scholarly journals Chemical constituents and their alpha-glucosidase inhibitory activity of Solanum procumbens

2021 ◽  
Vol 5 (3) ◽  
pp. 1326-1333
Author(s):  
Nhan Trung Nguyen ◽  
Truong Nhat Van Do ◽  
Tho Huu Le ◽  
Phu Hoang Dang ◽  
Hai Xuan Nguyen ◽  
...  

Solanum procumbens called ``Cà gai leo'' in Vietnam, belonged to the family of Solanaceae, which is a prickly diffuse, bright green perennial shrub, woody at the base. This plant has been sought for plenty of Vietnamese folk remedies for diseases such as rheumatism, back pain, detoxification, cough, pain relief, hemostasis, hepatitis, and cirrhosis. Chemical reports revealed the presence of lots of secondary metabolites such as steroids, triterpenoids, alkaloids, and phenolic compounds that have good biological activities such as antibacterial, antidiabetic, antioxidant, and antimicrobial... By column chromatography method together with thin layer normal-phase chromatography on the ethyl acetate extract of its entire plant, we isolated four compounds including dioscin (1), b -sitosterol (2), daucosterol (3) and 6'-O-acetyl-b -daucosterol (4). The result of theira-glucosidase inhibitory activity showed that compounds 2 and 4 had strong inhibition with IC50 values of 35.2 and 209.5 mM, comparing to the positive control, acarbose with an IC50 value of 214.5 mM. The results of this study have contributed to the scientific data of chemical compositions of Vietnamese medicinal plants, among them S. procumbens would potentially be developed as a plant-based drug to decrease the blood glucose level.

2021 ◽  
Vol 5 (3) ◽  
pp. 1334-1340
Author(s):  
Truong Nhat Van Do ◽  
Hai Xuan Nguyen ◽  
Tho Huu Le ◽  
Mai Thanh Thi Nguyen

Taxotrophis ilicifolius, called "Gai quít" in Vietnam, belonged to the family of Moraceae. The stems of T. ilicifolius are used in traditional medicine to cure pimples, anti-inflammatory, antibacterial... By column chromatography method together with thin layer chromatography on the ethyl acetate extract of its stems, six compounds were isolated including wogonin (1), 4-hydroxybenzoic acid (2), vanillic acid (3), vanillin (4), syringic acid (5), and syringaldehyde (6). Their chemical structures were elucidated by extensive NMR spectroscopic analysis and comparison with the literature data. The isolated compounds were tested fora-glucosidase inhibitory activity. All compounds showed more potent inhibitory activity with IC50 values 42–142 mM, than that of a positive control acarbose (IC50, 214.5 mM). Among all isolates, compounds 2, 4 and 6 exhibited significant a-glucosidase inhibitory activity with the IC50 values of 49.7, 42.6 and 55.9 mM, respectively. From the present investigation, all these compounds were isolated for the first time as well as their a-glucosidase inhibitoryactivity of T. ilicifolius. These results suggested that the traditional use of T. ilicifolius for the treatment of diabetes disease in Vietnam may be due to thea-glucosidase inhibitory activity of its phenolic constituents.


Author(s):  
Le Quy Thuong ◽  
Bach Tuyet Mai ◽  
Nguyen Minh Chau ◽  
Le Thi Phuong Hoa ◽  
Nguyen Quang Huy

Typhonium flagelliforme is a medicinal plant that has variety of uses. In medicinal traditional T. flagelliforme is used to treatment cough, headache, stomach pain chronic, and tracheitis. Moreover, use fresh bulbs treatment furuncle, the bites of poisonous insects. The active components in T. flagelliforme are flavonoids. In this study, the T. flagelliforme extract was obtained by methanol  to determine the chemical composition. Then, The extracts of methanol are extracted with polarization increases gradually solvents such as haxane, dichloromethane and ethyl acetate. Determination of antioxidant activity, cytotoxic activity of extracted fractions. Results obtained showed that the chemical compositions by the qualitative reaction preliminary were identified from T. flagelliforme containing reducing sugars, amino acids, organic acids, flavonoids, alcaloids, sterols. The antioxidant capacity of the ethyl acetate fraction reached 94.76 μg/ml, 10 times higher than the positive control is Quercetin. Cytotoxic activity of the haxane and diclomethane extracted fractions from T. flagelliforme exhibited cytotoxic activity on all three experimental cancers cell lines: KB, HepG2, Lu after 72h of culture with IC50 values ​​range from 92.8 to 107.76 μg/ml. From dichlomethane extracted of T. flagelliforme was purified TF1 as Stigmast-4-en- 3-on.    


