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1.
Surawat Jariyawat Thanapol Thammapratip Kanoknetr Suksen Podchanart Wanitchakool Jintapat Nateewattana Arthit Chairoungdua Apichart Suksamrarn Pawinee Piyachaturawat 《Cell biology and toxicology》2011,27(6):413-423
Diarylheptanoids, isolated from the rhizome of Curcuma comosa Roxb., have several biological activities including anti-oxidant and anti-inflammation. The present study investigated the
effect of five diarylheptanoids isolated from C. comosa rhizome on the proliferation of murine P388 leukemic cells. Compound-092, (3S)-1-(3,4-dihydroxyphenyl)-7-phenyl-(6E)-6-hepten-3-ol, bearing a catechol moiety, was the most potent diarylheptanoid (IC50 of 4 μM) in inhibiting P388 leukemic cell viability by causing DNA breakage and inducing apoptosis. Apoptotic cell death
was characterized by the presence of chromatin condensation, formation of apoptotic bodies, DNA fragmentation, and externalization
of plasma membrane phosphatidylserine. This compound increased caspase-3 activity about fivefold above the untreated control,
decreased the intracellular reduced glutathione level, and impaired mitochondrial transmembrane potential. In the presence
of Cu(II) ion, the compound exhibited a pro-oxidant activity causing DNA strand breakage and enhancing the anti-proliferative
activity. The results provide evidence for the pro-oxidant activity of the diarylheptanoid bearing a catechol moiety in the
induction of apoptosis in murine P388 leukemia. 相似文献
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3.
Sarawalee Arunkhamkaew Anan Athipornchai Nuttapon Apiratikul Apichart Suksamrarn Vachiraporn Ajavakom 《Bioorganic & medicinal chemistry letters》2013,23(10):2880-2882
The synthesis of racemic tetrahydrocurcumin- (THC-), tetrahydrodemethoxycurcumin- (THDC-) and tetrahydrobisdemethoxycurcumin- (THBDC-) dihydropyrimidinone (DHPM) analogues was achieved by utilizing the multi-component Biginelli reaction in the presence of copper sulphate as a catalyst. The evaluation of acetylcholinesterase inhibitors for Alzheimer’s disease of these compounds showed that they exhibited higher inhibitory activity than their parent analogues. THBDC–DHPM demonstrated the most potent inhibitory activity with an IC50 value of 1.34 ± 0.03 μM which was more active than the approved drug galanthamine (IC50 = 1.45 ± 0.04 μM). 相似文献
4.
Highly oxygenated ecdysteroids, (24R)-11 alpha, 20,24-trihydroxyecdysone and 11 alpha,20,26-trihydroxyecdysone, have been isolated from the polar fraction of Vitex canescens root bark. The latter exists as two C-25 epimers which could be separated by reversed-phase HPLC. 相似文献
5.
Arnab Nayek Parth Sarthi Sen Gupta Shyamashree Banerjee Vishma Pratap Sur Pratyay Seth Sunit Das Rifat Nawaz Ul Islam Amal Kumar Bandyopadhyay 《Bioinformation》2015,11(8):413-415
AvailabilityADSBET2 is freely available at http://sourceforge.net/projects/ADSBET2/ for all users. 相似文献
6.
Ratchanaporn Chokchaisiri Phongsak Innok Apichart Suksamrarn 《Phytochemistry letters》2012,5(2):361-366
Four new flavonoid glycosides, curcucomosides A–D (1–4), three known flavonoid glycosides, 5–7, and four known diarylheptanoids, 8–11, were isolated from the ethanol extract of the aerial parts of Curcuma comosa. The structures of the new compounds were established as rhamnazin 3-O-α-l-arabinopyranoside (1), rhamnocitrin 3-O-α-l-arabinopyranoside (2), rhamnazin 3-O-α-l-rhamnopyranosyl-(1→2)-O-α-l-arabinopyranoside (3), and rhamnocitrin 3-O-α-l-rhamnopyranosyl-(1→2)-O-α-l-arabinopyranoside (4) by spectroscopic analysis and chemical reactions whereas those of the known compounds were identified by spectral comparison with those of the reported values. 相似文献
7.
Jutamas Apisornopas Patamawadee Silalai Teerapich Kasemsuk Anan Athipornchai Uthaiwan Sirion Kanoknetr Suksen Pawinee Piyachaturawat Apichart Suksamrarn Rungnapha Saeeng 《Bioorganic & medicinal chemistry letters》2018,28(9):1558-1561
New iridoid glycoside derivatives from durantoside I, the latter from the dried flowers and leaves of Citharexylum spinosum, were synthesized by variously modifying a sugar moiety by silylation or acetylation and/or removal of cinnamate group at C-7 position and subsequent screening for comparative cytotoxicity against several cancer cell lines. Addition of alkylsilane to durantoside I and removal of cinnamate group were most effective in improving cytotoxicity. 相似文献
8.
