Inhibition of Key Enzymes Linked to Obesity and Cytotoxic Activities of Whole Plant Extracts of Vernonia mesplilfolia Less

The whole plant of Vernonia mespilifolia is widely used as a traditional remedy for obesity in South Africa. The aim of this study was to investigate the anti-obesity and cytotoxic effects of Vernonia mespilifolia extracts in vitro. The α-amylase, α-glucosidase, and lipase inhibitory activities of aqueous and ethanol extracts of Vernonia mespilifolia were investigated, while the cytotoxic effects of these extracts were analyzed using Hoechst 33342 and propidium iodide (PI) dual staining on a human cervical HeLa cell line. The results showed that the LC50 (the concentration of a material will kill 50% of test organisms) values of aqueous and ethanol extracts of Vernonia mespilifolia were >200 and 149 µg/mL, respectively, to HeLa cells. Additionally, the ethanol extract exhibited the strongest inhibitory effect on the pancreatic lipase (Half-maximal inhibitory concentration (IC50) = 331.16 µg/mL) and on α-amylase (IC50 = 781.72 µg/mL), while the aqueous extract has the strongest α-glucosidase (IC50 = 450.88 µg/mL). Our results suggest that Vernonia mespilifolia’s acclaimed anti-obesity effects could be ascribed to its ability to inhibit both carbohydrate and fat digesting enzymes.

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In-vitro Control of Oral Thrush Causal Organisms Using Medicinal Plants Extracts

Notulae Scientia Biologicae ◽

10.15835/nsb11310443 ◽

2019 ◽

Vol 11 (3) ◽

pp. 376-382

Author(s):

Abosede M. EBABHI ◽

Adedotun A. ADEKUNLE ◽

Yoma I. OGHENERHABOKE

Keyword(s):

Medicinal Plants ◽

Jatropha Curcas ◽

Ethanolic Extract ◽

Ethanol Extract ◽

Zone Of Inhibition ◽

Test Organisms ◽

Zones Of Inhibition ◽

Oral Thrush ◽

Ethanol Extracts

Oral hygiene is important to the generality of the human healthcare system. For this, the antifungal activities of the aqueous and ethanol extracts of four medicinal plants of Jatropha curcas (stem), Eucaluptus golbulus (leaves), Vernonia amygdalina (stem) and Zanthoxylum zanthoxyloides (root) were carried out in vitro against three species of Candida associated with oral thrush namely C. albicans, C. glabrata, C. tropicalis using the disc diffusion agar assay. The zones of inhibition varied with the test organisms as well as the extracts. The ethanolic extract of Jatropha curcas showed the highest zone of inhibition of 10.88 ± 0.22 mm against C. albicans while the least zone of inhibition (6.13 ± 0.13 mm) was exhibited by the ethanol extract of Z. zanthoxyloides on C. glabrata. The preliminary phytochemical screening showed the presence of tannin, saponin, alkaloids, flavonoids and reducing sugar in all plant samples. This study can be further used as a foundation for the screening of phytochemical constituents by pharmaceuticals for the control and eradication of oral thrush.

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Metabolomic Screening of Anti-Inflammatory Compounds from the Leaves of Actinidia arguta (Hardy Kiwi)

Foods ◽

10.3390/foods8020047 ◽

2019 ◽

Vol 8 (2) ◽

pp. 47 ◽

Cited By ~ 4

Author(s):

Gyoung-Deuck Kim ◽

Jin Lee ◽

Joong-Hyuck Auh

Keyword(s):

Nitric Oxide ◽

Ethanol Extract ◽

Inhibitory Effect ◽

Reversed Phase ◽

No Production ◽

Actinidia Arguta ◽

Bioassay Guided Fractionation ◽

Anti Inflammatory ◽

Ethanol Extracts

The metabolomic screening of potential anti-inflammatory compounds in the leaves of Actinidia arguta was performed by using LC-MS/MS. Ethanol extracts were prepared, and the anti-inflammatory effects were investigated based on nitric oxide (NO) synthesis and inducible nitric oxide synthase expression in lipopolysaccharide-induced RAW 264.7 macrophages. The 75% ethanol extract showed the highest inhibitory effect on nitric oxide (NO) production, and it was further separated by in vitro bioassay-guided fractionation using preparative LC with reversed-phase column separation. Through multiple steps of fractionation, sub-fraction 1-3 was finally purified, and caffeic acid derivatives, such as caffeoylthreonic acid and danshensu (salvianic acid A), were successfully identified as key anti-inflammatory compounds by LC-MS/MS and metabolomics analyses. This is the first study identifying anti-inflammatory compounds in A. arguta (Actinidia arguta) leaves through bioassay-guided fractionation and metabolomics screening. Results of this study would be useful for the application of A. arguta leaves as a nutraceutical.