Author(s):  
Huu Tho Le ◽  
Truc Thanh Thi Duong ◽  
Phu Hoang Dang ◽  
Truong Nhat Van Do ◽  
Hai Xuan Nguyen ◽  
...  

Salacia chinensis L., known as “Chop mao” in Vietnam, is a climbing shrub that belongs to the Celastraceae family. The stem of S. chinensis L. is used as a traditional medicine for the treatment of diabetes, rheumatoid arthritis, back pain, … The dried powdered stem of S. chinensis L. was collected in Phu Yen province and was extracted with methanol to yield methanol extract. The methanol extract was suspended in H2O and partitioned successively with n-hexane, CHCl3, EtOAc to obtain n-hexane, CHCl3, EtOAc, and H2O fractions, respectively. The CHCl3 fraction was subjected to a series of chromatographic separation to afford four purified compounds including 3-oxolup-20(29)-en-30-al (1), betulin-3-caffeate (2), 2-(4-hydroxy-3,5-dimethoxylphenyl)ethanol (3), and acetosyringone (4). Their structures were elucidated on the basis of the spectroscopic analysis and comparison with literature data. The isolated compounds were tested for their α-glucosidase inhibitory activity. The result indicated that all compounds (1-4) possessed significant α-glucosidase at the testing concentration of 100 µM with the percent inhibition values of 9.5 ± 1.3, 70.89 ± 0.25, 44.2 ± 1.6, and 6.7 ± 1.7 %, respectively. In addition, betulin-3-caffeate (2) and 2-(4-hydroxy-3,5-dimethoxylphenyl)ethanol (3) show more potent α-glucosidase inhibitory activity, with IC50 values of 69.7 and 152.0 µM, respectively, than that of positive control acarbose (IC50 = 214.5 µM).


2021 ◽  
Vol 23 (4) ◽  
Author(s):  
Thuy Thi Le Nguyen ◽  
Tung Thanh Bui ◽  
Phung Kim Phi Nguyen ◽  
Chi Minh Tran ◽  
Tu Dang Cam Phan ◽  
...  

Introduction: Bruguiera cylindrica is one of the mangrove plants belonging to Bruguiera genus. This genus is characterized by the presence of a large number of compounds, but the research on bioactivities has not been investigated so far. In the present research, the α-glucosidase inhibitory activity, as well as chemical constituents of the ethyl acetate extract of this plant, were studied. Methods: The chemical structures of two new compounds were elucidated by spectroscopic and computational methods. Results: Two new compounds, benzobrugierol (1) and bruguierine (2), were isolated from leaves of Bruguiera cylindrica (L.) Blume, together with nine known ones, including lupeol (3), betulin (4), chrysoeriol (5), glut-5-ene-3-ol (6), cholesta-4-ene-3-one (7), 3α-(Z)-coumaroyllupeol (8), 3α-(E)-coumaroyllupeol (9), 3β-hydroxycholesta-5-ene-7-one (10) and β-sitosterol 3-O-β-D-glucopyranoside (11). Extracts and some isolated compounds were evaluated for α-glucosidase inhibitory activities. Conclusion: The results showed that most of the extracts and tested compounds exhibited activities better than the positive control acarbose, especially two new compounds 1 and 2 with their IC50 values of 17.9 ± 0.4 and 34.6 ± 0.7 (mg/mL), respectively.


2011 ◽  
Vol 14 (2) ◽  
pp. 43-49
Author(s):  
Mai Thi Thanh Nguyen ◽  
Trong Nguyen Huu Phan ◽  
Hai Xuan Nguyen ◽  
Nhan Trung Nguyen

Our preliminary screening study revealed that the methanolic extract of Stholobus parviflorus (Roxb.) exhibited potent a-glucosidase inhibitory activity with an IC50 value of 0.05 μg mL-1. Therefore, we carried out activity-guided fractionation of the MeOH extract and isolated three compounds. These compounds were determinated as ferulic acid (1), protocatechuic acid (2) and epicatechin (3) by analysis of spectroscopic data. The IC50 values of these compounds were 45.30, 23.04 and > 100 μM, respectively. Acid tannic was used as a positive control with an IC50 value of 0.91 nM.


