Estudio fitoquímico y evaluación del potencial antiinflamatorio/antioxidante de Cleoserrata serrata (Jacq.) Iltis

Abstract

Cleoserrata serrata (familia Cleomacea) es utilizada en el estado de Tabasco, México para tratar la “úlcera del chiclero”. En este trabajo se describe por primera vez el potencial antioxidante y antiinflamatorio de los extractos CH2Cl2:EtOH (CHS), Hex, CH2Cl2 y MeOH de C. serrata. Algunos componentes identificados en las fracciones de baja y mediana polaridad del extracto CHS fueron el palmitato de etilo, ácido palmítico, fitol, acetato de fitol, γ- y β-sitosterol, ácido linoleico, y γ-sitosterol. En las fracciones polares se identificó rutina, un glucosilado de acacetina. Del extracto MeOH se obtuvo un precipitado (pCHS), el cual fue acetilado y de este se obtuvo sacarosa y un glucoflavonoide. En la fase orgánica de la hidrólisis ácida del extracto MeOH, se identificó la quercetina, camferol, escopoletina, ácido p-cumárico. Los extractos CHS, MeOH y pCHS contienen aminoácidos, polifenoles (rutina), azúcares diversos y glucosinolatos. Los extractos Hex, CH2Cl2 y fracciones de CHS de menor polaridad tuvieron mejor actividad antiinflamatoria en el modelo de TPA y los extractos MeOH y fracciones de CHS de mayor polaridad tuvieron mejor efecto en el modelo de carragenina. En el modelo de inflamación crónica a 28 días, CHS (150 mg/kg) presentó mejor efecto antiinflamatorio que el control Fenilbutazona; (FBZ).

Cleoserrata serrata (family Cleomacea) is used in the state of Tabasco, Mexico to treat chewing gum ulcer. In this work, the antioxidant and anti-inflammatory potential of the extracts CH2Cl2:EtOH (CHS), Hex, CH2Cl2 and MeOH of C. serrata is described for the first time. Some components identified in the low and medium polarity fractions of the CHS extract were ethyl palmitate, palmitic acid, phytol, phytol acetate, γ- and β-sitosterol, linoleic acid, vitamin E, and γ-sitosterol and stigamasterol. Rutin, a glycosylated derivative of acacetin, was identified in the polar fractions. Linoleic acid ethyl ester, ethyl palmitate, vitamin E, and γ-sitosterol were identified in the Hex extract. Palmitic acid, vitamin E, stigamasterol, γ- and β-sitosterol were detected in the CH2Cl2 extract. A precipitate (pCHS) was obtained from the MeOH extract, which was acetylated and sucrose and an acacetin-type glucoflavonoid were obtained from it. Acid hydrolysis of the MeOH extract allowed the organic phase (HMeOH) to be obtained. In HMeOH, quercetin, campferol, scopoletin, p-coumaric acid were identified and sugars were detected in the aqueous phase. CHS, MeOH and pCHS extracts contain amino acids, polyphenols (rutin), sugars and glucosinolates. The antioxidant effect of the extracts of C. serrata was scarce. The anti-inflammatory effect of carrageenan, CHS at 300 mg/kg inhibited 60.83% at 5 hours and its primary fractions showed a better anti-inflammatory effect at lower doses. The Hex extract and pCHS showed a dose-dependent effect (ED50 = 131.46 and 64.86 mg/kg, respectively). The MeOH extract at the three doses tested showed around 45% inhibition, without a dose-dependent effect. HMeOH was more active at a lower dose (25 mg/kg). The sample rich in polyphenols (rCHS) showed 34.28% at 150 mg/kg. The anti-inflammatory effect evaluated in the TPA (phorbol ester) model, the CHS extract inhibited 66.66% at 1 mg/ear. The primary fractions of this extract were equal to or more active than the original extract. The MeOH and Hex extracts showed an inhibition of inflammation between 40 and 57% at 1 and 2 mg/ear, and only the CH2Cl2 and pCHS extracts showed a dose-dependent effect (ED50= 0.79 and 0.47 mg/ear). HMeOH at 0.5, 1 and 2 mg/ear inhibited 38.44, 37.51 and 41.03%, respectively. rCHS inhibited better than the positive control with 63.63% at 2 mg/ear. In the chronic inflammation model at 28 days, the CHS extract was administered i.g. from day 7 to 27. The CHS extract at a dose of 150 mg/kg presented a better anti-inflammatory effect than the positive control (Phenylbutazone; FBZ), from day 7 to 27, the anti-inflammatory effect being greater (40.69 and 39.72%) in on days 13 and 19. At a higher dose (300 mg/kg) it only showed an anti- inflammatory effect between days 17 and 19 with 35.06 and 34.33% inhibition. Animals treated with CHS (150 and 300 mg/kg) showed body weight gain from day 19 to day 27, whereas animals treated with FBZ lost weight from day 7 to 27, as did those treated with AFC. The CHS extract at 150 and 300 mg/kg reduced the size of the ganglia compared to the AFC group, with a similar effect to that of the FBZ. In addition, the weight of liver, kidneys, and heart was lower in the FBZ and extract groups at both doses compared to the AFC group. The LD50 of CHS, MeOH, Hex, CH2Cl2 was > 2 g/kg, i.g. in male Balb/C mice. C. serrata contains compounds of a different chemical nature that are responsible for its biological effect.