[Moxibustion combined with acupoint catgut embedding promotes recovery of injured colonic mucosa by suppressing inflammation in ulcerative colitis rats].

OBJECTIVE: To observe the effect of moxibustion and acupoint catgut embedding (ACE) at "Tianshu"(ST25) "Dachangshu"(BL25) and "Shangjuxu"(ST37) on changes of body mass, stool property, histopathological conditions and expression levels of interleukin 6 (IL-6) in colonic mucosa of ulcerative colitis (UC) rats, so as to reveal its anti-inflammatory mechanisms underlying improvement of UC. METHODS: SD rats were randomized into normal, model, moxibustion, ACE and moxibustion＋ACE groups (n＝6 in each group). The UC model was established by enema of trinitro-benzene-sulfonic acid and ethanol. Moxibustion was applied to bilateral ST25, BL25 and ST37 for 10 min, once daily for 14 days, and ACE applied to the same 3 acupoints, once a week for two weeks. After the treatment, the rats' general conditions were observed, and the severity of UC was assessed by using disease activity index (DAI) score. Colonic mucosal pathological changes were observed under microscope after hematoxylin eosin (H.E.) stain, and the expression levels of IL-6 in the colonic mucosa tissue detected by using immunohistochemical stain and Western blot, respectively. RESULTS: After modeling, the DAI score, and expression level of colonic IL-6 protein detected by immunohistochemistry and Western blot were obviously increased in the model group relevant to the normal group (P<0.01). Following the intervention, the increase of DAI score and IL-6 expression were reversed in moxibustion, ACE and moxibustion＋ACE groups (P<0.01, P<0.05). The therapeutic effects of moxibustion＋ACE were considerably superior to those of simple ACE and simple moxibustion in down-regulating the levels of DAI score and IL-6 expression (P<0.01). H．E. staining showed severe defect of the colonic mucosal epithelium with infiltration of a large number of inflammatory cells in the model group, which was milder in moxibustion, ACE and moxibustion＋ACE groups. CONCLUSION: Moxibustion combined with ACE is able to improve the inflammatory injury of colonic mucosa in UC rats, which may be related with its effect in suppressing the expression of colonic IL-6; and the efficacy of moxibustion＋ACE is apparently superior to that of moxibustion and ACE alone.

Preparation of S14161 and its analogues and the discovery of 6-bromo-8-ethoxy-3-nitro-2H-chromene as a more potent antitumor agent in vitro.

The small chemical compound 8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene (S14161) was recently identified as an inhibitor of the phosphoinositide 3-kinase (PI3K). In the present study, we designed a novel synthesis of S14161 and prepared a series of its analogues via the oxa-Michael-Henry reaction in the presence of catalytic amounts of l-proline and triethylamine. Further structural simplification led to the identification of 6-bromo-8-ethoxy-3-nitro-2H-chromene (BENC-511) that exhibited potent antiproliferative activities against a panel of 12 tumor cell lines. Compared with S14161, BENC-511 was more potent in blocking the AKT phosphorylation and inducing cancer cell apoptosis. BENC-511 also displayed more potent effects on human umbilical vein epithelial cells (HUVEC) migration, suggesting its anti-angiogenesis activity.