1.A new monacolin analogue from Xuezhikang capsule.
Xuemei LI ; Xinghai SHEN ; Zhenwen DUAN ; Shuren GUO
Acta Pharmaceutica Sinica 2011;46(5):564-7
Xuezhikang capsule (ethanol extract of red yeast rice) which produced by Beijing WBL Peking University Biotech Co., Ltd., is a traditional Chinese medication with 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibiting activity. Clinical trials indicated that Xuezhikang with lipid-lowering action could reduce the risk of cardiac events and total mortality of Chinese coronary heart disease patients. To exactly explain the clinical features of Xuezhikang, we undertook a complete study of the chemical constituents of Xuezhikang. This study resulted in the isolation of a new monacolin analogue, named alpha, beta-dehydromonacolin L (1), along with two known compounds: monacolin L (2) and 3-(2, 6-dimethyl-1, 2, 4a, 5, 6, 7, 8, 8a-octahydronaphthalen-1-yl)propanoic acid (3). The chemical structures were determined by extensive 1D and 2D NMR and MS spectroscopic analysis.
2.Optimization, validation and application of an assay for the activity of HMG-CoA reductase in vitro by LC-MS/MS
Jing WANG ; Jiye SUN ; Chunjie SHA ; Yufeng SHAO ; Yanhong LIU ; Youxin LI ; Zhenwen DUAN ; Wanhui LIU
Journal of Pharmaceutical Analysis 2015;(6):383-388
A stable HMG-CoA reductase (HMGR) reaction in vitro was developed by a sensitive, selective and precise liquid chromatography–tandem mass spectrometry (LC–MS/MS) method. The optimized enzyme reac-tion condition contained 1.5μg of HMGR, 20 nM of NADPH with 50 min of reaction time. The method was validated by several intra-and inter-day assays. The production transitions of m/z 147.0/59.1 and m/z 154.0/59.1 were used to detect and quantify mevalonolactone (MVAL) and MVAL-D7, respectively. The accuracy and precision of the method were evaluated over the concentration range of 0.005–1.000μg/mL for MVAL and 0.010–0.500μg/mL for lovastatin acid in three validation batch runs. The lower limit of quantitation was found to be 0.005μg/mL for MVAL and 0.010μg/mL for lovastatin acid. Intra-day and inter-day precision ranged from 0.95%to 2.39%and 2.26%to 3.38%for MVAL, 1.46%to 3.89%and 0.57% to 5.10% for lovastatin acid, respectively. The results showed that the active ingredients in Xuezhikang capsules were 12.2 and 14.5 mg/g, respectively. This assay method could be successfully applied to the quality control study of Xuezhikang capsule for the first time.
3.Epidemiologic study on thyroid nodules in community population of Jiangsu
Shangyong FENG ; Yan ZHU ; Zhenwen ZHANG ; Yu DUAN ; Xiaoyun LIU ; Xiaodong WANG ; Wei TANG ; Xiaodong MAO ; Shuhang XU ; Yu FENG ; Cuiping LIU ; Youwen QIN ; Hongbing SHEN ; Rongbin YU ; Ruifang BU ; Junjian CHEN ; Wei LI ; Zemin SHI ; Xu HU ; Chao LIU
Chinese Journal of Endocrinology and Metabolism 2011;27(6):492-494
The residents who had lived for at least 5 years and aged over 20 years old were sampled from urban to rural districts of Jiangsu Province with a stratified cluster sampling technique. B mode ultrasonography and thyroid function determination were carried out in 6 128 persons. The location, diameter, number, boundary, and calcification in thyroid nodules were described by using 7.5 MHz/50 mm transducer of thyroid ultrasonography. TSH was measured by chemiluminescence immunoassay. Free triiodothyronine(FT3)and free thyroxin(FT4)were measured when TSH was abnormal. The crude prevalence of thyroid nodules was 21.12% in total population, 14.55% in male, and 25.24% in female. The standardized prevalence was 15.69%, 11.20%, and 20.40%, respectively. The prevalence was lower in male than in female, and increased with age(P<0.05). Thyroid nodules in Jiangsu Province were highly prevalent and more attention should be paid to the follow-up, early diagnosis, and treatment.