Hippolides A-H, Acyclic Manoalide Derivatives from the Marine Sponge Hippospongia lachne
Hippolides A-H, Acyclic Manoalide Derivatives from the Marine Sponge Hippospongia lachne
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Hippolides A-H，来自海洋海绵 Hippospongia lachne 的无环 Manoalide 衍生物
DOI：
10.1021/np200227s
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发表时间：
2011-05-01
影响因子：
5.1
通讯作者：
Lin, Hou-Wen
中科院分区：
文献类型：
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作者：
Piao, Shu-Juan;Zhang, Hong-Jun;Lin, Hou-Wen
从南中国海绵Hippospongia lachne中分离得到8个新的与甘露内酯相关的开环倍半萜类化合物，Hippolids A H(1-8)和(6e)-新甘露内酯(9)和(6z)-新甘露内酯(10)。用改进的Mosher方法和CD数据建立了1-8的绝对构型。化合物1对A549、HeLa和HCT-116细胞具有明显的细胞毒作用，其IC50值分别为5.22×10~(-2)、4.80×10~(-2)和9.78µM。化合物1具有中等的PTP1B抑制活性，IC50值为23.81mU，化合物2对HCT-116细胞具有中等的细胞毒作用，IC50值分别为35.13和39.67YM。此外，化合物1和5的抗炎活性较弱，对PKC-γ和PKC-α的IC50值分别为61.97和40.35µM。
Eight new acyclic manoalide-related sesterterpenes, hippolides A H (1-8), together with two known manoalide derivatives, (6E)-neomanoalide (9) and (6Z)-neomanoalide (10), were isolated from the South China Sea sponge Hippospongia lachne. The absolute configurations of 1-8 were established by the modified Mosher's method and CD data. Compound 1 exhibited cytotoxicity against A549, HeLa, and HCT-116 cell lines with IC50 values of 5.22 x 10(-2), 4.80 x 10(-2), and 9.78 mu M, respectively. Compound 1 also showed moderate PTP1B inhibitory activitiy with an IC50 value of 23.81 mu M, and compound 2 showed moderate cytotoxicity against the HCT-116 cell line and PTP1B inhibitory activity with IC50 values of 35.13 and 39.67 yM, respectively. In addition, compounds 1 and 5 showed weak anti-inflammatory activity, with IC50 values of 61.97 and 40.35 mu M for PKC gamma and PKC alpha, respectively.