolism , Lipopolysaccharides/toxicity , Male , Plant Extracts/chemistry , Protective Agents/chemistry , Rats , Rats, Sprague-Dawley
20.
J Pharm Biomed Anal ; 165: 374-380, 2019 Feb 20.
Article En | MEDLINE | ID: mdl-30590334

This study attempts to compare the pharmaceutical potential (antioxidant and key enzyme inhibition of clinical relevance) of organic and aqueous extracts of Parentucellia latifolia (L.) Caruel subsp. latifolia (L.) Caruel as well as phytochemical composition. The phytochemical compounds were evaluated by spectrophotometric methods (for total amounts) and HPLC-ESI-DAD-MSn (for individual compounds). The extracts were screened for antioxidant abilities by in vitro assays. Inhibition effects were also investigated against a set of enzymes linked to major health problems. Generally, the methanol (MeOH) and aqueous extracts displayed higher scavenging abilities on radicals and reductive effects when compared with the ethyl acetate (EtOAc) extract. On the other hand, the EtOAc extract was the most active inhibitor on cholinesterases (1.81-1.88 mg GALAE/g), amylase (0.70 mmol ACAE/g), glucosidase (2.85 mmol ACAE/g) and lipase (33.24 mg OE/g). The highest TPC was observed in the aqueous extract (25.07 mg GAE/g) while MeOH extract possessed the highest level of TFC (44.15 mg RE/g) and TPAC (3.46 mg CE/g). LC-MSn metabolite profiling indicated that loganin and its isomers, rutin, and luteolin-O-hexoside were the most abundant compounds. Our results suggest that P. latifolia may be valuable source of phyto-agents for the management of noncommunicable diseases.


Antioxidants/isolation & purification , Chromatography, High Pressure Liquid/methods , Iridoids/isolation & purification , Orobanchaceae/chemistry , Antioxidants/pharmacology , Enzyme Inhibitors/isolation & purification , Enzyme Inhibitors/pharmacology , Free Radical Scavengers/isolation & purification , Free Radical Scavengers/pharmacology , Iridoids/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology , Spectrometry, Mass, Electrospray Ionization/methods
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