scholarly journals In vitro α-glucosidase inhibitory activity of compounds isolated from mangrove Lumnitzera littorea leaves

2019 ◽  
Vol 22 (1) ◽  
Author(s):  
Thuy Thi Le Nguyen ◽  
Thuy Thi Pham ◽  
Poul Erik Hansen ◽  
Phung Kim Phi Nguyen
Keyword(s):  
Oleanolic Acid ◽  
Inhibitory Activity ◽  
Mangrove Forest ◽  
2D Nmr ◽  
Positive Control ◽  
Spectroscopic Methods ◽  
Corosolic Acid ◽  
Ic50 Values ◽  
Alpha Glucosidase

Introduction: Lumnitzera littorea grown at CanGio Mangrove Forest has been investigated. The present study reports the isolation, characterization and evaluation of the alpha-glucosidase inhibitory activity of isolated compounds from Lumnitzera littorea leaves. Methods: Their structures were elucidated by spectroscopic methods (including MS, 1D and 2D–NMR) and comparison with values from the literature. From the n-hexane extract, nine compounds including lupeol (1), betulin (2), betulinic acid (3), oleanolic acid (4), corosolic acid (5), -sitosterol (6), beta-sitosterol 3-O- beta-D-glucopyranoside (7), stigmast-5-ene-3beta-O-(6-O-hexadecanoyl-beta-D-glucopyranoside) (8), and stigmast-4-ene-3-one (9) were isolated and identified. Results: The results of the alpha-glucosidase inhibitory activity showed thatcorosolic acid (5) and oleanolic acid (4) were the most potent, with IC50 values of 17.86 +/- 0.42 and 18.82 +/- 0.59 ug/mL, respectively. Five of the other seven compounds exhibited inhibitory activity with IC50 values below 100 ug/mL, and higher than the positive control acarbose (127.64 +/- 0.64 ug/mL).  

α-Glucosidase Inhibitory Depsidones from the Lichen Parmotrema tsavoense

Planta Medica ◽  
2020 ◽  
Vol 86 (11) ◽  
pp. 776-781 ◽  
Author(s):  
Thuc-Huy Duong ◽  
Tai-Xuan-Hoa Hang ◽  
Pierre Le Pogam ◽  
Thanh-Nha Tran ◽  
Dinh-Hung Mac ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
2D Nmr ◽  
Positive Control ◽  
Chemical Investigation ◽  
Spectroscopic Methods ◽  
Nmr Data ◽  
Ic50 Values

AbstractChemical investigation of the lichen Parmotrema tsavoense led to the isolation of 5 new depsidones, parmosidones F – J (1 – 5). These compounds were structurally elucidated using spectroscopic methods including HRESIMS and 2D NMR data. Compounds 1, 3, and 4 were evaluated for their inhibition of α-glucosidase. All exhibited potent α-glucosidase inhibitory activity with IC50 values ranging from 10.7 to 17.6 µM, which was much lower than that of the positive control acarbose (IC50 449 µM).

Homoadamantane and Adamantane Acylphloroglucinols from Hypericum hirsutum

Planta Medica ◽  
2021 ◽  
Author(s):  
Julianna Max ◽  
Jörg Heilmann
Keyword(s):  
Petroleum Ether Extract ◽  
2D Nmr ◽  
Positive Control ◽  
Ionization Mass ◽  
2D Nmr Spectroscopy ◽  
Vitro Assay ◽  
Ionization Mass Spectroscopy ◽  
Ic50 Values ◽  
Adamantane Skeleton

