ABSTRACT Purpose: To investigate the impact of the Chinese medicine compound Ento-PB on oxazolone (OXZ)-induced ulcerative colitis (UC) in rats. Methods: UC rats induced by OXZ were treated with Ento-PB. The damage to the colon was assessed using several measures, including the disease activity index (DAI), colon length, colon weight/length ratio, colonic mucosal damage index, and histological score. The levels of interleukin-4 (IL-4), interleukin-10 (IL-10), interleukin-13 (IL-13), epidermal growth factor (EGF), inducible nitric oxide synthase, and total nitric oxide synthase (tNOS) in rat serum, as well as the levels of tumor necrosis factor-α (TNF-α) and myeloperoxidase (MPO) in rat colon tissue, were determined using enzyme-linked immunosorbent assay and conventional kits. Results: After being treated with Ento-PB, the DAI score and macroscopic lesion score of OXZ-induced UC rats were significantly reduced. Ento-PB prevented the shortening of rat colons, reduced the ratio of colon weight to length, and improved colon tissue lesions. Meanwhile, Ento-PB could significantly inhibit the activities of proinflammatory cytokines TNF-α, IL-13, and MPO, as well as tNOS and iNOS, while upregulating the expression of anti-inflammatory cytokines IL-4 and IL-10. Moreover, a significant increase in the expression level of EGF was observed in UC rats treated with Ento-PB, indicating that Ento-PB could enhance the repair of damaged intestinal epithelial tissue. Conclusions: Ento-PB demonstrates significant anti-UC activities in OXZ-induced UC rats by regulating the expression levels of inflammatory factors and promoting the repair of colon tissue. This study provides scientific evidence to support the further development of Ento-PB. Purpose EntoPB Ento PB OXZinduced (UC Methods EntoPB. PB. measures DAI, , (DAI) length weightlength interleukin4 interleukin 4 interleukin- IL4, IL4 IL (IL-4) interleukin10 10 interleukin-1 IL10, IL10 (IL-10) interleukin13 13 IL13, IL13 (IL-13) EGF, (EGF) (tNOS serum factorα α TNFα TNF (TNF-α MPO (MPO enzymelinked enzyme linked kits Results EntoPB, PB, colons lesions Meanwhile TNFα, α, TNF-α 13, IL-13 iNOS antiinflammatory anti IL- IL10. 10. IL-10 Moreover Conclusions antiUC (DAI (IL-4 interleukin1 1 IL1 (IL-10 (IL-13 (EGF IL-1 (IL- (IL-1 (IL

Este é o primeiro relato mostrando que 3-(diclorofenil)isocumarinas e (±)-3,4-(dihidroisocumarinas) são inibidores do crescimento de plantas e fungos. 3-Diclorofenilisocumarinas foram sintetizadas pela condensação de ácido homoftálico com cloretos de diclorobenzoíla. A hidrólise alcalina destas isocumarinas formou ceto ácidos. 3-(Diclorofenil)-3,4-dihidroisocumarinas racêmicas foram obtidas pela redução de ceto ácidos a hidróxi-ácidos racêmicos, seguida pela ciclodehidratação, usando anidrido acético. As atividades herbicida, fungicida e inseticida dos compostos sintetizados foram avaliadas. Alguns dos compostos sintetizados mostraram excelentes atividades fungicida e herbicida, mas nenhum deles apresentou efeito inseticida nos insetos usados nos testes. Este estudo sugere que isocumarinas e compostos relacionados podem ser usados como guias para o planejamento de herbicidas e fungicidas bioativos.

This is the first report showing that 3-(dichlorophenyl)isocoumarins and (±)-3,4-dihydroisocoumarins are plant and plant fungus growth inhibitors. 3-Dichlorophenylisocoumarins were synthesized by condensation of homophthalic acid with dichlorobenzoyl chlorides. The alkaline hydrolysis of these isocoumarins afforded keto acids. Racemic 3-(Dichlorophenyl)-3,4-dihydroisocoumarins were obtained by reduction of keto acids to racemic hydroxy acids, followed by cyclodehydration using acetic anhydride. The herbicidal, fungicidal and insecticidal activities of the synthesized compounds have been evaluated. Some of the synthesized compounds show excellent herbicidal and fungicidal activities but none of the synthesized compounds presented any insecticidal effects on the test insects. The findings of this study suggest that isocoumarins and related compounds may serve as lead compounds towards the design of bioactive herbicides and fungicides.