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首页> 外文期刊>RSC Advances >16-Tigloyl linked barrigenol-like triterpenoid from Semen Aesculi and its anti-tumor activity in vivo and in vitro
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16-Tigloyl linked barrigenol-like triterpenoid from Semen Aesculi and its anti-tumor activity in vivo and in vitro

机译：16-替洛oyl从Semen Aesculi及其体内和体外抗肿瘤活性连接的贫苯酚样Triterpenoid

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Barrigenol-like triterpenoids (BATs) showed promising anti-tumor, anti-inflammatory and anti-Alzheimer's activities, while, the inhibitory strength was usually affected by their states with aglycones or glycosides. In order to find more BATs as new anti-tumor agents with much more efficiency, the chemical and pharmaceutical studies were carried out on the acid hydrolysate product (AHP) of Semen Aesculi crude extract. Thirteen BATs, including three new aglycones ( 1–3 ), two new glycosides ( 4 , 5 ) and eight known glycosides ( 6–13 ) were obtained. Compound 1 , as the main product in AHP, with a tigloyl unit linked at the C-16 position was an unusual aglycone. All compounds exhibited various degrees of inhibitory activity against human breast cell line (MCF-7) and cervical cancer cell line (HeLa) growth, moreover, new aglycones 1 and 2 , and the known glycoside 6 (escin Ia) and 9 were found to exhibit potent inhibitory activity which were similar to the positive control (doxorubicin hydrochloride). Compound 1 , named 16-tigloyl- O -protoaescigenin, could suppress tumor progression and decreased lung metastasis focuses in mice, and no pathological change was observed at the end of the treatment course. Besides that, the hemolysis experiment between 1 and 6 revealed that the hemolysis toxicity of 1 was much less than that of 6 . According to these results, 16-tigloyl- O -protoaescigenin, with the powerful anti-tumor activity and cancer cell apoptosis induction, might be considered as a new promising anti-tumor agent.
机译：贫瘠之类的三萜（蝙蝠）显示出有前途的抗肿瘤，抗炎和抗阿尔茨海默氏症的活动，而抑制强度通常受到糖基或糖苷的含量的影响。为了在具有更高效率的新的抗肿瘤剂中找到更多蝙蝠，在Semen Aesculi粗提取物的酸水解产物（AHP）上进行化学和药物研究。在包括三种新的糖苷（1-3），包括三种新的糖苷（4,5）和8个已知的糖苷（6-13）的十三桶。化合物1，作为AHP中的主要产物，用在C-16位置连接的替代单位是不寻常的糖苷酮。所有化合物均显示出对人乳腺细胞系（MCF-7）和宫颈癌细胞系（HELA）生长的各种抑制活性，此外，新的糖苷1和2，以及已知的糖苷6（escin Ia）和9表现出与阳性对照（盐酸多柔比星）类似的有效抑制活性。据称16-Tigloyl-O-protoaescinin的化合物1可以抑制肿瘤进展和降低的肺转移侧重于小鼠，并且在治疗过程结束时没有观察到病理变化。除此之外，1至6之间的溶血实验表明，溶血毒性为1的毒性远小于6。根据这些结果，16-Tigloyl-O-Protoaescinin，具有强大的抗肿瘤活性和癌细胞凋亡诱导，可能被认为是一种新的有前途的抗肿瘤剂。

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