Abstract 1H NMR-guided fractionation of the petroleum ether extract of the aerial parts from Hypericum hirsutum yielded to the isolation of 19 polyprenylated polycyclic acylphloroglucinols. Structure elucidation based on 1D and 2D NMR spectroscopy together with high-resolution electrospray ionization mass spectroscopy revealed 14 acylphloroglucinols with a homoadamantane scaffold (1–14), while 5 further compounds showed an adamantane skeleton (15–19). Except for hookerione C (15), all isolated metabolites are hitherto unknown. While structurally-related metabolites have been isolated from other Hypericum species, it is the first report of admantan and homoadamantan type acylphloroglucinols in section Taeniocarpium Jaub. & Spach (Hypericaceae). The isolated compounds have been tested in a crystal violet-based in vitro assay on their properties to reduce the proliferation of human microvascular endothelial cells compared to hyperforin as the positive control. They showed a moderate reduction of proliferation with IC50 values in the range ~ 3 – 22 µM, with the homoadamantane-based compounds 2 and 4 being the most active. In addition, inhibition of the TNF-α-induced ICAM-1 expression was determined for 1 – 5, 7, and 10 – 12. Substances 3 and 12 reduced the ICAM-1 expression significantly (to 46.7% of control for 3, 62.3% for 12, at 50 µM).

scholarly journals Structure Revision and Protein Tyrosine Phosphatase Inhibitory Activity of Drazepinone

Marine Drugs ◽  
2021 ◽  
Vol 19 (12) ◽  
pp. 714
Author(s):  
Fei Cao ◽  
Li Pan ◽  
Wen-Bin Gao ◽  
Yun-Feng Liu ◽  
Cai-Juan Zheng ◽  
...  
Keyword(s):  
Detailed Analysis ◽  
Protein Tyrosine Phosphatase ◽  
Inhibitory Activity ◽  
Chemical Shifts ◽  
Tyrosine Phosphatase ◽  
2D Nmr ◽  
Nmr Data ◽  
Structure Revision ◽  
Ic50 Values

From the marine-derived fungus Penicillium sumatrense (Trichocomaceae), a pair of enantiomers [(+)-1 and (−)-1] were isolated with identical 1D NMR data to drazepinone, which was originally reported to have a trisubstituted naphthofuroazepinone skeleton. In this study, we confirmed the structures of the two enantiomers as drazepinone and revised their structures by detailed analysis of extensive 2D NMR data and a comparison of the calculated 13C chemical shifts, ECD, VCD, and ORD spectra with those of the experiment ones. (+)-1 and (−)-1 were evaluated for their PTP inhibitory activity in vitro. (−)-1 showed selective PTP inhibitory activity against PTP1B and TCPTP with IC50 values of 1.56 and 12.5 μg/mL, respectively.

Phenylpropanoid and Iridoid Glucosides from the Whole Plant of Hemiphragma heterophyllum and Their alpha-Glucosidase Inhibitory Activities

Planta Medica ◽  
2020 ◽  
Vol 86 (03) ◽  
pp. 205-211
Author(s):  
Yan-Hong Li ◽  
Jia-Meng Dai ◽  
Cui Yang ◽  
Meng-Yuan Jiang ◽  
Yong Xiong ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Ethanol Extract ◽  
2D Nmr ◽  
Positive Control ◽  
Iridoid Glucoside ◽  
2D Nmr Spectroscopy ◽  
Whole Plant ◽  
Ic50 Value ◽  
Iridoid Glucosides ◽  
Alpha Glucosidase

AbstractThree phenylpropanoid glucosides (1 – 3) and one iridoid glucoside (11), together with eleven known glucosides, were isolated from the ethanol extract of the whole plant of Hemiphragma heterophyllum. Their structures were elucidated by means of 1D and 2D NMR spectroscopy, HRMS, and chemical methods. All compounds except 11 and 13 – 15 showed varying degrees of α-glucosidase inhibitory activity. Compounds 5, 9, and 12 were marginally active in the bioassay, while compounds 1 – 4, 6 – 8, and 10 exhibited appreciable inhibitory activity with an IC50 value of 33.6 ~ 83.1 µM, which was much lower than that of the positive control acarbose (IC50 = 310.8 µM).

scholarly journals Chemical Constituents of the Deep-Sea-Derived Penicillium solitum

Marine Drugs ◽  
2021 ◽  
Vol 19 (10) ◽  
pp. 580
Author(s):  
Zhi-Hui He ◽  
Jia Wu ◽  
Lin Xu ◽  
Man-Yi Hu ◽  
Ming-Ming Xie ◽  
...  
Keyword(s):  
Deep Sea ◽  
Chemical Constituents ◽  
A549 Cells ◽  
Acid Methyl Ester ◽  
2D Nmr ◽  
Positive Control ◽  
Ic50 Values ◽  
Penicillium Solitum ◽  
New Compounds

