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: 新的次生代谢产物及其细胞毒性活性。

: new secondary metabolites and their cytotoxic activities.

机构信息

Department of Pharmacognosy Faculty of Pharmacy, Mansoura University, Mansoura, Egypt.

Division of Systematic Forest and Forest Products Sciences, Department of Agro-Environmental Sciences, Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, Japan.

出版信息

Nat Prod Res. 2022 Oct;36(20):5134-5141. doi: 10.1080/14786419.2021.1922902. Epub 2021 Jun 28.

DOI:10.1080/14786419.2021.1922902
PMID:34180314
Abstract

Two new compounds, 11-methoxy-11,12-dihydro phytuberin (2) and 9-methoxy-benzocyclononan-7-one (6), together with twenty-six known ones were isolated from (Solanaceae). Their planar structure was established by extensive spectroscopic analyses. The absolute configuration of compound 6 was determined by time dependent density functional theory calculations (TDDFT). The cytotoxic potential of the isolates was assessed in cultured skin cancer (G-361) and colon cancer (HCT-116 and CaCo-2) cell lines. Certain flavonoids showed the highest cytotoxic activity, with IC values ranging from 7.1 to 63.3µM; meanwhile 5-flurouracil showed IC values ranging from 62.4 to >100 µM. All compounds showed minimal toxicity towards normal cells from skin (NHDF-4) and colon (CCD-841), indicating their potential selectivity and safety as cytotoxic candidates.

摘要

从茄科植物中分离得到了两个新化合物,11-甲氧基-11,12-二氢千里光菲灵(2)和 9-甲氧基-苯并环壬酮(6),以及另外 26 个已知化合物。通过广泛的光谱分析确定了它们的平面结构。通过时间依赖密度泛函理论计算(TDDFT)确定了化合物 6 的绝对构型。对分离得到的化合物进行了体外细胞毒性实验,实验对象为皮肤癌细胞(G-361)、结肠癌细胞(HCT-116 和 CaCo-2)。某些类黄酮表现出最高的细胞毒性,IC 值范围为 7.1-63.3μM;而 5-氟尿嘧啶的 IC 值范围为 62.4->100μM。所有化合物对皮肤正常细胞(NHDF-4)和结肠正常细胞(CCD-841)的毒性最小,表明它们具有作为细胞毒性候选药物的潜在选择性和安全性。

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