Cleoserrata serrata is used in Mexican-south traditional medicine to treat chicleros ulcer. The phytochemical profile and the anti-inflammatory effect from four extracts obtained by maceration proccess and of the primary fractions from two extracts are described. In addition, the antioxidant, leishmanicidal and antimycobaterial activities and LD 50 from active extracts are reported. Anti-inflammatory activity was evaluated in TPA and carrageenan assays. Ethyl palmitate and γ-sitosterol were detected in Hexanic and CH 2 Cl 2 extracts. Same compounds and stigmasta-3,5-dien-7-one, palmitic acid, phytol acetate and phytol were detected in primary fractions from CH 2 Cl 2 :EtOH extract. In this and in MeOH extracts a polyphenolmixture was obtained. The MeOH extract was subjected to acid hydrolysis, and kaempferol, quercetin and scopoletin were detected in organic-phase. Polyphenol-mixture and organic-phase (IC 50 =3730 and 2338 μg/mL) showed moderate antioxidant activity; meanwhile MeOH extract exhibited scarce activity. In carrageenan model, Hexanic extract and polyphenol-mixture showed ED 50 =131.46 and 64.89 mg/ kg, respectively. Three extracts were active but not-dose-dependent. In TPA-model, CH 2 Cl 2 extract and polyphenol-mixture showed ED 50 <0.79 mg/ear, and three extracts were active, however the effect was not-dose-dependent. CH 2 Cl 2 :EtOH showed antimycobacterial and leishmanicidal activities. The LD 50 was >2 g/kg for all extracts.