scholarly journals New Fluorene Derivatives from Dendrobium gibsonii and Their α-Glucosidase Inhibitory Activity

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4931
Author(s):  
May Thazin Thant ◽  
Nutputsorn Chatsumpun ◽  
Wanwimon Mekboonsonglarp ◽  
Boonchoo Sritularak ◽  
Kittisak Likhitwitayawuid
Keyword(s):  
Kinetic Study ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Enzyme Kinetic ◽  
Whole Plant ◽  
Noncompetitive Inhibitor ◽  
Inhibitory Activities ◽  
New Compounds ◽  
Enzyme Kinetic Study

Two new compounds, dihydrodengibsinin (1) and dendrogibsol (2), were isolated from the whole plant of Dendrobium gibsonii, together with seven known compounds (3–9). The structures of the new compounds were elucidated by their spectroscopic data. All these isolates were evaluated for their α-glucosidase inhibitory activities. Dendrogibsol (2) and lusianthridin (7) showed strong α-glucosidase inhibitory activity when compared with acarbose. An enzyme kinetic study revealed that dendrogibsol (2) is a noncompetitive inhibitor of α-glucosidase.

scholarly journals α-Amylase and α-Glucosidase Inhibitory Activities of Chemical Constituents from Wedelia chinensis (Osbeck.) Merr. Leaves

2018 ◽  
Vol 2018 ◽  
pp. 1-8 ◽  
Author(s):  
Nguyen Phuong Thao ◽  
Pham Thanh Binh ◽  
Nguyen Thi Luyen ◽  
Ta Manh Hung ◽  
Nguyen Hai Dang ◽  
...  
Keyword(s):  
Spectroscopic Data ◽  
Chemical Constituents ◽  
2D Nmr ◽  
Inhibitory Effects ◽  
Meoh Extract ◽  
Inhibitory Activities ◽  
Isolated Compound ◽  
New Compounds ◽  
Modified Mosher’S Method

As part of an ongoing search for new natural products from medicinal plants to treat type 2 diabetes, two new compounds, a megastigmane sesquiterpenoid sulfonic acid (1) and a new cyclohexylethanoid derivative (2), and seven related known compounds (3–9) were isolated from the leaves of Wedelia chinensis (Osbeck.) Merr. The structures of the compounds were conducted via interpretation of their spectroscopic data (1D and 2D NMR, IR, and MS), and the absolute configurations of compound 1 were determined by the modified Mosher’s method. The MeOH extract of W. chinensis was found to inhibit α-amylase and α-glucosidase inhibitory activities as well as by the compounds isolated from this extract. Furthermore, compound 7 showed the strongest effect with IC50 values of 112.8 ± 15.1 μg/mL (against α-amylase) and 785.9 ± 12.7 μg/mL (against α-glucosidase). Compounds 1, 8, and 9 showed moderate α-amylase and α-glucosidase inhibitory effects. Other compounds showed weak or did not show any effect on both enzymes. The results suggested that the antidiabetic properties from the leaves of W. chinensis are not simply a result of each isolated compound but are due to other components such as the accessibility of polyphenolic groups to α-amylase and α-glucosidase activities.

CYP2C9 Ile359 and Leu359 variants: enzyme kinetic study with seven substrates

2000 ◽  
Vol 10 (2) ◽  
pp. 95-104 ◽  
Author(s):  
Kenji Takanashi ◽  
Hitoshi Tainaka ◽  
Kaoru Kobayashi ◽  
Toshio Yasumori ◽  
Masakiyo Hosakawa ◽  
...  
Keyword(s):  
Kinetic Study ◽  
Enzyme Kinetic ◽  
Enzyme Kinetic Study

Human Hepatic ß-Glucuronidase: An Enzyme Kinetic Study

Enzyme ◽  
1985 ◽  
Vol 33 (1) ◽  
pp. 9-17 ◽  
Author(s):  
Yen-Ching Ho ◽  
Le-Hong C. Ho ◽  
Kang-Jey Ho
Keyword(s):  
Kinetic Study ◽  
Enzyme Kinetic ◽  
Enzyme Kinetic Study

scholarly journals Inhibition of SARS-CoV 3C-like Protease Activity by Theaflavin-3,3'-digallate (TF3)

2005 ◽  
Vol 2 (2) ◽  
pp. 209-215 ◽  
Author(s):  
Chia-Nan Chen ◽  
Coney P. C. Lin ◽  
Kuo-Kuei Huang ◽  
Wei-Cheng Chen ◽  
Hsin-Pang Hsieh ◽  
...  
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Inhibitory Activity ◽  
Black Tea ◽  
Host Cells ◽  
Epicatechin Gallate ◽  
Natural Polyphenols ◽  
Different Types ◽  
Natural Product Library ◽  
Inhibitory Activities ◽  
New Compounds

