1.The interactions between natural products and OATP1B1.
Meizhi SHI ; Yu LIU ; Jialin BIAN ; Meng JIN ; Chunshan GUI
Acta Pharmaceutica Sinica 2015;50(7):848-53
Organic anion transporting polypeptide 1B1 (OATP1B1) is an important liver-specific uptake transporter, which mediates transport of numerous endogenous substances and drugs from blood into hepatocytes. To identify and investigate potential modulators of OATP1B1 from natural products, the effect of 21 frequently used natural compounds and extracts on OATP1B1-mediated fluorescein methotrexate transport was studied by using Chinese hamster ovary cells stably expressing OATP1B1 (CHO-OATP1B1) in 96-well plates. This method could be used for the screening of large compound libraries. Our studies showed that some flavonoids (e.g., quercetin, quercitrin, rutin, chrysanthemum flavonoids and mulberrin) and triterpenoids (e.g., glycyrrhetinic acid and glycyrrhizic acid) were inhibitors of OATP1B1 with IC50 values less than 16 µmol · L(-1). The IC50 value of glycyrrhetinic acid on OATP1B1 was comparable to its blood concentration in clinics, indicating an OATPlB1-mediated drug-drug interaction could occur. Structure-activity relationship analysis showed that flavonoids had much higher inhibitory activity than their glycosides. Furthermore, the type and length of saccharides had a significant effect on their activity. In addition, we used OATP1B1 substrates fluvastatin and rosuvastatin as probe drugs to investigate the substrate-dependent effect of several natural compounds on the function of OATP1B1 in vitro. Our results demonstrated that the effect of these natural products on the function of OATPlB1 was substrate-dependent. In summary, this study would be conducive to predicting and avoiding potential OATP1B1-mediated drug-drug and drug-food interactions and thus provide the experimental basis and guidance for rational drug use.
2.Clinical Observation on Treatment of Advanced Menorrhea with QingJing Capsule
Xiaojin ZHANG ; Jialin YANG ; Shaobin WEI ; Hong DING ; Suiqi GUI
Traditional Chinese Drug Research & Clinical Pharmacology 1993;0(01):-
Objective To investigate the effect of Qingjing Capsule (QC) in treating advance menorrhea (AM) and to evaluate its safety. Methods Double- blind, double- imitating, parallel- controlled and randomized trial was performed in 63 cases of AM with deficiency- heat syndrome.Thirty- two cases was in QC group(Group A) and other 31 in Gujing pill group(Group B).The menstrual cycle, clinical symptoms and signs, basal body temperature (BBT), serum levels of estradiol (E2) and progesterone and endometrium biopsy were observed to evaluate the effects of QC. Results The short- term markedly- effective rate was 90.63% and 77.42% and the short- term effective rate was 96.88% and 93.55% in Group A and Group B respectively. The long- term markedly- effective rate was 83.87% and 67.74% and the long- term effective rate was 93.55% and 80.65% in Group A and Group B respectively. The long- term markedly- effective rate in QC group is superior to that in Gujing pill group, the differences being significant(P
3.Influence of popularizing relevant knowledge on voluntary blood donation of patients′ families: in terms of knowledge, attitude and practice
Shujun SHAO ; Hongwei MA ; Na WANG ; Lanju WANG ; Xin QI ; Zongjian LIU ; Shuaiqi LAN ; Jialin GUI
Chinese Journal of Blood Transfusion 2021;34(12):1354-1356
【Objective】 To investigate the influence of knowledge popularization concerning blood donation and blood use on the knowledge, attitudes and practice(KAP) of voluntary blood donation of patients′ families. 【Methods】 Knowledge popularization on voluntary blood donation and clinical blood use was conducted to family members of tumor patients. A questionnaire was designed according to KAP theory to capture the general situation, blood donation history and demographic characteristics of patients′ family members, their knowledge on blood donation and clinical blood use, as well as their intention, attitude and behavior changes on voluntary blood donation before and after popularization. 【Results】 13.49%(104/771) of the family members of tumor patients donated, and most of them aged 28~37 years old(19.7%, 26/132). The awareness rate of patients′ family members on voluntary blood donation and clinical blood use after popularizing was significantly increased as compared with before(P<0.05). Especially, the awareness rate of "blood transfusion significance and the risk of infectious diseases", and " patients were given priority to use blood if their family members donated blood" increased to 61.35%(473/771) and 68.74%(530/771), respectively.Their intention, attitude and behavior of blood donation also changed significantly(P<0.05). The intention of supporting voluntary blood donation increased to 78.21%(603/771), and non-supporting decreased to 4.15%(32/771). Such three behaviors led to a donation rate higher than 70% as donating for charity and sense of responsibility(74.06%, 571/771), donating blood after reassuring(70.69%, 545/771), and promoting their family members′ priority in blood use(71.47%, 551/771). 【Conclusion】 The popularization of knowledge concerning blood donation and blood use can change the intention and attitude of patients′ family members towards voluntary blood donation and further effectively promote their donation behavior.