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Antileishmanial and cytotoxic activities of four Andean plant extracts from Colombia

Veterinary World ◽

10.14202/vetworld.2020.2178-2182 ◽

2020 ◽

Vol 13 (10) ◽

pp. 2178-2182

Author(s):

Wilson Cardona-G ◽

Sara Robledo ◽

Fernando Alzate ◽

Andrés F. Yepes ◽

Cristian Hernandez ◽

...

Keyword(s):

Ethyl Acetate ◽

Plant Extracts ◽

Ethyl Acetate Extract ◽

Ethanol Extract ◽

Cytotoxic Activities ◽

Moderate Activity ◽

Leishmania Panamensis ◽

Ethanol Extracts ◽

Ethyl Acetate Extracts

Background and Aim: Licania salicifolia (L.S) Cuatrec., Persea ferruginea (P.F) Kunth, Oreopanax floribundus (O.F), and Psychotria buchtienii (P.B) belong to the families Chrysobalanaceae, Lauraceae, Araliaceae, and Rubiaceae, respectively, which have been used as medicines by communities in the Andes. This study evaluated the leishmanicidal and cytotoxic activities of alcohol and non-alcohol extracts from four Andean plant extracts (L.S, O.F, P.F, and P.B). Materials and Methods: Extracts were obtained by percolation with solvents of different polarities – hexane, dichloromethane, ethyl acetate, and ethanol. Phytochemical screening was conducted based on reported methods. All products were evaluated in vitro to determine the leishmanicidal activity against amastigotes of Leishmania panamensis and cytotoxicity against U937 cells. Results: Flavonoids, triterpenes, and tannins were the main secondary metabolites found. From the results, dichloromethane extracts from O.F and P.B, ethanol extract from P.B, and ethyl acetate extracts of all plants were active, with EC50 <30 μg/mL. Ethyl acetate was the most active extract, which showed EC50 values of 9.8, 14.1, 23.7, and 25.5 μg/mL, for L.S, P.B, O.F, and P.F, respectively. Hexane extracts from P.B and O.F exhibited moderate activity with EC50 values of 84.8 and 87.4 μg/mL, respectively. Hexane and ethanol extracts from O.F, ethyl acetate, and ethanol extracts from L.S, and all extracts from P.F were not toxic. Alternatively, hexane and dichloromethane extracts from L.S and P.B as well as dichloromethane and ethyl acetate extracts from O.F displayed high toxicity. Conclusion: Based on the activity we observed, ethyl acetate extract can continue in its usage in the search for new antileishmanial drugs, mainly ethyl acetate extract from L.S showed activity comparable to meglumine antimoniate and was not cytotoxic.

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Tyrosinase Inhibitory Effect and Antioxidative Activities of Fermented and Ethanol Extracts ofRhodiola roseaandLonicera japonica

The Scientific World JOURNAL ◽

10.1155/2013/612739 ◽

2013 ◽

Vol 2013 ◽

pp. 1-5 ◽

Cited By ~ 8

Author(s):

Yuh-Shuen Chen ◽

Hua-Chian Liou ◽

Chin-Feng Chan

Keyword(s):

