Research on Preparation of Colon-site Guar-based Hydrophilic Matrix Tablets Containing TASA And Its Therapeutic Effect on UC Mice
Ulcerative colitis (UC), non-specific autoimmune disease, is a idiopathic, chronic, relapsing inflammatory conditions that are immunologically mediated and is characterized by bloody diarrhea, abdominal cramps, fatigue, weight loss, nausea, and so on.Its pathogenesis is inflammatory mucus of colon and ulceration.Prevalence of clinical studies indicate that the incidence of UC is 50-100 per 100 000, and the patients often develop UC at the age of 15-30 years old.Nowdays, the risk of UC for people increases with change of diet structure, lifestyle and increasing pressure in modern society.Patients with UC are at an increased risk of developing colorectal cancer, and so far, there isn”t still an effective measure in clinic.Hence, UC is regarded as one of refractory diseases by WHO.Although the etiologies of UC remains an enigma, the research work in animal models, human genetics and clinical trials, have provided new insights into the pathogenesis of these diseases.There is evidence that it involves the interaction of the immune system, genetic susceptibility and the environment.Most prevailing therapies for UC include glucocorticosteroids, sulfasalazine, and so on.However, the therapies not only show limited benefits, but also have unwanted side effects.Consequently, there is a need for alternative anti-inflammatory agents that are equally or more effective and cause fewer side effects.Some constituents of plants, particularly Sophora alopecurodes L., have been reported to be useful in the management of inflammatory bowel diseases in Chinese fork medicine for a long time.TASA are a mixture of extract from root or seed of Sophora alopecuroides L, Chinese medicine Ku-dou-zi.They are mainly made up of six active components i.e.sophoridine, sophocarpine, matrine, oxymatrine,sophoraramine, aloperine, and have been widely used as an ingredient approved by Chinese SFDA for many years, which contain not less than 24% sophoridine and not less than 95% alkaloids, calculated reference as sophoridine.The pharmacological studies have shown that TASA have pleiotropic effects including anti-inflammation, antivirus, antitumor and immunomodulation, and so on.Great evidences demonstrate the effectiveness of matrine and oxymatrine for colitis.Our recent work showed that TASA could yield protective effect against colitis in 2,4,6-trinitrobenzene sulphonic acid TNBS/ethanol-inducing rat via antioxidation and patented ”Application of TASA in drugs for UC treatment and the method for colon-site release preparation, ZL200410052029.0”.The advantages and necessity of colon targeting provide more effective therapy for colon-related diseases, such as irritable bowel syndrome, colon cancer and inflammatory bowel disease (IBD).Therefore, it is necessary to target TASA to colon in order to improve its effectiveness and delve its mechanism.
Total alkaloids of Sophora alopecuroides Ulcerative colitis Colon-site targetting NF-κB signal transduction pathway Chromatin immunoprecipitation assay
Zhao Wen-chang Song Li-jun
School of Pharmacy, Guangdong Medical University, Dongguan 523808, China
国内会议
世界中医药学会联合会中药新药创制专业委员会成立大会暨第一届学术年会
成都
英文
324-327
2016-03-26（万方平台首次上网日期，不代表论文的发表时间）