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1.
Acta Pharmaceutica Sinica B ; (6): 639-644, 2018.
Article in English | WPRIM | ID: wpr-690876

ABSTRACT

Four new limonoid-type nortriterpenoids, 1-detigloyl-1--methacryloylsalannin (), 28-deoxo-2,3-dihydronimbolide (), 12-acetoxy-3--acetyl-7--tigloylvilasinin () and 12-acetoxy-3--acetyl-7--methacryloylvilasinin (), along with five known ones, were isolated from seeds of A. Juss. Their structures were elucidated by various spectroscopic methods, including UV, IR, MS, NMR, X-ray crystallography, quantum chemical calculation, as well as by comparison of their spectroscopic data with those reported. In the cytotoxic assay, showed inhibitory activity against human breast cancer MDA-MB-231 cell line with IC value of 7.68±1.74 μmol/L, and inhibited growth of human cervical cancer Hela cell line, melanoma A375 cell line and promyelocytic leukemia HL-60 cell line, with IC 12.00±2.08, 17.44±2.11, and 13.95±5.74 μmol/L, respectively.

2.
Article in Chinese | WPRIM | ID: wpr-509648

ABSTRACT

The antitumor activities of artemisinin and its derivatives has become a hot topic in recent years.Artemisinin and its derivatives have been reported to exert antitumor effects mainly by blocking the cell cycle, promoting tumor cell apoptosis, inhibiting angiogenesis and so on.Also, their influence on signaling pathways has attracted considerable interest of many scholars.Currently, in order to discover some compounds with better therapeutic potentials, many studies dedicated to the synthesis and development of new artemisinin derivatives.In addition, the effects of artemisinin and its derivatives on multi-drug resistantace in tumor cells also become a trend of the future research.In this paper, we review the research advances in the antitumor activities of artemisinin and its derivatives during the past five years to provide a reference for future study .

3.
Article in Chinese | WPRIM | ID: wpr-482356

ABSTRACT

Connexin (Cx) is the main component of gap junction channels, which is essential for intercellular communication between adjacent cells.Cx plays an important role in regulation of the growth, differentiation and apoptosis of cells and is closely related to tumor formation and development.The expression of Cx appears to be different in different stages of tumor development, and the regulatory mechanism of Cx is also involved in many aspects.In this paper, recent advances in the studies on Cx are reviewed, including the relationship between Cx and development of tumor, the basic mechanism of Cx, as well as its applications in antitumor-drug screening and tumor therapy.

4.
Article in Chinese | WPRIM | ID: wpr-298407

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the antioxidant and cytotoxic properties of five diarylheptanoids (1-5) isolated from the rhizomes of Zingiber officinale.</p><p><b>METHOD</b>Various models such as scavenging superoxide anions and 1,1-diphenyl-2- picrylhydrazyl (DPPH) radicals, inhibiting lipid peroxidation, as well as protecting of rat pheochromocytoma (PC12) cells induced by hydrogen peroxide (H2O2) were employed to assay the antioxidative effects of the diarylheptanoids. The cytotoxicities of compounds 1-5 were measured with MTT assays.</p><p><b>RESULT</b>The test compounds (1-5) showed promising DPPH inhibitory activities, and compound 5 exhibited the strongest DPPH scavenging activity with an IC50 value of (22.6+/-2.4) micromol x L(-1). Compounds 1, 3 and 4 showed potential anti-peroxidative effects with inhibitory rates of (66.3+/-15.4)%, (68.7+/-15.8)% and (72.2+/-10.6)%, respectively, at 100 microg x mL(-1). It could be observed that compounds 1, 3 and 4 demonstrated significant neuroprotective activities in a dose-dependent manner. Moreover, compound 3 exhibited certain cytotoxicities against human chronic myelogenous leukemia cells (K562) and its adriamycin-resistant cells (K562/ADR) with IC50 values of (34.9+/-0.6), (50.6+/-23.5) micromol x L(-1), respectively.</p><p><b>CONCLUSION</b>In vitro results demonstrated that five diarylheptanoids (1-5) isolated from the roots of Z. officinale were capable of scavenging radicals, inhibiting lipid peroxidation and protecting PC12 cells against the insult by H2O2. Additionally, compound 3 could inhibit the growth of K562 and K562/ADR cells.</p>


Subject(s)
Animals , Humans , Rats , Antioxidants , Toxicity , Cell Proliferation , Cytotoxins , Toxicity , Diarylheptanoids , Metabolism , Toxicity , Free Radicals , Metabolism , Zingiber officinale , Chemistry , Hydrogen Peroxide , Metabolism , K562 Cells , Oils, Volatile , Pharmacology , PC12 Cells , Rats, Sprague-Dawley
5.
Article in Chinese | WPRIM | ID: wpr-577079

ABSTRACT

Objective To establish the HPLC fingerprint of cultured Cordyceps militaris. MethodsHPLC Method was used for the determination of C. militaris on Agilent ZOBAX SB-Aq C18 column (250 mm?4.0 mm, 5 ?m), and measuring with methanol 5%—60% in 30 min as elution detective wavelength at 260 nm, injection sample of 1.0 ?L and flow rate of 1.0 mL/min. The systematic optimized design of the chromatographic conditions, such as supersonic extraction, mobile phase, and detective wavelength as well was carried out. Results Fingerprint consisted of 11 common peaks and the result of methodology determination fitted to the related standards. The evaluation of cultured C. militaris by systematically comparing chromatograms with a professional analytical software recommended by National Institute for the Control of Pharmaceutical and Biological Products has been established. Conclusion The method is accurate, simple, and useful for the quality control of cultured C. militaris.

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