Biological Activities ◽

Ethanol Extract ◽

Inhibitory Effect ◽

Rhodiola Rosea ◽

Lonicera Japonica ◽

Inhibitory Effects ◽

Scavenging Effect ◽

Ethanol Extracts ◽

Dpph Scavenging

This is the first study to investigate the biological activities of fermented extracts ofRhodiola roseaL. (Crassulaceae) andLonicera japonicaThunb. (Caprifoliaceae).Alcaligenes piechaudiiCC-ESB2 fermented and ethanol extracts ofRhodiola roseaandLonicera japonicawere prepared and the antioxidative activities of different concentrations of samples were evaluated usingin vitroantioxidative assays. Tyrosinase inhibition was determined by using the dopachrome method with L-DOPA as substrate. The results demonstrated that inhibitory effects (ED50values) on mushroom tyrosinase of fermentedRhodiola rosea, fermentedLonicera japonica, ethanol extract ofLonicera japonica,and ethanol extract ofRhodiola roseawere 0.78, 4.07, 6.93, and >10 mg/ml, respectively. The DPPH scavenging effects of fermentedRhodiola rosea(ED50= 0.073 mg/ml) and fermentedLonicera japonica(ED50= 0.207 mg/ml) were stronger than effects of their respective ethanol extracts. Furthermore, the scavenging effect increases with the presence of high content of total phenol. However, the superoxide scavenging effects of fermentedRhodiola roseawas less than effects of fermentedLonicera japonica. The results indicated that fermentation ofRhodiola roseaandLonicera japonicacan be considered as an effective biochemical process for application in food, drug, and cosmetics.

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Different Morphotypes of Fusarium oxysporum Isolated from Xanthosoma sagittifolium L. Schott Roots: Action of Ethanol Leaf Extracts of Psidium guajava on their in Vitro Inhibition and on X. Sagittifolium Plants Inoculated with F. oxysporum

International Journal of Pathogen Research ◽

10.9734/ijpr/2020/v5i430142 ◽

2020 ◽

pp. 25-41

Author(s):

A. C. Djeuani ◽

H. D. Mbouobda ◽

T. A. Mbekem ◽

N. Niemenak

Keyword(s):

Fusarium Oxysporum ◽

Ethanol Extract ◽

Maximum Growth ◽

Psidium Guajava ◽

Inhibitory Effect ◽

Leaf Extracts ◽

Xanthosoma Sagittifolium ◽

In Vitro Inhibition ◽

Ethanol Extracts

The objective of this study was to determine the different morphotypes of Fusarium oxysporum present in the root of Xanthosoma sagittifolium and evaluate the effect of alcoholic extracts of Psidium guajava on their in vitro inhibition. Strains of Fusarium oxysporum were collected in eight localities where X. sagittifolium is grown. Fusarium strains isolated from roots of X. sagittifolium harvested in each locality were grown on PDA medium. The antifungal test was evaluated using ethanol extracts from P. guajava leaves at 30 and 60%. The virulence test of each strain on young plants of X. sagittifolium aged three months were realized. Eight strain of Fusarium oxysporum were successfully isolated. After maximum growth, five morphological types were observed (pionnotal, sclerotic, clowny, cottony and ras senescent). The cottony strain was abundant and present in all the locality. Histological analysis of the different strains obtained revealed the presence of septate or siphoned hyphae and three types of conidia (microconidia, macroconidia and sporangiospores or chlamidospores). The inhibition tests were very high with 60% of ethanol extract of P. guajava, and 83.33% of inhibitory effect were observed after eight days of growth, in the strains collected in X. sagittifolium roots, in L3 (Loum) and L4 (Bangoua) localities. After infection of X. sagittifolium plants with each strain of F. oxysporum isolated, symptoms observed were yellowing and wilting of leaves. However, plants inoculated with the L3 (Loum) strain showed both yellowing and wilting of leaves. The application of ethanol extracts from P. guajava leaves reduced the severity of the disease in the inoculated plants after 14 days. These results obtained showed that F. oxysporum is not only saprophytic fungi, it’s also able to induce yellowing and wilting of leaves in X. sagittifolium.

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UJI IN VITRO EKSTRAK AIR DAN ETANOL DARI BUAH ASAM GELUGUR, RIMPANG LENGKUAS, DAN KENCUR SEBAGAI INHIBITOR AKTIVITAS LIPASE PANKREAS

Jurnal Sains dan Teknologi Indonesia ◽

10.29122/jsti.v12i1.845 ◽

2012 ◽

Vol 12 (1) ◽

Author(s):

Dyah Iswantini ◽

Latifah K. Darusman ◽

Ana Fitriyani

Keyword(s):

