Helichrysetin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Helichrysetin 具有轻微的抗 HIV-1 PR 活性。 Helichrysetin 作为抗癌剂具有巨大的开发潜力，它对四种选定的癌细胞系 A549、MCF-7、Ca Ski 和 HT-29 具有细胞毒作用。 寻找泰国的抗 HIV-1 蛋白酶 (PR) 抑制剂药用植物导致从 Boesenbergia pandurata 根茎的甲醇提取物中分离出一种名为 panduratin C 的新环己烯基查耳酮和查耳酮衍生物 。

Helichrysetin has mild anti-HIV-1 PR activity. Helichrysetin has great potentials for development as an anticancer agent, it has cytotoxic effect on four selected cancer cell lines, A549, MCF-7, Ca Ski, and HT-29.Searching for anti-HIV-1 protease (PR) inhibitors of Thai medicinal plants led to the isolation of a new cyclohexenyl chalcone named panduratin C and chalcone derivatives from the methanol extract of Boesenbergia pandurata rhizomes. The known compounds were identified to be panduratin A, hydroxypanduratin A, Helichrysetin, 2',4',6'-trihydroxyhydrochalcone, and uvangoletin . The structures of all compounds were elucidated on the basis of chemical and spectroscopic methods.

Cell Viability AssayCell Line:HT-29, A549, MCF-7, and Ca SkiConcentration:1.56, 3.13, 6.25, 12.5, 25, 50, 100 μg/mL Incubation Time:72 h Result:Inhibited cell growth in a dose-dependent manner.IC50 for A549, Ca Ski, HT29, MCF-7 was 50.72 ± 1.26 μM (14.52 ± 0.36 μg/mL), 31.02 ± 0.45 μM (8.88 ± 0.13 μg/mL), 102.94 ± 2.20 μM (29.47 ± 0.63 μg/mL) and 97.35 ± 1.71 μM (27.87 ± 0.49 μg/mL).Apoptosis Analysis Cell Line:A549 Concentration:5, 15, 20 μg/mL Incubation Time:24-72 h Result:The population of early apoptotic cells increased from 2.65 ± 0.31% (control) to 2.78 ± 0.21%, 14.98 ± 0.79%, and 28.55 ±1.19%.Caused accumulation of cells in S phase, occurring simultaneously with the significant reduction of cell percentage in G0/G1 phase with 15 and 20 μg/mL.Western Blot Analysis Cell Line:MGC803 Concentration:10, 20 40 μM Incubation Time:24 h Result:Increased the protein expression of cleaved caspase 3 (20 and 40 μM) and reduced protein expression of Bcl-2 (40 μM), but had no significant effect on the protein expression of Bax.RT-PCR Cell Line:MGC803 Concentration:10, 20 40 μM Incubation Time:24 h Result:Reduced the mRNA and protein expression of PDHK1 and LDHA but only decreased the mRNA level of LDHB.

Animal Model:MGC803 cell-xenografted mouse model Dosage:3, 10, 30 mg/kg Administration:i.p.Result:Decreased the tumor size and weight without an obvious effect on body weight in nude mice.Reduced the expression of Ki67 and increased the number of apoptotic cells in tumor tissues.

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Microbiology/Virology

HIV

HIV

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62014-87-3

286.3

C16H14O5

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (174.65 mM)

O=C(C1=C(OC)C=C(O)C=C1O)/C=C/C2=CC=C(O)C=C2

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(-20℃)

With Ice Pack

≥ 2 years