Studies On The Chemical Constituents And Bioactivities Of Aconiti Lateralis Radix Praeparata

The daughter roots of Aconitum carmichaeli Debx.(Ranunculaceae), a famous Chinese traditional herbal known as "Fuzi", found mainly distributed in Jiangyou City of Sichuan Province in China, have long been used as an analgesic, anti-inflammatory and anti-tumor agent in clinic for more than two thousand years.Traditional theories of Chinese medical science deem that, Fuzi is very hot and toxic and the only processed aconite roots can be used to treat disease. Modern experimental studies have shown that diester diterpenoid alkaloids in Fuzi are active ingredients and toxic ones at same time. This toxic diterpenoid alkaloids have cardiac, analgesic, anti-inflammatory activity. But, except for diterpenoid alkaloids, what is other effective material basis for? In order to find more effective and less toxic natural ingredients, a preliminary study of its composition and pharmacological effects is conducted, providing valuable reference for the clinical application.This dissertation consists of three parts mainly:Chapter1:Summary on the literatures of Aconitum carmichaeli Debx..By consulting and sorting the relevant literatures, the research of chemical constituents and bioactivities in recent50years has been reviewed of plants from Fuzi, Aconitum carmichaeli Debx.. This plant mostly contains the constituents such as diterpenoid alkaloid, polysaccharide, fatty acid, flavonoid, et al. These compounds or plant extracts mainly show cardioactive, analgesic, anti-inflammatory, insecticidal, hpyerglycemic activities and so on. The systemic research about chemical constituents and bioactivities of Fuzi will play important roles in the discovery of novel natural products and active constituents, and provide valuable reference for the clinical application.Chapter2:Study on chemical constituents of Fuzi. The compounds were isolated and purified by recrystallization and column chromatography with silica gel. Their structures were elucidated on the basis of physicochemical properties and spectral analysis. Twenty-six compounds were isolated and twenty-one compounds were identified respectively, includining ten C-19diterpenoid alkaloids, two C-20diterpenoid alkaloids, two ceramides, one base, two steroids, four fatty acids compounds and at al.Ten C-19diterpenoid alkaloids:lipopenduline (1)、mesaconitine (2)、hypaconitine (3)、penduline (4)、hokbusine A (8-O-methyl-benzoylmesaconine)(5)、neoline (6)、lipoaconitine (7)、lipomesaconitine (8)、lipohypaconitine (9)、lipodeoxyaconitine (10).Two C-20diterpenoid alkaloids:songorine (11)、songoramine (12)Two ceramides:(2S,3S,4R,8E)-2-[(2’R)-2’-hydroxylignoceroylamino]-8(E)-octadec ene-1,3,4-triol(13)、1-O-β-D-glucopyranosyl-(2S,3S,4R,8E)-2-[(2’R)-2’-hydroxy-tetraco sanoyl]-8(E)-octadecene-1,3,4-triol (14)One base:urical (15).Two steroids:p-sitosterol (16)、daucosterol (17)Four fatty acids:glyceryl monopalmitate (18)、palmitic acid (19)、tridecanoic acid (20)、linoleic acid (21)Chapter3:The analgesic effect of different isolated diterpenoid alkaloids were tested by the acetic acid-induced writhing body method in mice, and the cytotoxic activity were tested against several cell lines (A549、Bel-7402、HCT-8) by the MTT method. The results showed that mesaconitine (diester alkaloid)obviously decreased the times of the acetic acid-induced writhing test in mice, having a significant analgesic activity. By contrast, other lipo-alkaloids and neoline that are less poison display not obvious analgesic and cytotoxic activity in5μg/mL.