Body Weight ◽

Pancreatic Lipase ◽

Lipase Activity ◽

Water Extract ◽

Ethanol Extract ◽

Inhibitory Effect ◽

Positive Control ◽

Reduce Body Weight ◽

Ethanol Extracts

Asam gelugur fruits of Garcinia often used to reduce body weight. Lengkuas and kencur are traditional herbal that potential for antiobesity because they could reduce the level of phospholipids, triglycerides, and cholesterol. The aim of the research was to evaluate the potencies of these herbal as antiobesity by measurement of their water and ethanol extracts capabilities as in vitro inhibitor of pancreatic lipase activity. The water and ethanol extracts of asam gelugur fruits contained saponins and alkaliods, respectively. The water extract of lengkuas rhizomes contained alkaloids, flavonoids, saponins, and quinones, while the ethanol extract contained alkaloids, flavonoids, saponins, and steroids. The water extract of kencur rhizomes contained saponins and quinones, while the ethanolextract contained alkaloids, flavonoids, steroids, and quinones. The highest inhibitory effect of all extracts was obtained from the ethanol extract of asam gelugur fruits with value of 86.3% at 150 ppm. The highest inhibitory effect of lengkuas extracts was from the ethanol extract at 200 ppm (56.2%). The highestinhibitory effect of kencur was showed by the ethanol extract with the value 37.6% at 300 ppm. These values were higher than the inhibitory effect of the positive control (Xenical®) at 100 ppm (10.6%).

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Inhibisi Lipase Pankreas secara In Vitro oleh Ekstrak Air dan Etanol Daun Asam Jawa (Tamarindus indica) dan Rimpang Kunci Pepet (Kaempferiae rotundae)

Jurnal Natur Indonesia ◽

10.31258/jnat.13.2.146-154 ◽

2012 ◽

Vol 13 (2) ◽

pp. 146

Author(s):

Dyah Iswantini Pradono ◽

Latifah Kosim Darusman ◽

Ai Susanti

Keyword(s):

Body Weight ◽

Pancreatic Lipase ◽

Water Extract ◽

Ethanol Extract ◽

Inhibitory Effect ◽

Sesame Oil ◽

Tamarindus Indica ◽

Reduce Body Weight ◽

Ethanol Extracts

Tamarind and kunci pepet has been used traditionally as herbal medicine to reduce body weight or used asantiobesity. But the mechanism in vitro of this herbal in reducing body weight has not been known yet. Theobjective of this research is to evaluate these herbal as antiobesity by their water and ethanol extracts capabilityin inhibiting pancreatic lipase activity in vitro at pH 8, incubation time 45 minutes, and temperature 400C. Pancreaticlipase used in this research was human pancreatic lipase with concentration of 1.4 × 10-5 μg/μl and the substratewas sesame oil with concentration of 16.2 μg/μl. The water and ethanol extracts of tamarind leaves containedalkaloids, flavonoids, saponins, steroids, and tannins. Water extract of kunci pepet contained alkaloids, flavonoids,saponins, and tannins, while ethanol extract contained alkaloids, flavonoids, saponins, and triterpenoids. Theresults of tamarind leaves extracts showed that ethanol extract in concentration of 150 ppm had the highestinhibitory effect, with the value of 49.0%. Water extract of kunci pepet at concentration of 200 ppm had the highestinhibition, with the value of 65.1%. These values were higher than inhibitory effect of Xenical® 100 ppm as thepositive control, with the inhibition value of 10.6%.

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Synergistic Antitumor Effect of 5-Fluorouracil Combined with Constituents from Pleurospermum lindleyanum in Hepatocellular carcinoma SMMC-7721 Cells

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520620666200824094624 ◽

2020 ◽

Vol 20 ◽

Author(s):

Xiao-Feng Zhu ◽

Xiao-Jin Li ◽

Zhong-Lian Cao ◽

Xiu-Jie Liu ◽

Ping Yang ◽

...

Keyword(s):

