四環(huán)三萜化合物是植物來源中藥里具有多種生物活性的一類重要化合物，但研究發(fā)現(xiàn)四環(huán)三萜類化合物普遍口服生物利用度低，腸吸收不佳，嚴(yán)重影響了該類成分的開發(fā)和應(yīng)用。四環(huán)三萜類化合物按照苷元不同大致可以分為達瑪烷型、羊毛脂烷型、葫蘆素烷型、環(huán)阿屯烷型、原帖烷型、楝烷型等幾類，總結(jié)了不同結(jié)構(gòu)類型的四環(huán)三萜化合物單體的腸吸收機制，探討其腸吸收不佳的原因；綜述發(fā)現(xiàn)腸吸收多用于研究中藥單體、單味中藥和中藥復(fù)方配伍的有效吸收成分及其相互作用規(guī)律，并表明中藥配伍對有效成分的腸道吸收具有很好的改善作用，以期為改善中藥四環(huán)三萜類化合物的口服利用度、新劑型的研發(fā)設(shè)計以及臨床的合理用藥提供參考。

Tetracyclic triterpenes are a kind of important compounds with a variety of biological activities in traditional Chinese medicine, but it has been found that tetracyclic triterpenes have low oral bioavailability and poor intestinal absorption, which seriously affect the development and application of tetracyclic triterpenes. Intestinal perfusion in vivo and Caco-2 cell model are often used to study the intestinal absorption of drugs. According to the difference of aglycone, tetracyclic triterpenes can be roughly divided into damarane type, lanolin type, cucurbitane type, cycloartenane type, protopane type, neem type and so on. in this paper, the intestinal absorption mechanism of tetracyclic triterpenes with different structures was summarized, and the reasons for their poor intestinal absorption were discussed. It is found that intestinal absorption is mainly used to study the effective absorption components and their interaction of monomer, single traditional Chinese medicine and compound prescription of traditional Chinese medicine, and shows that the compatibility of traditional Chinese medicine can improve the intestinal absorption of effective components. in order to provide reference for improving the oral availability of tetracyclic triterpenes in traditional Chinese medicine, the research and design of new dosage forms and the rational use of drugs in clinic.

R969.1;R285.6

國家重點研發(fā)計劃資助項目（2019YFC1711300）；廣西科技重大專項（桂科AA18118049-3）；中醫(yī)藥國際合作專項（基地類項目）（0610-2140NF020630）