2018 ◽  
Vol 17 (3) ◽  
pp. 134-139
Author(s):  
R.M. Perez-Gutierrez

Methanol extract from Lippia graveolens (Mexican oregano) was studied in order to identify inhibitory bioactives for protein tyrosine phosphatase 1B (PTP1B). Known flavone as lutein (1), and another flavone glycoside such as lutein-7-o-glucoside (2), 6-hydroxy-lutein-7-ohexoside (3) and lutein-7-o-ramnoide (4) were isolated from methanol extract of aerial parts of the Lippia graveolens. All isolates were identified based on extensive spectroscopic data analysis, including UV, IR, NMR, MS and compared with spectroscopic data previously reported. These flavones were evaluated for PTP1B inhibitory activity. Among them, compounds 1 and 3 displayed potential inhibitory activity against PTP1B with IC50 values of 7.01 ± 1.25 μg/ml and 18.4 μg/ml, respectively. In addition, compound 2 and 4 showed moderate inhibitory activity with an IC50 value of 23.8 ± 6.21 and 67.8 ± 5.80 μg/ml respectively. Among the four compounds, luteolin was found to be the most potent PTP1B inhibitor compared to the positive control ursolic acid, with an IC50 value of 8.12 ± 1.06 μg/ml. These results indicate that flavonoids constituents contained in Lippia graveolens can be considered as a natural source for the treatment of type 2 diabetes.


Planta Medica ◽  
2021 ◽  
Author(s):  
Birgit Waltenberger ◽  
Françoise Lohézic-Le Dévéhat ◽  
Thi Huyen Vu ◽  
Olivier Delalande ◽  
Claudia Lalli ◽  
...  

AbstractProtein tyrosine phosphatase 1B plays a significant role in type 2 diabetes mellitus and other diseases and is therefore considered a new drug target. Within this study, an acetone extract from the lichen Stereocaulon evolutum was identified to possess strong protein tyrosine phosphatase 1B inhibition in a cell-free assay (IC50 of 11.8 µg/mL). Fractionation of this bioactive extract led to the isolation of seven known molecules belonging to the depsidones and the related diphenylethers and one new natural product, i.e., 3-butyl-3,7-dihydroxy-5-methoxy-1(3H)-isobenzofurane. The isolated compounds were evaluated for their inhibition of protein tyrosine phosphatase 1B. Two depsidones, lobaric acid and norlobaric acid, and the diphenylether anhydrosakisacaulon A potently inhibited protein tyrosine phosphatase 1B with IC50 values of 12.9, 15.1, and 16.1 µM, respectively, which is in the range of the protein tyrosine phosphatase 1B inhibitory activity of the positive control ursolic acid (IC50 of 14.4 µM). Molecular simulations performed on the eight compounds showed that i) a contact between the molecule and the four main regions of the protein is required for inhibitory activity, ii) the relative rigidity of the depsidones lobaric acid and norlobaric acid and the reactivity related to hydrogen bond donors or acceptors, which interact with protein tyrosine phosphatase 1B key amino acids, are involved in the bioactivity on protein tyrosine phosphatase 1B, iii) the cycle opening observed for diphenylethers decreased the inhibition, except for anhydrosakisacaulon A where its double bond on C-8 offsets this loss of activity, iv) the function present at C-8 is a determinant for the inhibitory effect on protein tyrosine phosphatase 1B, and v) the more hydrogen bonds with Arg221 there are, the more anchorage is favored.


2021 ◽  
Vol 63 (4) ◽  
pp. 42-46
Author(s):  
Thi-My-Linh Lam ◽  
◽  
Minh-Tuan Le ◽  
Manh-Ha Bui ◽  
◽  
...  

