Objective: To study the chemical constituents and bioactivity of Teurium pilosum.
Method: Various column chromatographic techniques were used to isolate the constituents. A combination of EI-MS, NMR spectroscopy and X-Ray were applied to identify the structures. The anti-microorganism was accomplished by disk diffusion method, the antioxidant activity was assayed by the DPPH microanalysis models and the inhibitory activity of alpha-glucosidase was screened In vitro.
Result: Eight compounds were isolated and identified as: glyceryl tristearate (1), 2,5-dioxolanone (2), fernenol (3), stigmasta-5,22-dien-3P-ol (4), 24-nor cholesta-5,22 (E)-dien-3beta-ol (5), ca-spinasterol (6), (3,4-dihydroxyphenyl) acrylate (7), 3,4-dihydroxy phenyl acrylic acid (8).
Conclusion: All compounds have been isolated from the genus for the first time. Compound 3 [IC50 = (37.63 +/- 3.45) mg +/- L(-1)], 6 [IC50 = (178.92 +/- 4.99) mg x L(-1)] and 8 [IC50 = (44.32 +/- 7.02) mg x L(-1)] are of higher inhibitory alpha-glucosidase activity than that of acarbose [IC50 = (1081.27 +/- 12.3) mg x L(-1)]. Compound7 [IC50 = (4.81 +/- 0.96) mg x L(-1)] and 8 [IC50 = (4.16 +/- 0.11) mg L(-1)] showed higher antioxidant activity than that of BHT [IC50 = (35.64 +/- 0.36) mg x L(-1)] and BHA [IC50 = (8.74 +/- 0.39) mg x L(-1)]. Compound 5-8 exhibited inhibitory activity against Fusarium graminearum. Compound 5 and 8 showed inhibitory activity against Botrytis cinerea.
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Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, UCSI University, No. 1, Jalan Menara Gading, Taman Connaught, Cheras, Kuala Lumpur, 56000, Malaysia.
The third most prevalent type of cancer in the world, colorectal cancer, poses a significant treatment challenge due to the nonspecific distribution, low efficacy, and high systemic toxicity associated with chemotherapy. To overcome these limitations, a targeted drug delivery system with a high cytotoxicity against cancer cells while maintaining a minimal systemic side effects represents a promising therapeutic approach. Therefore, the aim of this study was to develop an efficient gold nanocarrier for the targeted delivery of the anticancer agent everolimus to Caco-2 cells.
View Article and Find Full Text PDFNaunyn Schmiedebergs Arch Pharmacol
January 2025
School of Pharmacy, Jiangxi University of Chinese Medicine, Nanchang, China.
Microglia-mediated neuroinflammation plays a crucial role in Alzheimer's disease (AD). Tinosinenside A (Tis A) is a novel sesquiterpene glycoside isolated from the dried rattan stem of Tinospora sinensis (Lour.) Merr.
View Article and Find Full Text PDFEndocr Relat Cancer
January 2025
A Nikitski, Department of Pathology, University of Pittsburgh, Pittsburgh, 15261, United States.
Approximately 10-20% of thyroid cancers are driven by gene fusions, which activate oncogenic signaling through aberrant overexpression, ligand-independent dimerization, or loss of inhibitory motifs. We identified 13 thyroid tumors with thyroglobulin (TG) gene fusions and aimed to assess their histopathology and the fusions' oncogenic and tumorigenic properties. Of 11 cases with surgical pathology, 82% were carcinomas and 18% noninvasive follicular thyroid neoplasms with papillary-like nuclear features (NIFTP).
View Article and Find Full Text PDFAim: Human carbonic anhydrases (hCAs) are involved in many physiological processes including respiration, pH control, ion transport, bone resorption, and gastric fluid secretion. Recently, CA IX and CA XII have been studied for their role in cancer diseases, motivating the design of inhibitors of these isoforms.
Material And Method: Here, we used the tail approach to design a new series of monoaryl () and bicyclic () benzensulfonamide derivatives CA IX and CA XII inhibitors.
Elife
January 2025
Centre for Cellular Biology and Signalling, Zhejiang University-University of Edinburgh (ZJU-UoE) Institute, Haining, China.
Mitochondrial dysfunction is involved in numerous diseases and the aging process. The integrated stress response (ISR) serves as a critical adaptation mechanism to a variety of stresses, including those originating from mitochondria. By utilizing mass spectrometry-based cellular thermal shift assay (MS-CETSA), we uncovered that phosphatidylethanolamine-binding protein 1 (PEBP1), also known as Raf kinase inhibitory protein (RKIP), is thermally stabilized by stresses which induce mitochondrial ISR.
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