Human DNA topoisomerase I (Topo I) is an essential enzyme in regulating DNA supercoiling during transcription and replication, and it is an important therapeutic target for anti-tumor agents. L. is a medicinal herb that is used as a folk medicine for cancers in China. A new flavonoid () and a new polyacetylene (), along with eighteen flavonoids (-) and nine polyacetylenes (-), were isolated and identified from the methanol extract of the whole plant of , and some of the compounds (, , and ) exhibited potent cytotoxicity against a panel of five human cancer cell lines. The DNA relaxation assay revealed that some flavonoids and polyacetylenes exerted inhibitory activities on human DNA Topo I, among them compounds , , , , , , , , , , and were the most active ones, with IC values of 393.5, 328.98, 145.57, 239.27, 224.38, 189.84, 89.91, 47.5, 301.32, 178.03, and 218.27 μM, respectively. The structure-activity analysis of flavonoids was performed according to the results from the Topo I inhibition assay. The DNA content analysis revealed that , , and potently arrested cell cycle at the G/S and G/M phases in human colon cancer cell DLD-1 depending on the concentration of the inhibitors. The levels of protein expression related to the G/S and G/M cell cycle checkpoints were in accordance with the results from the DNA content analysis. These findings suggest that flavonoids are one of the key active ingredients accounting for the anti-tumor effect of .
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http://dx.doi.org/10.3390/molecules29153547 | DOI Listing |
Fitoterapia
October 2024
H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan; Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan; Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia. Electronic address:
The present study is focused on the isolation and identification of new therapeutic candidates from Chrysanthellum americanum Vatke., and their efficacy against pteridine reductase-1 (PTR1), a valid chemotherapeutic target in the Leishmania parasite. Henceforth, a new compound, chrysanamerine (1), along with 7 known compounds, polyacetylene 2, and flavonoids 3-8, were isolated from C.
View Article and Find Full Text PDFMolecules
July 2024
Key Laboratory of Chemistry in Ethnic Medicinal Resources, State Ethnic Affairs Commission and Ministry of Education, Yunnan Minzu University, Kunming 650504, China.
Chin Herb Med
July 2024
Nankai University, Tianjin 300353, China.
(Jiegeng in Chinese) is a well-known traditional Chinese medicine used for both medicinal and culinary purposes. Its historical use as an antitussive and expectorant has been extensively documented. Researchers, to date, have identified 219 chemical constituents in (Jacq.
View Article and Find Full Text PDFJ Ethnopharmacol
November 2024
Key Laboratory of Chinese Materia Medica, Heilongjiang University of Chinese Medicine, Ministry of Education, Harbin, 150040, China. Electronic address:
Ethnopharmacological Relevance: NOTOPTERYGII RHIZOMA ET RADIX (NRR), a traditional Chinese medicine (TCM), has been utilized in China for millennia. Thriving in high-altitude regions with cold climates, wild NRR has been heavily exploited for its significant economic worth, particularly in the medical sector.
The Aim Of The Review: This paper presents a comprehensive review of the botany, traditional uses, phytochemistry, analytical methods, quality control, processing methods, pharmacological effects, and pharmacokinetics of NRR.
Medicine (Baltimore)
June 2024
Chongqing College of Traditional Chinese Medicine, Chongqing, China.
Species of the genus Codonopsis (Campanulaceae) have a long history of application, acclaimed for its edible and therapeutic attributes. Scholarly inquiries into Codonopsis span botany, phytochemistry, quality assurance, pharmacodynamics, and toxicity, revealing a rich and comprehensive body of knowledge. This study synthesizes information from esteemed scientific databases like SciFinder, PubMed, China National Knowledge Infrastructure, and Chinese herbal classics to create a thorough scientific conceptual and theoretical framework for Codonopsis research.
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