SARS-CoV is the causative agent of severe acute respiratory syndrome (SARS). The virally encoded 3C-like protease (3CLPro) has been presumed critical for the viral replication of SARS-CoV in infected host cells. In this study, we screened a natural product library consisting of 720 compounds for inhibitory activity against 3CLPro. Two compounds in the library were found to be inhibitive: tannic acid (IC50 = 3 µM) and 3-isotheaflavin-3-gallate (TF2B) (IC50 = 7 µM). These two compounds belong to a group of natural polyphenols found in tea. We further investigated the 3CLPro-inhibitory activity of extracts from several different types of teas, including green tea, oolong tea, Puer tea and black tea. Our results indicated that extracts from Puer and black tea were more potent than that from green or oolong teas in their inhibitory activities against 3CLPro. Several other known compositions in teas were also evaluated for their activities in inhibiting 3CLPro. We found that caffeine, (—)-epigallocatechin gallte (EGCg), epicatechin (EC), theophylline (TP), catechin (C), epicatechin gallate (ECg) and epigallocatechin (EGC) did not inhibit 3CLPro activity. Only theaflavin-3,3′-digallate (TF3) was found to be a 3CLPro inhibitor. This study has resulted in the identification of new compounds that are effective 3CLPro inhibitors.

scholarly journals Agelasine Diterpenoids and Cbl-b Inhibitory Ageliferins from the Coralline Demosponge Astrosclera willeyana

Marine Drugs ◽  
2021 ◽  
Vol 19 (7) ◽  
pp. 361
Author(s):  
Wei Jiang ◽  
Dongdong Wang ◽  
Brice A. P. Wilson ◽  
Unwoo Kang ◽  
Heidi R. Bokesch ◽  
...  
Keyword(s):  
Ubiquitin Ligase ◽  
Spectroscopic Data ◽  
Active Compounds ◽  
Spectrometric Data ◽  
Ubiquitin Ligase Activity ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Immunomodulatory Protein ◽  
New Compounds

An extract of the coralline demosponge Astrosclera willeyana inhibited the ubiquitin ligase activity of the immunomodulatory protein Cbl-b. The bioassay-guided separation of the extract provided ten active compounds, including three new N-methyladenine-containing diterpenoids, agelasines W–Y (1–3), a new bromopyrrole alkaloid, N(1)-methylisoageliferin (4), and six known ageliferin derivatives (5–10). The structures of the new compounds were elucidated from their spectroscopic and spectrometric data, including IR, HRESIMS, and NMR, and by comparison with spectroscopic data in the literature. While all of the isolated compounds showed Cbl-b inhibitory activities, ageliferins (4–10) were the most potent metabolites, with IC50 values that ranged from 18 to 35 μM.

scholarly journals Bioactive Compounds from an Endophytic Fungi Nigrospora Aurantiaca

2021 ◽  
Author(s):  
Safwan Safwan ◽  
George Hsiao ◽  
Tzong-Huei Lee ◽  
Ching-Kuo Lee
Keyword(s):  
Bioactive Compounds ◽  
Endophytic Fungi ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Biological Activities ◽  
Fungal Strain ◽  
No Production ◽  
Chemical Structures ◽  
Inhibitory Activities ◽  
Melaleuca Leucadendra

Abstract Background: Many groups of fungi live as an endophyte in plants . Endophytic fungi could produce the bioactive compounds which was new or know compounds. Various biological activities of bioactive compounds from endophytic fungi had been reported, including anti-inflammatory and anticancer. Chemical investigation and biological activities of bioactive compounds from endophytic fungi from Melaleuca leucadendra Linn. have not yet been reportedResults: One new compound, namely nigaurdiol (1), together with five known compounds, xyloketal K (2), bostrycin (3), deoxybostrycin (4), xylanthraquinone (5), and ergosterol (6), were isolated from the Melaleuca leucadendra Linn. associated fungal strain Nigrospora aurantiaca #TMU062. Their chemical structures were elucidated by spectroscopic data and compared with literatures. All isolated compounds were evaluated for NO production inhibitory activity in LPS-activated microglial BV-2 cells. Conclusions: Compound 6 exhibited markedly inhibitory activities on NO production with IC50 values of 7.2 ± 1.4 µM and the survival of the cells was 90.8 ± 6.7% at the concentration of 10 µM.

scholarly journals Saccharpiscinols A–C: Flavans with Potential Inflammatory Activities from One Actinobacteria Saccharomonospora piscinae

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4909
Author(s):  
Yung-Shun Su ◽  
Jih-Jung Chen ◽  
Ming-Jen Cheng ◽  
Chee-Yin Chai ◽  
Aij-Lie Kwan ◽  
...  
Keyword(s):  
Data Analysis ◽  
Chromatographic Separation ◽  
Spectroscopic Data ◽  
2D Nmr ◽  
No Production ◽  
Raw 264.7 ◽  
Phytochemical Investigation ◽  
Inhibitory Activities ◽  
New Compounds ◽  
First Time

