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柴胡皂苷 D 抑制选择素介导的细胞黏附。

Saikosaponin D isolated from Bupleurum falcatum inhibits selectin-mediated cell adhesion.

机构信息

Enviromental Agriculture Research Division, Gyeonggido Agricultural Reaearch and Extension Services(GARES), Hwaseong, Gyeonggi-do 445-784, Korea.

Bioindustial Process Research Center, Korea Research Institute of Bioscience and Biotechnology (KRIBB), Jeongeup-si, Jeollabuk-do 580-185, Korea.

出版信息

Molecules. 2014 Dec 4;19(12):20340-9. doi: 10.3390/molecules191220340.

DOI:10.3390/molecules191220340
PMID:25486247
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6271981/
Abstract

Three saikosaponins were isolated from the MeOH extract of the roots of Bupleurum falcatum L.: saikosaponins B3 (1); B4 (2); and D (3). Of the three, compound 3 inhibited the interaction of selectins (E, L, and P) and THP-1 cells with IC50 values of 1.8, 3.0 and 4.3 µM, respectively. Also, the aglycone structure 4 of compound 3 showed moderate inhibitory activity on L-selectin-mediated cell adhesion. From these results, we suspect that compound 3 isolated from Bupleurum falcatum roots would be a good candidate for therapeutic strategies to treat inflammation.

摘要

从柴胡根的甲醇提取物中分离得到三种柴胡皂苷

柴胡皂苷 B3（1）；B4（2）；和 D（3）。这三种化合物中，化合物 3 对选择素（E、L 和 P）与 THP-1 细胞的相互作用具有抑制作用，IC50 值分别为 1.8、3.0 和 4.3µM。此外，化合物 3 的苷元结构 4 对 L-选择素介导的细胞黏附也表现出中等抑制活性。基于这些结果，我们怀疑从柴胡根中分离得到的化合物 3 可能是治疗炎症的一种有前途的治疗策略候选药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/ec05241f812f/molecules-19-20340-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/8243882a826c/molecules-19-20340-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/0317adfa29cc/molecules-19-20340-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/9613f1aa0f79/molecules-19-20340-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/5edf828766bc/molecules-19-20340-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/ec05241f812f/molecules-19-20340-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/8243882a826c/molecules-19-20340-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/0317adfa29cc/molecules-19-20340-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/9613f1aa0f79/molecules-19-20340-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/5edf828766bc/molecules-19-20340-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e23/6271981/ec05241f812f/molecules-19-20340-g005.jpg

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本文引用的文献

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Expression and function of endothelial selectins during human development.内皮选择素在人类发育过程中的表达与功能
Immunology. 2014 Nov;143(3):406-15. doi: 10.1111/imm.12318.
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Saikosaponin a inhibits the proliferation and activation of T cells through cell cycle arrest and induction of apoptosis.柴胡皂苷a通过细胞周期阻滞和诱导凋亡来抑制T细胞的增殖和活化。
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Saikosaponin-d inhibits T cell activation through the modulation of PKCtheta, JNK, and NF-kappaB transcription factor.柴胡皂苷d通过调节蛋白激酶Cθ、应激活化蛋白激酶和核因子κB转录因子来抑制T细胞活化。
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Development of cell adhesion molecule antagonists as therapeutics for asthma and COPD.开发细胞粘附分子拮抗剂作为哮喘和慢性阻塞性肺疾病的治疗药物。
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Lymphocyte homing and leukocyte rolling and migration are impaired in L-selectin-deficient mice.在缺乏L-选择素的小鼠中，淋巴细胞归巢以及白细胞滚动和迁移均受损。
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