A study on the α-glucosidase inhibitory activity of 40 kinds of vegetables, tubers, and fruits found in the An Giang province was conducted. The results indicated that all 40 extracted samples displayed α-glucosidase inhibitory activity at a concentration of 250 μg ml-1, 36 extracted samples showed an inhibition rate greater than 50% at 250 μg ml-1, 25 extracted samples had over 50% at 100 μg ml-1, 17 extracted samples possessed more than 50% at 50 μg ml-1, 7 extracted samples sampled showed over 50% at 25 μg ml-1, 5 extracted samples were greater than 50% at 10 μg ml-1, and 1 extracted sample was greater than 50% at 1 μg ml-1. Among the 40 samples, those taken from the seeds of Areca catechu, the fruits of Cassia grandis, the fruits of Syzygium cumini, the seeds of Glycine max,andthe stems of Enydra fluctuansexhibited the strongest α-glucosidase inhibitory activity in methanol, with IC50 values of 0.15, 2.54, 4.05, 5.17 and 8.68 μg ml-1, respectively, which were stronger than the positive control acarbose with an IC50 value of 214.5 μg ml-1


Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1996 ◽  
Author(s):  
Ngoc Hong Nguyen ◽  
Thuy Trang Nguyen ◽  
Phu Cuong Ma ◽  
Qui Thanh Hoai Ta ◽  
Thuc-Huy Duong ◽  
...  

Bouea macrophylla is a tree widely grown throughout South East Asia. It is used in folk medicine for the treatment of various illnesses. The present study aimed to identify the chemical constituents and to test the antimicrobial and anticancer activities of an ethanol extract from B. macrophylla leaves. The extract exhibited excellent antibacterial properties against 9 out of 10 target microorganisms. including four Gram-negative bacteria (Escherichia coli, Shigella flexneri, Vibrio cholera, and Pseudomonas aeruginosa) and four Gram-positive bacteria (Staphylococcus aureus, Listeria monocytogenes, Enterococcus faecalis, and Bacillus cereus), as well as a fungus (Candida albicans). In addition, the extract was also tested on HeLa and human colorectal carcinoma (HCT116) cells to evaluate its cytostatic effects. The ethanol extract was able to inhibit the proliferation of HeLa and HCT116 cells, showing IC50 = 24 ± 0.8 and 28 ± 0.9 µg/mL, respectively, whereas the IC50 values of doxorubicin (standard) were 13.6 ± 1.3 and 15.8 ± 1.1 µg/mL respectively. Also, we identified various bioactive compounds in the extract such as polyphenols, flavonoids, caryophyllene, phytol, and trans-geranylgeraniol by GC-MS, which could contribute to the extract’s biological activities. Therefore, our findings strongly indicate that the constituents of the B. macrophylla ethanol extract could be active against the tested bacteria and fungi as well as cancer cells. Further investigation is needed to understand the mechanisms mediating the antimicrobial and anticancer effects and identify signaling pathways that could be targeted for therapeutic application.


Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3880 ◽  
Author(s):  
Nidal Jaradat ◽  
Nawaf Al-Maharik

The present study aimed to identify the chemical constituents and to assess the in-vitro, antimicrobial, anticancer, antioxidant, metabolic enzymes and cyclooxygenase (COX) inhibitory properties of essential oil (EO) of Stachys viticina Boiss. leaves. The S. viticina EO was isolated and identified using microwave-ultrasonic and GC-MS techniques, respectively. Fifty-two compounds were identified, of which endo-borneol was the major component, followed by eucalyptol and epizonarene. The EO was evaluated against a panel of in-vitro bioassays. The EO displayed antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA), Escherichia coli and Epidermophyton floccosum, with MIC values of 0.039, 0.078 and 0.78 mg/mL, respectively. The EO exhibited cytotoxicity against HeLa (cervical adenocarcinoma) and Colo-205 (colon) cancer cell lines with percentages of inhibition of 95% and 90%, for EO concentrations of 1.25 and 0.5 mg/mL, respectively. Furthermore, it showed metabolic enzyme (α-amylase, α-glucosidase, and lipase) inhibitory (IC50 = 45.22 ± 1.1, 63.09 ± 0.26, 501.18 ± 0.38 µg/mL, respectively) and antioxidant activity, with an IC50 value of 19.95 ± 2.08 µg/mL. Moreover, the S. viticina EO showed high cyclooxygenase inhibitory activity against COX-1 and COX-2 with IC50 values of 0.25 and 0.5 µg/mL, respectively, similar to those of the positive control (the NSAID etodolac). Outcomes amassed from this investigation illustrate that S. viticina EO represents a rich source of pharmacologically active molecules which can be further validated and explored clinically for its therapeutic potential and for the development and design of new natural therapeutic preparations.


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