Phytochemical investigation and chromatographic separation of extracts from the actinobacteria strain Saccharomonospora piscinae that was isolated from dried fishpond sediment of Kouhu township, in the south of Taiwan, led to the isolation of three new compounds, saccharpiscinols A–C (1–3, respectively), and three new natural products, namely (2S)-5,7,3′,4′-tetrahydroxy-6,8-dimethylflavanone (4), methyl-4-hydroxy-2-methoxy-6-methylbenzoate (5), and (±)-7-acetyl-4,8-dihydroxy-6-methyl-1-tetralone (6). Compounds 4–6 were reported before as synthesized products, herein, they are reported from nature for the first time. The structures of the new compounds were unambiguously elucidated on the basis of extensive spectroscopic data analysis (1D- and 2D-NMR, MS, and UV) and comparison with literature data. The effect of some isolates on the inhibition of NO production in lipopolysaccharide-activated RAW 264.7 murine macrophages was evaluated. Saccharpiscinol A showed inhibitory activities against LPS-induced NO production.

Synthesis and Antibacterial Evaluation of Thiouracil Derivatives Contain-ing 1,2,4-Triazolo[1,5-a]Pyrimidine

2020 ◽  
Vol 17 ◽  
Author(s):  
Penglei Cui ◽  
Di Zhang ◽  
Xiumin Guo ◽  
Shujing Ji ◽  
Qingmei Jiang
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Inhibitory Activity ◽  
Bacillus Amyloliquefaciens ◽  
Antibacterial Activities ◽  
Inhibitory Activities ◽  
New Compounds ◽  
Thiouracil Derivatives ◽  
Antibacterial Evaluation

: A series of new thiouracil compounds containing 1,2,4-triazolo[1,5-a]pyrimidine were designed and synthesized. The in vitro antibacterial activities of the new compounds against Bacillus amyloliquefaciens, Staphylococcus aureus and Bacillus subtilis were tested. The results showed that some of the new compounds had strong inhibitory activities against the tested bacteria. At the concentration of 50 μg/mL, the compound 12d had broad and the highest inhibitory activity with the 100% inhibition against the three tested strains, the same as norfloxacin which was used as the control.

scholarly journals Evaluation of the Antibacterial, Antioxidant and α-Glucosidase Inhibitory Activities of Withanolides from Physalis gracilis

2018 ◽  
Vol 5 (01) ◽  
pp. e1-e4
Author(s):  
Gerardo Padierna ◽  
Ana Pérez-Castorena ◽  
Mahinda Martínez ◽  
Antonio Nieto-Camacho ◽  
Jesús Morales-Jiménez ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
2D Nmr ◽  
Chemical Investigation ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Inhibitory Activities

AbstractA chemical investigation of the leaves, flowers, and stems of Physalis gracilis led to the isolation of three withanolides identified as withanolide D (1), 24,25-dihydrowithanolide D (2), and withaphysacarpin (3). The structures of these compounds were determined by analyses of their spectroscopic data, including 1D and 2D NMR. The antibacterial, antioxidant, and α-glucosidase inhibitory activities of compounds 1 and 3 and derivatives 4 and 5 were evaluated. None of the compounds showed antioxidant or glucosidase inhibitory activity. Also, they were inactive against gram-negative bacteria. However, compound 3 was found active against Bacillus subtilis (MIC=65.5 µM) and compound 5 against Staphylococcus aureus (MIC=27.9 µM).

scholarly journals Three Novel Biphenanthrene Derivatives and a New Phenylpropanoid Ester from Aerides multiflora and Their α-Glucosidase Inhibitory Activity

Plants ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 385
Author(s):  
May Thazin Thant ◽  
Boonchoo Sritularak ◽  
Nutputsorn Chatsumpun ◽  
Wanwimon Mekboonsonglarp ◽  
Yanyong Punpreuk ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Spectroscopic Data ◽  
Competitive Inhibition ◽  
Positive Control ◽  
The Other ◽  
Biological Investigation ◽  
Phytochemical Investigation ◽  
Whole Plants ◽  
New Compounds ◽  
Burk Plot

A phytochemical investigation on the whole plants of Aerides multiflora revealed the presence of three new biphenanthrene derivatives named aerimultins A–C (1–3) and a new natural phenylpropanoid ester dihydrosinapyl dihydroferulate (4), together with six known compounds (5–10). The structures of the new compounds were elucidated by analysis of their spectroscopic data. All of the isolates were evaluated for their α-glucosidase inhibitory activity. Aerimultin C (3) showed the most potent activity. The other compounds, except for compound 4, also exhibited stronger activity than the positive control acarbose. Compound 3 showed non-competitive inhibition of the enzyme as determined from a Lineweaver–Burk plot. This study is the first phytochemical and biological investigation of A. multiflora.

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