ABSTRACT
Atherosclerotic cardiovascular disease (ASCVD) frequently results in sudden death and poses a serious threat to public health worldwide. The drugs approved for the prevention and treatment of ASCVD are usually used in combination but are inefficient owing to their side effects and single therapeutic targets. Therefore, the use of natural products in developing drugs for the prevention and treatment of ASCVD has received great scholarly attention. Andrographolide (AG) is a diterpenoid lactone compound extracted from Andrographis paniculata. In addition to its use in conditions such as sore throat, AG can be used to prevent and treat ASCVD. It is different from drugs that are commonly used in the prevention and treatment of ASCVD and can not only treat obesity, diabetes, hyperlipidaemia and ASCVD but also inhibit the pathological process of atherosclerosis (AS) including lipid accumulation, inflammation, oxidative stress and cellular abnormalities by regulating various targets and pathways. However, the pharmacological mechanisms of AG underlying the prevention and treatment of ASCVD have not been corroborated, which may hinder its clinical development and application. Therefore, this review summarizes the physiological and pathological mechanisms underlying the development of ASCVD and the in vivo and in vitro pharmacological effects of AG on the relative risk factors of AS and ASCVD. The findings support the use of the old pharmacological compound ('old bottle') as a novel drug ('novel wine') for the prevention and treatment of ASCVD. Additionally, this review summarizes studies on the availability as well as pharmaceutical and pharmacokinetic properties of AG, aiming to provide more information regarding the clinical application and further research and development of AG.
ABSTRACT
To determine the concentration of menthol in rat plasma by GC. Rats were administered with single dose of Zhike Chuanbei Pipa dropping pills (ZCPDP) and different doses of menthol herbs. DAS 3. 1.6 software was used to calculate pharmacokinetic parameters, and the accumulative absorption percentage of menthol was calculated by Loo-Riegelman method. The linear regression analysis was made in vitro/in vivo accumulative absorption percentages to detect the in vitro/in vivo correlation. The results of the study showed that the pharmacokinetics behavior of menthol in ZCPDP was in conformity with two-compartment model characteristics. The main parameters were: tmax was 10 min, t1/2beta was (183. 93 52. 75) min, CL/F was (0. 426 +/- 0. 194) L . min-1 . kg-1, all of which were no difference between ZCPDP and menthol herbs with the same dosage. There were significant differences in tmax, t1/2beta, CL/F between menthol herbs with different dosages (P <0. 05) , with indirect proportion between AUC0-infinity and dosage. The regression equation of ZCPDP's accumulative absorption percentage and accumulative release percentage was Fa = 1. 160 3Q - 19. 968, r = 0. 981 3. These results suggested that the pharmacokinetics behavior was similar between ZCPDP and menthol herbs with the same dosage in rats, with good in vitro/in vivo correlation. There were significant differences in pharmacokinetics of menthol in the range of 19.2-570 mg . kg-1.