College of Pharmacy, Jinan University, Guangzhou 510632, China.
College of Pharmacy, Jinan University, Guangzhou 510632, China.
Chin J Nat Med. 2018 Nov;16(11):871-880. doi: 10.1016/S1875-5364(18)30129-8.
Poliumoside is representative of phenylethanoid glycosides, which are widely found in many plants. Poliumoside is also regarded as the main active component of Callicarpa kwangtungensis Chun (CK), though its oral bioavailability in rat is extremely low (0.69%) and its in vivo and in vitro metabolism has not yet been systematically investigated. In the present study, an ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) method was employed to identify the metabolites and investigate the metabolic pathways of poliumoside in rat after oral administration 1.5 g·kg of poliumoside. As a result, a total of 34 metabolites (30 from urine, 17 from plasma, and 4 from bile) and 9 possible metabolic pathways (rearrangment, reduction, hydration, hydrolyzation, dehydration, methylation, hydroxylation, acetylation, and sulfation) were proposed in vivo. The main metabolite, acteoside, was quantified after incubated with rat intestinal bacteria in vitro. In conclusion, the present study systematically explored the metabolites of poliumoside in vivo and in vitro, proposing metabolic pathways that may be significant for further metabolic studies of poliumoside.
梓醇苷是苯乙醇苷类的代表化合物,广泛存在于多种植物中。梓醇苷也被认为是岗梅(Callicarpa kwangtungensis Chun)(CK)的主要活性成分,尽管其在大鼠体内的口服生物利用度极低(0.69%),但其体内和体外代谢尚未得到系统研究。本研究采用超高效液相色谱/四极杆飞行时间质谱(UPLC/Q-TOF-MS)法鉴定大鼠口服 1.5 g·kg 梓醇苷后梓醇苷的代谢产物并探讨其代谢途径。结果,共鉴定出 34 种代谢产物(尿液中 30 种,血浆中 17 种,胆汁中 4 种)和 9 种可能的代谢途径(重排、还原、水合、水解、脱水、甲基化、羟化、乙酰化和硫酸化)。将梓醇苷与大鼠肠道细菌在体外孵育后,对主要代谢产物獐牙菜苷进行了定量分析。总之,本研究系统地探讨了梓醇苷在体内和体外的代谢产物,提出了可能对进一步研究梓醇苷代谢具有重要意义的代谢途径。