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总二萜类化合物通过抑制肾组织 PKC 活性改变水通道蛋白表达从而抑制腹水生成

Anti-Malignant Ascites Effect of Total Diterpenoids from Radix Is Attributable to Alterations of Aquaporins via Inhibiting PKC Activity in the Kidney.

机构信息

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.

Jiangsu Key Laboratory of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Nanjing 210023, China.

出版信息

Molecules. 2021 Feb 10;26(4):942. doi: 10.3390/molecules26040942.

DOI:10.3390/molecules26040942
PMID:33578967
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7916655/
Abstract

This study evaluated the anti-ascites effect of total diterpenoids extracted from Radix (TDEE) on malignant ascitic mice and elucidated its underlying mechanism. TDEE was extracted by dichloromethane and subjected to column chromatography. The purity of six diterpenoids isolated from TDEE was determined to be 77.18% by HPLC. TDEE (3 and 0.6 g raw herbs/kg, p.o.) reduced ascites and increased urine output. Meanwhile, analysis of tumor cell viability, cycle and apoptosis indicated that TDEE had no antitumor activity. In addition, the expression levels of aquaporins (AQPs) and the membrane translocation levels of protein kinase C (PKC) α and PKCβ in kidney and cells were measured. TDEE reduced the levels of AQP1-4, and inhibited PKCβ expression in membrane fraction. Four main diterpenoids, except compound , reduced AQP1 level in human kidney-2 cells. Compounds and inhibited AQP2-4 expression in murine inner medullary collecting duct cells. The diterpenoid-induced inhibition of AQP1-4 expression was blocked by phorbol-12-myristate-13-acetate (PMA; agonist of PKC). The diterpenoids from TDEE are the main anti-ascites components. The anti-ascites effect of diterpenoids may be associated with alterations in AQPs in the kidneys to promote diuresis. The inhibition of AQP1-4 expression by TDEE is related to the inhibition of PKCβ activation.

摘要

本研究评价了从 Radix 中提取的总二萜（TDEE）对恶性腹水小鼠的抗腹水作用，并阐明了其作用机制。TDEE 用二氯甲烷提取，并用柱色谱法进行分离。通过高效液相色谱法确定从 TDEE 中分离的六种二萜的纯度为 77.18%。TDEE（3 和 0.6 g 生药/kg，po）减少腹水并增加尿量。同时，肿瘤细胞活力、周期和凋亡分析表明 TDEE 没有抗肿瘤活性。此外，还测量了水通道蛋白（AQPs）的表达水平和蛋白激酶 C（PKC）α和 PKCβ在肾脏和细胞中的膜转位水平。TDEE 降低了 AQP1-4 的水平，并抑制了 PKCβ在膜部分的表达。除化合物 外的四种主要二萜降低了人肾-2 细胞中的 AQP1 水平。化合物 和 抑制了小鼠内髓集合管细胞中 AQP2-4 的表达。PKC 激动剂佛波醇-12-肉豆蔻酸-13-醋酸酯（PMA）阻断了二萜诱导的 AQP1-4 表达抑制。TDEE 中的二萜是主要的抗腹水成分。二萜的抗腹水作用可能与肾脏中 AQPs 的改变有关，以促进利尿。TDEE 对 AQP1-4 表达的抑制与 PKCβ 激活的抑制有关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/204a2d40c914/molecules-26-00942-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/27d8f65c81ad/molecules-26-00942-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/b12cb872a5eb/molecules-26-00942-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/ff0eaf86f6a0/molecules-26-00942-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/6c1b92d98dad/molecules-26-00942-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/cc711df7760c/molecules-26-00942-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/1df07785c06c/molecules-26-00942-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/a6f9bb2b162c/molecules-26-00942-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/fb16c29d46d0/molecules-26-00942-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/8514a68f5e01/molecules-26-00942-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/204a2d40c914/molecules-26-00942-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/27d8f65c81ad/molecules-26-00942-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/b12cb872a5eb/molecules-26-00942-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/ff0eaf86f6a0/molecules-26-00942-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/6c1b92d98dad/molecules-26-00942-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/cc711df7760c/molecules-26-00942-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/1df07785c06c/molecules-26-00942-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/a6f9bb2b162c/molecules-26-00942-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/fb16c29d46d0/molecules-26-00942-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/8514a68f5e01/molecules-26-00942-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6078/7916655/204a2d40c914/molecules-26-00942-g010.jpg

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