Six new 2-hydroxy ursane triterpenoids, 3---coumaroyloxy-2,19-dihydroxy-12-ursen-28-oic acid (), 3--coumaroyloxy-2,19-dihydroxy-12-ursen-28-oic acid (), 3---coumaroyloxy-2-hydroxy-12-ursen-28-oic acid (), 3--coumaroyloxy-2-hydroxy-12,20(30)-ursadien-28-oic acid (), 3-feruloyloxy-2-hydroxy-12,20(30)-ursadien-28-oic acid (), and 3-feruloyloxy-2-hydroxy-12,20(30)-ursadien-28-oic acid (), along with eleven known triterpenoids (-), were isolated from the leaves of . Their chemical structures were elucidated by comprehensive analysis of UV, IR, HRESIMS, and NMR spectra. All the isolated compounds were evaluated for their PTP1B inhibitory activity. 3---feruloyl-2-hydroxy-urs-12-en-28-oic acid () showed the best inhibition activity with an IC value of 10.32 ± 1.21 μM. The molecular docking study found that the binding affinity of compound for PTP1B was comparable to that of oleanolic acid (positive control).
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http://dx.doi.org/10.3390/molecules29071640 | DOI Listing |
Int J Biol Macromol
January 2025
Key Laboratory of Phytochemistry and Natural Medicines, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, People's Republic of China; University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China. Electronic address:
Diabetes mellitus (DM) is a chronic metabolic disorder characterized by elevated blood glucose levels, generally due to defects of insulin action or secretion. Inhibition of α-glucosidase, an enzyme responsible for carbohydrate degradation, is a promising strategy for managing postprandial hyperglycemia in diabetic patients. In this study, two new C-linked diarylheptanoid dimers, kaemgalanganols A (1) and B (2), were isolated from K.
View Article and Find Full Text PDFJ Nat Prod
December 2024
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China.
-Terphenyl compounds are known to possess a diverse range of biological activities, making the synthesis of novel -terphenyl derivatives a significant research objective. In this study, we report the first synthesis of nocarterphenyl A (), characterized by a thiazole-fused -terphenyl framework. Furthermore, we synthesized 18 additional analogs, including the naturally occurring compound 5-methoxy-4,7-bis(4-methoxyphenyl)benzo[]thiazol-6-ol (), employing a similar synthetic approach.
View Article and Find Full Text PDFInt J Mol Sci
November 2024
Department of Chemistry, College of Science, Engineering and Technology, University of South Africa, Private Bag X06, Florida 1710, South Africa.
The prevalence of small multi-target drugs containing a fluorinated aromatic moiety among approved drugs in the market is due to the unique properties of this halogen atom. With the aim to develop potent antidiabetic agents, a series of phenylsulfonic esters based on the conjugation of the 5-substituted 2-hydroxy-3-nitroacetophenones - with phenylsulfonyl chloride derivatives substituted with a fluorine atom or fluorine-containing (-CF or -OCF) group were prepared. Their structures were characterized using a combination of spectroscopic techniques complemented with a single-crystal X-ray diffraction (XRD) analysis on a representative example.
View Article and Find Full Text PDFChin J Nat Med
November 2024
Key Laboratory of Functional Molecules Analysis and Biotransformation of Universities in Yunnan Province, Yunnan Characteristic Plant Extraction Laboratory, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China; College of Traditional Chinese Medicine, Yunnan University of Chinese Medicine, Kunming 650500, China. Electronic address:
Three novel, highly oxygenated polyketides, multioketides A-C (1-3), and three previously described multioxidized aromatic polyketides (4-6), were isolated from an endophytic Penicillium sp. YUD17006 associated with Gastrodia elata. Their chemical structures were elucidated using extensive spectroscopic data, electronic circular dichroism calculations, and single X-ray diffraction analysis.
View Article and Find Full Text PDFEur J Med Chem
December 2024
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China. Electronic address:
A library of 4-Hydroxy Pd-C-Ⅲ derivatives (5a-5p and 8a-8h) as α-glucosidase inhibitors was prepared and the activity of these compounds against α-glucosidase was evaluated. The outcomes displayed that most of the derivatives had moderate to potent α-glucosidase inhibition with IC values ranging from 66.3 ± 2.
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