Hepatocellular Carcinoma ◽

Treatment Effectiveness ◽

Synergistic Effects ◽

Folk Medicine ◽

Inhibitory Effect ◽

Caspase 9 ◽

Whole Plant ◽

Anti Cancer ◽

Induced Apoptosis

Background: A Chinese folk medicine plant Pleurospermum lindleyanum possesses pharmacological activities of heat-clearing, detoxifying and preventing from hepatopathy, coronary heart disease, hypertension, and high altitude sickness. We isolated and characterized its constituents to investigate its synergistic effects against human hepatoma SMMC-7721 cells. Objective: The aim of this study was to explore the synergistic anti-cancer activities of isolates from P. lindleyanum with 5-FU on hepatoma SMMC-7721 cells in vitro and their primary mechanisms. Methods: Sequential chromatographic techniques were conducted for the isolation studies. The isolates structures were established by spectroscopic analysis as well as X-ray crystallographic diffraction. Growth inhibition was detected by MTT assay. The isobologram method was used to assess the effect of drug combinations. Flow cytometry and western blot were used to examine apoptosis and protein expression. Results: A new coumarin (16), along with sixteen known compounds, were isolated from the whole plant of P. lindleyanum and their structures were elucidated by spectroscopic methods. Four coumarins (2, 3, 5, and 16), two flavonoids (8 and 9) and three phytosterols and triterpenes (12-14) were found to synergistically enhance the inhibitory effect of 5-FU against SMMC-7721 cells. Among them, compounds 3 and 16 exhibited the best synergistic effects with IC50 of 5-FU reduced by 16-fold and 22-fold possessing the minimum Combination Index (CI) 0.34 and 0.27. The mechanism of action of combinations might be through synergistic arresting for the cell cycle at G1 phases and the induction of apoptosis. Moreover, western blotting and molecular docking revealed that compounds 3 or 5 might promote 5-FU-induced apoptosis by regulating the expression of Caspase 9 and PARP. Conclusion: Constituents from P. lindleyanum may improve the treatment effectiveness of 5-FU against hepatocellular carcinoma cells.

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Evaluation of Snake Venom’s PhospholipaseA2 Enzyme Inhibition Activity of Cyphostemma adenocoule

Current Chemical Biology ◽

10.2174/2212796814999200917114914 ◽

2020 ◽

Vol 14 (3) ◽

pp. 196-202

Author(s):

Atul Kaushik ◽

Teamrat S. Tesfai ◽

Daniel K. Barkh ◽

Furtuna K. Ghebremeskel ◽

Habtom G. Zerihun ◽

...

Keyword(s):

Enzyme Inhibition ◽

Snake Venom ◽

Ethanol Extract ◽

Egg Yolk ◽

Chloroform Extract ◽

Inhibition Activity ◽

Traditional Use ◽

Snake Bites ◽

Ethanol Extracts

Background: A snake bite is fundamentally an injury often resulting in puncture wounds meted out by the animal's fangs and occasionally resulting in envenomation. Rate of snake bites around 5,400,000 bites per year leads to over 2,500,000 envenomings and around 125,000 fatal cases annually. Snake venom enzymes are rich in metalloproteinases, phospholipaseA2, proteinases, acetylcholinesterases and hyaluronidases. Objective: Cyphostemma adenocoule is traditionally being used for the treatment of snake bites in Eritrea. The present research was aimed at evaluating the snake venom enzyme inhibition activity of C. adenocoule against puff adder venom and developing a base for the traditional use of the plant against snakebites in Eritrea. Methods: The anti-venom activity of C. adenocoule was assessed in-vitro through phospholipaseA2 enzyme inhibition assay using egg yolk as a cell. The ethanol and chloroform extracts of C. adenocoule showed in vitro anti phospholipase A2 activity, whereas the water extracts of the plant showed no activity. Results: Among the extracts of C. adenocoule, the highest percentage of inhibition was obtained from chloroform extract (95.55% at 100mg/ml). The extract showed prominent activity at different concentrations (34.7% at10mg/ml, 48.8% at 20mg/ml, 54.8% at 40mg/ml, 60.9% at 60mg/ml, 80.5% at 80mg /ml). The ethanol extract also showed certain activity at various concentrations (25.22% at10mg/ml, 14.78% at 20mg/ml, 2.6% at40mg/ml). The activity of the chloroform extracts increases as concentration increases, whereas the activity of the ethanol extracts decreases as concentration increases. The aqueous extract of C. adenocoule did not show any activity at all concentrations. Conclusion: In this study, the chloroform and ethanol extracts of the plant inhibited the enzyme of interest and thus proved the efficacy of anti-snake venom activity of the plant.

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In Vitro Cytotoxic Effects of Secondary Metabolites Present in Sarcopoterium Spinosum L.

Applied Sciences ◽

10.3390/app11115300 ◽

2021 ◽

Vol 11 (11) ◽

pp. 5300

Author(s):

Jozef Hudec ◽

Jan Mojzis ◽

Marta Habanova ◽

Jorge A. Saraiva ◽

Pavel Hradil ◽

...

Keyword(s):

Mammary Gland ◽

Ethyl Acetate ◽

Cytotoxic Activity ◽

Cell Lines ◽

Benzalkonium Chloride ◽

Ethanol Extract ◽

Cytotoxic Activities ◽

Sarcopoterium Spinosum ◽

Mcf 7

Sarcopoterium spinosum (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of S. spinosum were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC50 8.10−7 M) and MCF-7 cells (IC50 5.10−6 M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of S. spinosum remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.

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