Sudarat Sombut Rada Bunthawong Uthaiwan Sirion Teerapich Kasemsuk Pawinee Piyachaturawat Kanoknetr Suksen Apichart Suksamrarn Rungnapha Saeeng 《Bioorganic & medicinal chemistry letters》2017,27(23):5139-5143
A series of 14-deoxy-11,12-didehydroandrographolide analogues were synthesized from naturally occurring andrographolide and their cytotoxicity evaluated against nine cancer cell lines including cholangiocarcinoma. Analogues 5a and 5b exhibited the most potent cytotoxicity with ED50s of 3.37 and 3.08?μM on KKU-M213 cell lines and 2.93 and 3.27?μM on KKU-100 cell lines, respectively. Selective cytotoxicity on cholangiocarcinoma cell lines identified in this study highlight the importance of structural modification in the development of drugs for this cancer. 相似文献
9.
Kevin T. Gobeske Sunit Das Michael A. Bonaguidi Craig Weiss Jelena Radulovic John F. Disterhoft John A. Kessler 《PloS one》2009,4(10)
Exposure to exercise or to environmental enrichment increases the generation of new neurons in the adult hippocampus and promotes certain kinds of learning and memory. While the precise role of neurogenesis in cognition has been debated intensely, comparatively few studies have addressed the mechanisms linking environmental exposures to cellular and behavioral outcomes. Here we show that bone morphogenetic protein (BMP) signaling mediates the effects of exercise on neurogenesis and cognition in the adult hippocampus. Elective exercise reduces levels of hippocampal BMP signaling before and during its promotion of neurogenesis and learning. Transgenic mice with decreased BMP signaling or wild type mice infused with a BMP inhibitor both exhibit remarkable gains in hippocampal cognitive performance and neurogenesis, mirroring the effects of exercise. Conversely, transgenic mice with increased BMP signaling have diminished hippocampal neurogenesis and impaired cognition. Exercise exposure does not rescue these deficits, suggesting that reduced BMP signaling is required for environmental effects on neurogenesis and learning. Together, these observations show that BMP signaling is a fundamental mechanism linking environmental exposure with changes in cognitive function and cellular properties in the hippocampus. 相似文献
10.
Mitra PS Basu NK Basu M Chakraborty S Saha T Owens IS 《The Journal of biological chemistry》2011,286(2):1639-1648
Whereas UDP-glucuronosyltransferase-2B7 is widely distributed in different tissues, it preferentially detoxifies genotoxic 4-OH-estradiol and 4-OH-estrone (4-OHE(1)) with barely detectable 17β-estradiol (E(2)) conversion following expression in COS-1 cells. Consistent with the UDP-glucuronosyltransferase requirement for regulated phosphorylation, we discovered that 2B7 requires Src-dependent tyrosine phosphorylation. Y236F-2B7 and Y438F-2B7 mutants were null and 90% inactive, respectively, when expressed in COS-1. We demonstrated that 2B7 incorporated immunoprecipitable [(33)P]orthophosphate and that 2B7His, previously expressed in SYF-(Src,Yes,Fyn)(-/-) cells, was Src-supported or phosphorylated under in vitro conditions. Unexpectedly, 2B7 expressed in SYF(-/-) and SYF(+/-) cells metabolized 4-OHE(1) at 10- and 3-fold higher rates, respectively, than that expressed in COS-1, and similar analysis showed that E(2) metabolism was 16- and 9-fold higher than in COS-1. Because anti-Tyr(P)-438-2B7 detected Tyr(P)-438-2B7 in each cell line, results indicated that unidentified tyrosine kinase(s) (TKs) phosphorylated 2B7 in SYF(-/-). 2B7-transfected COS-1 treated with increasing concentrations of the Src-specific inhibitor PP2 down-regulated 4-OHE(1) glucuronidation reaching 60% maximum while simultaneously increasing E(2) metabolism linearly. This finding indicated that increasing PP2 inhibition of Src allows increasing E(2) metabolism caused by 2B7 phosphorylation by unidentified TK(s). Importantly, 2B7 expressed in SYF(-/-) is more competent at metabolizing E(2) in cellulo than 2B7 expressed in COS-1. To confirm Src-controlled 2B7 prevents toxicity, we showed that 2B7-transfected COS-1 efficiently protected against 4-OH-E(1)-mediated depurination. Finally, our results indicate that Src-dependent phosphorylation of 2B7 allows metabolism of 4-OHE(1), but not E(2), in COS-1, whereas non-Src-phosphorylated 2B7 metabolizes both chemicals. Importantly, we determined that 2B7 substrate selection is not fixed but varies depending upon the TK(s) that carry out its required phosphorylation. 相似文献