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Isocoreopsin: An active constituent of n-butanol extract of Butea monosperma flowers against colorectal cancer (CRC)

机译:Isocoreopsin:单精子花正丁醇提取物抗结直肠癌(CRC)的活性成分

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摘要

The herb Butea monosperma constitutes several human health beneficial components, which are mostly studied for their anticancer effects. In this study, the activity of n-butanol fractions of B. monosperma floral extract was examined on inhibiting aberrant crypt foci (ACF) formation in azoxymethane induced Wistar albino rats. The n-butanol extracts (150 mg/kg) decreased the ACF formation (per rat) by 92% and 78% in short- and long-term in vivo treatments, respectively. All the compounds in the n-butanol extract were isolated and purified using column and reverse-phase high pressure liquid chromatography (HPLC). Their structures were characterized using UV–visible spectroscopy, nuclear magnetic resonance (NMR) and electrospray–ionisation mass spectrometry (ESI–MS) to determine important flavonoids, namely isocoreopsin, butrin and isobutrin. These compounds were studied for their free radical scavenging and anticancer activities. The compound isocoreopsin showed significantly greater efficacy in cell death on human colon and liver cancer cell lines (50 μg/mL in HT-29 and 100 μg/mL in HepG2) than butrin (100 μg/mL in HT-29 and 500 μg/mL in HepG2) and isobutrin (80 μg/mL in HT-29 and 150 μg/mL in HepG2). These results suggest that isocoreopsin, butrin and isobutrin are the important key compounds for the chemoprevention of colon cancer and isocoreopsin can be considered as a promising novel drug.
机译:紫丁香药草构成了对人体健康有益的几种成分,人们大多对其抗癌作用进行了研究。在这项研究中,检查了单精子孢子花提取物的正丁醇部分的活性,以抑制在由乙氧基甲烷诱导的Wistar白化病大鼠中异常隐窝灶(ACF)的形成。在短期和长期体内治疗中,正丁醇提取物(150 mg / kg)分别使每只大鼠的ACF形成减少92%和78%。正丁醇提取物中的所有化合物均使用柱和反相高压液相色谱法(HPLC)进行分离和纯化。使用紫外可见光谱,核磁共振(NMR)和电喷雾电离质谱(ESI–MS)对它们的结构进行了表征,以确定重要的类黄酮,即异核视黄素,丁香精和异丁香精。研究了这些化合物的自由基清除和抗癌活性。异异视蛋白复合物在人结肠和肝癌细胞系的细胞死亡中显示出显着更高的效力(HT-29中为50μg/ mL,HepG2中为100μg/ mL),而丁蛋白(HT-29和500μg/ mL中为100μg/ mL)毫升在HepG2中)和异丁蛋白(在HT-29中为80μg/ mL,在HepG2中为150μg/ mL)。这些结果表明异科普索辛,丁香精和异丁香精是化学预防结肠癌的重要关键化合物,异科普索辛被认为是一种有前途的新药。

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