A systematic chemical investigation of the deep-sea-derived fungus Penicillium solitum MCCC 3A00215 resulted in the isolation of one novel polyketide (1), two new alkaloids (2 and 3), and 22 known (4–25) compounds. The structures of the new compounds were established mainly on the basis of exhaustive analysis of 1D and 2D NMR data. Viridicatol (13) displayed moderate anti-tumor activities against PANC-1, Hela, and A549 cells with IC50 values of around 20 μM. Moreover, 13 displayed potent in vitro anti-food allergic activity with an IC50 value of 13 μM, compared to that of 92 μM for the positive control, loratadine, while indole-3-acetic acid methyl ester (9) and penicopeptide A (10) showed moderate effects (IC50 = 50 and 58 μM, respectively).

scholarly journals IN VITRO ALPHA-GLUCOSIDASE INHIBITORY ACTIVITY OF EGYPTIAN PLANT EXTRACTS AS AN INDICATION FOR THEIR ANTIDIABETIC ACTIVITY

2018 ◽  
Vol 11 (7) ◽  
pp. 360 ◽  
Author(s):  
May A El-manawaty ◽  
Lamiaa Gohar
Keyword(s):  
Plant Extracts ◽  
Inhibitory Activity ◽  
The Body ◽  
Antidiabetic Activity ◽  
Pinus Roxburghii ◽  
Systematic Screening ◽  
Ic50 Values ◽  
Rich Flora ◽  
Alpha Glucosidase

Objective: Diabetes mellitus is a highly prevalent chronic disease in Egypt leading to high socioeconomic problems, especially in the cities due to the unhealthy life style. Although many drugs are available, they have many side effects. Furthermore, the body arouses resistance after a while for the drug so it should be changed every once in a while. Plants could be a good source for drugs. In Egypt, we have a rich flora which has not been subjected to systematic screening for antidiabetic activity.Methods: The aim of this work was to screen 264 plant extracts for their in vitro α-glucosidase inhibitory activity. Those extracts which gave more than 70% inhibition were screened on different concentrations and their inhibitory concentrations giving 50% activity (IC50) were calculated.Results: Out of all the tested extracts, 63 gave more than or equal 70% inhibition on α-glucosidase at the tested concentration (25 ppm). After the calculation of the IC50 values, 10 extracts were chosen for further study having 5 ppm and less IC50.Conclusion: The most active plant extract is Pinus roxburghii Sarg. branches (IC50 is 2.47 ppm).

scholarly journals Preparation, COX-2 Inhibition and Anticancer Activity of Sclerotiorin Derivatives

Marine Drugs ◽  
2020 ◽  
Vol 19 (1) ◽  
pp. 12
Author(s):  
Tao Chen ◽  
Yun Huang ◽  
Junxian Hong ◽  
Xikang Wei ◽  
Fang Zeng ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Inhibitory Activity ◽  
Positive Control ◽  
Human Lung Cancer ◽  
Binding Modes ◽  
Ic50 Values ◽  
Cox 2 ◽  
Inhibitory Agents

The latest research has indicated that anti-tumor agents with COX-2 inhibitory activity may benefit their anti-tumor efficiency. A series of sclerotiorin derivatives have been synthesized and screened for their cytotoxic activity against human lung cancer cells A549, breast cancer cells MDA-MB-435 using the MTT method. Among them, compounds 3, 7, 12, 13, 15, 17 showed good cytotoxic activity with IC50 values of 6.39, 9.20, 9.76, 7.75, 9.08, and 8.18 μM, respectively. In addition, all compounds were tested in vitro the COX-2 inhibitory activity. The results disclosed compounds 7, 13, 25 and sclerotiorin showed moderate to good COX-2 inhibition with the inhibitory ratios of 58.7%, 51.1%, 66.1% and 56.1%, respectively. Notably, compound 3 displayed a comparable inhibition ratio (70.6%) to the positive control indomethacin (78.9%). Furthermore, molecular docking was used to rationalize the potential of the sclerotiorin derivatives as COX2 inhibitory agents by predicting their binding energy, binding modes and optimal orientation at the active site of the COX-2. Additionally, the structure-activity relationships (SARS) have been addressed.

