GuangYu Chen, JuanJiang Wu, Huaxue Huang, Jianan Mao, Shuang Zhan, Zhi Peng, Dai Liu, Wang Wei
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引用次数: 0
Abstract
Ethnopharmacological relevance: Siraitia grosvenorii (S. grosvenorii) is a traditional herbal medicine employed for the prevention of lung diseases. Mogrosides and flavonoids are postulated to be the principal active components. Nevertheless, the dynamic distribution of its active components in vivo and the amount of accumulation in the lung target tissue remain indistinct.
Aim of the study: This study investigates the dynamic distribution patterns of 9 bioactive components within the extract of S. grosvenorii in rat blood, heart, liver, spleen, lung, and kidney, along with its pulmonary targeting.
Materials and methods: The blood, heart, liver, spleen, lung, and kidney samples of rats were obtained at diverse time points after oral administration of S. grosvenorii decotion, and a UPLC-MS/MS method was developed to determine the contents of 9 bioactive components (Siamenoside I, Grosvenorine, 11-O-Mogroside V, Mogroside II-E, Mogroside III-E, Mogroside IV-A, Mogroside V, Mogroside VI and Kaempferitrin) within the samples. The concentration-time curves of each component in each sample were plotted and the pharmacokinetic parameters were computed.
Results: The AUC0→∞ and Cmax of 9 bioactive components in lung tissue were conspicuously higher than those in heart, liver, spleen, and kidney. For instance, the AUC0→∞ of Mogroside V in lung tissue was 7.20 to 55.54 times higher than that in blood and other tissues, and the Cmax in lung tissue was 3.315 to 96.70 times higher than that in blood and other tissues. The lung target efficiency of 9 bioactive components ranged from 1.885 to 15.80, indicating that the active components of S. grosvenorii exerting pharmacological effects are highly concentrated in the lung target tissue. The Tmax of 9 bioactive components in blood was within the range of 10.20 to 100.2 min, while the Tmax of the heart and liver was 20 min. The Tmax of all the components in the lung was 50 min, while the Tmax of the spleen and kidney was from 80 to 100 min, suggesting that 9 bioactive components entered the blood rapidly and then distributed to the heart and liver in large quantities, before entering the lung tissue in large quantities and eventually distributing to the spleen and kidney. The elimination half-life (T1/2) of the majority of 9 bioactive components was less than 1 hour, and the MRT of most of them was less than 3 hours.
Conclusions: S. grosvenorii is a naturally lung-targeted herbal medicine, and the clinical administration ought to be based on pharmacokinetic parameters such as Tmax, Cmax, AUC0→∞, T1/2, and MET0→∞ in lung tissue for designing a precise, rigorous, and rational administration plan.
期刊介绍：
The Journal of Ethnopharmacology is dedicated to the exchange of information and understandings about people''s use of plants, fungi, animals, microorganisms and minerals and their biological and pharmacological effects based on the principles established through international conventions. Early people confronted with illness and disease, discovered a wealth of useful therapeutic agents in the plant and animal kingdoms. The empirical knowledge of these medicinal substances and their toxic potential was passed on by oral tradition and sometimes recorded in herbals and other texts on materia medica. Many valuable drugs of today (e.g., atropine, ephedrine, tubocurarine, digoxin, reserpine) came into use through the study of indigenous remedies. Chemists continue to use plant-derived drugs (e.g., morphine, taxol, physostigmine, quinidine, emetine) as prototypes in their attempts to develop more effective and less toxic medicinals.
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