Jia Yan-jun, Zhang Yan, Liu Jun, Guo Yuan-lin, Xu Rui-xia, Li Jian-jun
Division of Dyslipidemia, State Key Laboratory of Cardiovascular Disease, Fuwai Hospital, National Center for Cardiovascular Disease, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100037, China.
Chin J Integr Med. 2016 Feb;22(2):96-100. doi: 10.1007/s11655-014-1846-y. Epub 2014 Jul 4.
To investigate the short- and long-term effects of Xuezhikang (XZK), an extract of cholestin, on proprotein convertase subtilisin/kexin type 9 (PCSK9) level.
Thirty rats were randomly divided into three groups and were given saline, XZK 1,200 mg/kg or lovastatin 10 mg/kg respectively by daily gavage for 3 days (n=10 for each). Sixteen patients without previous lipid-lowering drug treatment for dyslipidemia received XZK 1,200 mg daily for 8 weeks. Fasting blood samples and liver tissue were collected at day 3 for rats, while the blood samples were obtained at baseline and week 8 from patients. The serum PCSK9 and lipid profile were measured. The expression of hepatic low density lipoprotein (LDL) receptor and sterol regulatory element binding protein 2 (SREBP-2) were measured by real time-PCR.
PCSK9 levels in rats were significantly increased in the XZK and lovastatin groups (P=0.002, P=0.003 vs. control) at day 3, while no significant differences were found in the levels of lipid parameters. PCSK9 levels in patients increased by 34% (P=0.006 vs. baseline) accompanied by total cholesterol and LDL-cholesterol decreased by 22% and 28% P=0.001, P=0.002 vs. baseline). The hepatic mRNA levels of LDL-receptor and SREBP-2 were significantly increased in the XZK and lovastatin groups.
XZK has significant impact on PCSK9 in a short- and long-term manner in both rats and humans. Moreover, the data indicated that as lovastatin, XZK increased PCSK9 levels through SREBP-2 pathway.
研究血脂康（XZK，一种红曲提取物）对前蛋白转化酶枯草溶菌素/kexin 9型（PCSK9）水平的短期和长期影响。
30只大鼠随机分为三组，分别每日经口灌胃给予生理盐水、1200mg/kg血脂康或10mg/kg洛伐他汀，共3天（每组n = 10）。16例既往未接受过降脂药物治疗的血脂异常患者每日服用1200mg血脂康，共8周。大鼠在第3天采集空腹血样和肝组织，而患者在基线和第8周采集血样。检测血清PCSK9和血脂谱。通过实时定量PCR检测肝低密度脂蛋白（LDL）受体和固醇调节元件结合蛋白2（SREBP-2）的表达。
第3天时，血脂康组和洛伐他汀组大鼠的PCSK9水平显著升高（与对照组相比，P = 0.002，P = 0.003），而血脂参数水平无显著差异。患者的PCSK9水平升高了34%（与基线相比，P = 0.006），同时总胆固醇和低密度脂蛋白胆固醇分别降低了22%和28%（与基线相比，P = 0.001，P = 0.002）。血脂康组和洛伐他汀组肝LDL受体和SREBP-2的mRNA水平显著升高。
血脂康在大鼠和人类中对PCSK9均有短期和长期的显著影响。此外，数据表明，与洛伐他汀一样，血脂康通过SREBP-2途径增加PCSK9水平。