scholarly journals Two new compounds from leaves of Bruguiera cylindrica (L.) Blume with the in vitro α-glucosidase inhibitory activity

2021 ◽  
Vol 23 (4) ◽  
Author(s):  
Thuy Thi Le Nguyen ◽  
Tung Thanh Bui ◽  
Phung Kim Phi Nguyen ◽  
Chi Minh Tran ◽  
Tu Dang Cam Phan ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Ethyl Acetate Extract ◽  
Chemical Constituents ◽  
Positive Control ◽  
Chemical Structures ◽  
Ic50 Values ◽  
Bruguiera Cylindrica ◽  
New Compounds ◽  
Better Than

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.

scholarly journals Novel Polyketides Produced by the Endophytic Fungus Aspergillus Fumigatus from Cordyceps Sinensis

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1709 ◽  
Author(s):  
Da-Le Guo ◽  
Xiao-Hua Li ◽  
Dan Feng ◽  
Meng-Ying Jin ◽  
Yu-Mei Cao ◽  
...  
Keyword(s):  
Aspergillus Fumigatus ◽  
Inhibitory Activity ◽  
Endophytic Fungus ◽  
Fermentation Broth ◽  
2D Nmr ◽  
Cordyceps Sinensis ◽  
Two Dimensional ◽  
One Dimensional ◽  
Ic50 Values

Five new polyketides, including two pairs of enantiomers and a racemate, were isolated from the fermentation broth of Aspergillus fumigatus, an endophytic fungus isolated from Cordyceps sinensis. Their structures were identified using one-dimensional (1D) and two-dimensional (2D) NMR experiments, and the absolute configurations of the enantiomers were confirmed using electronic circular dichroism (ECD) calculations. Compounds 1a and 2a exhibited inhibitory activity against the MV4-11 cell line in vitro, with IC50 values of 23.95 µM and 32.70 µM, respectively.

scholarly journals Phytochemical screening and in vitro evaluation of alpha amylase, alpha glucosidase and beta galactosidase inhibition by aqueous and organic Atractylis gummifera L. extracts

2018 ◽  
Vol 5 (3) ◽  
pp. 103-112 ◽  
Author(s):  
Khadija Bouabid ◽  
Fatima Lamchouri ◽  
Hamid Toufik ◽  
Karima Sayah ◽  
Yahia Cherrah ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Alpha Amylase ◽  
Phytochemical Screening ◽  
Phytochemical Study ◽  
Organic Extracts ◽  
Ic50 Values ◽  
Inhibitory Potential ◽  
Alpha Glucosidase ◽  
Beta Galactosidase

Diabetes is a chronic condition which is increasingly progressing throughout the world. To treat it, several methods are used, among which is medicinal plants that still have an unknown mechanism of action. The objective of this work is to evaluate the in vitro hypoglycemic effect of the extracts of the underground part of Atractylis gummifera, a member of Asteraceae used in traditional Moroccan medicine. A phytochemical study of the aqueous extracts (decocted, infused and macerated) and organic extracts (methanol, methanol macerate, chloroformic, ethyl acetate and petroleum ether), and a phytochemical screening of the different secondary metabolites was done. The antidiabetic power of the extracts of A. gummifera by testing the inhibitory activity of ?-amylase, ?-glucosidase and ?-galactosidase, which are enzymes responsible for the digestion of polysaccharides was determined. The extracts of A. gummifera are very rich in flavonoids and tannins, and are inhibitory to?-amylase and ?-glucosidase, mainly the macerate of methanol with IC50 values of 0.557 ± 0.013 and 0.743 ± 0.017 mg / mL respectively. Higher ?-galactosidase inhibitory potential than quercetin was observed for aqueous macerates and methanol with IC50 values of 2.23 ± 0.012 and 2.443 ± 0.071 mg / mL respectively. The extracts of A. gummifera possess a significant inhibitory activity of the alpha amylase and alpha glucosidase and beta-galactosidase enzymes, in particular the macerate of methanol followed by the aqueous macerate, among the eight extracts tested.

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