Key Laboratory of Modern Preparation of Traditional Chinese Medicine of Ministry of Education & Research Center of Natural Resources of Chinese Medicinal Materials and Ethnic Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, PR China.
College of Chemistry and Pharmaceutical Engineering, Nanyang Normal University, Nanyang 473061, PR China.
Bioorg Chem. 2021 Dec;117:105450. doi: 10.1016/j.bioorg.2021.105450. Epub 2021 Oct 23.
The fruit of Citrus medica L. var. sarcodactylis Swingle is not only used as a traditional medicinal plant, but also served as a delicious food. Six new (3'→7″)-biflavonoids (1-6), and twelve known biflavonoid derivatives (7-18) were isolated and characterized from the fruits of C. medica L. var. sarcodactylis Swingle for the first time. Their structures were determined by extensive and comprehensive analyzing NMR, HR-ESI-MS, UV, and IR spectral data coupled with the data described in the literature. Compounds (1-18) were evaluated for their hypolipidemic activities with Orlistat as the positive control, and assayed for their immunosuppressive activities with Dexamethasone as the positive control, respectively. Among them, compounds (1-3) exhibited moderate inhibition of pancreatic lipase activity by inhibiting 68.56 ± 1.40%, 56.18 ± 1.57%, 53.51 ± 1.59% of pancreatic lipase activities at the concentration of 100 μM, respectively. Compounds (4-6) and 8 showed potent immunosuppressive activities with the IC values from 16.83 ± 1.32 to 50.90 ± 1.79 μM. The plausible biogenetic pathway and preliminary structure activity relationship of the selected compounds were scientifically summarized and discussed in this study.
柑橘的果实不仅作为一种传统药用植物，而且也作为美味的食物。从柑橘果实中首次分离并鉴定了六种新的（3'→7″）-双黄酮（1-6）和十二种已知的双黄酮衍生物（7-18）。通过广泛而全面的分析 NMR、HR-ESI-MS、UV 和 IR 光谱数据，并结合文献中描述的数据，确定了它们的结构。将化合物（1-18）分别评估了它们的降脂活性，以奥利司他为阳性对照，评估了它们的免疫抑制活性，以地塞米松为阳性对照。其中，化合物（1-3）在 100μM 浓度下分别抑制胰腺脂肪酶活性 68.56±1.40%、56.18±1.57%和 53.51±1.59%，表现出中等的胰腺脂肪酶抑制活性。化合物（4-6）和 8 具有很强的免疫抑制活性，IC 值范围为 16.83±1.32 至 50.90±1.79μM。在本研究中，对选定化合物的可能生物合成途径和初步结构活性关系进行了科学总结和讨论。
