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ETHNOPHARMACOLOGICAL IMPORTANCE: Achillea millefolium L. (Asteraceae) is a perennial herb used in Mexican folk medicine for treatment of several pathologies, including inflammatory and spasmodic gastrointestinal disorders, hepatobiliary complaints, overactive cardiovascular, respiratory ailments and diabetes. AIM OF THE STUDY: To evaluate the potential antidiabetic effect in vivo and to establish the potential mode of action through in vitro approaches of Achillea millefolium. MATERIALS AND METHODS: The antidiabetic effect of hydroalcoholic extract of Achillea millefolium (HAEAm) was evaluated on the oral glucose tolerance tests, in normoglycemic and experimental Type 2 diabetic mice models. In addition, we evaluated the possible mode of action in in vitro assays to determine α-glucosidases inhibition, the insulin secretion and calcium mobilization in RINm5F cells and PPARγ and GLUT4 expression in 3T3-L1 cells. RESULTS: HAEAm showed significant glucose diminution on oral glucose tolerance test and in acute experimental Type 2 diabetic assay with respect to the control (p < 0.05). In addition, HAEAm promoted the α-glucosidases inhibition by 55% at 1mg/ml respect to control. On the other hand, HAEAm increased the PPARγ (five-times) and GLUT4 (two-fold) relative expression than control (p < 0.05). Finally, HAEAm significantly increased the insulin secretion and [Ca2+]i compared with control. CONCLUSION: The HAEAm possesses in vivo antidiabetic effect, having such effect through multitarget modes of action that involve antihyperglycemic (α-glucosidases inhibition), hypoglycemic (insulin secretion) and potential insulin sensitizer (PPARγ/GLUT4 overexpression) actions.

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RESUMO

Euphorbia dioeca Kunth belongs to the Wanderer’s herb complex that is traditionally used for skin diseases and recently as antidiabetic. The methanol and aqueous extracts were evaluated for their in vitro alpha-glucosidase inhibitory activity and an oral starch tolerance test. These extracts showed an IC50 of 0.55 and 0.85 mg/mL, respectively. In diabetic Long Evans rats, the methanol and aqueous extracts reduced significantly the postprandial hyperglycemia peak in 15.2 percent and 12.8 percent, respectively. The alpha-glucosidase inhibitory activity is related with the presence of glycosides, phenolic compounds and flavonoids. Additionally, the safety parameters of both extracts were assessed by means of an acute toxicity test, being classified as innocuous. The traditional use of E. dioeca to control type 2 diabetes was confirmed, being an important source of alfa-glucosidase inhibitors.

Euphorbia dioeca Kunth, pertenece al complejo de plantas medicinales denominado Hierba de la Golondrina; el cual se utiliza para diversos padecimientos, destacando su uso como antidiabético. En dicho marco, se evaluó tanto la actividad inhibitoria de alfa-glucosidasa in vitro, como su desempeño en una prueba de tolerancia a una carga de almidón postprandial. Los extractos inhibieron la actividad de la alfa-glucosidasa con una CI50 de 0.55 y 0.85 mg/mL, respectivamente. Los extractos metanólico y acuoso disminuyeron significativamente el pico hiperglucémico postprandial en un 15.2 por ciento y un 12.8 por ciento, respectivamente, cuando se evaluó en ratas diabéticas. La actividad inhibitoria de alfa-glucosidasa, reflejada en ambas pruebas, está relacionada con la presencia de glicósidos, compuestos fenólicos y flavonoides. De manera adicional, ambos extractos fueron evaluados en una prueba de toxicidad aguda, siendo clasificados como inocuos. Se corroboró el uso tradicional de E. dioeca para el control de la diabetes tipo 2, siendo una importante fuente de compuestos inhibidores de alfa-glucosidasa.

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The EtOAc extract of the stem bark of Hintonia latiflora showed the suppression of total parasitemia and the chemosuppression of schizont numbers, when tested in vivo against Plasmodium berghei infection in mice. Bioassay-directed fractionation of the EtOAc extract, using the in vitro 16 h and the in vivo 4-day suppression tests on P. berghei schizont numbers, led to the isolation of the new compound 5-O-beta-D-glucopyranosyl-7,4'-dimethoxy-3'-hydroxy-4-phenylcoumarin (1), along with the known 5-O-beta-D-glucopyranosyl-7-methoxy-3',4'-dihydroxy-4-phenylcoumarin (2). The structure of compound 1 was established on the basis of spectroscopic data interpretation. Compounds 1 and 2 suppressed the development of P. berghei schizonts in vitro with IC50 values of 24.7 and 25.9 microM, respectively. Compound 2 suppressed the development of schizonts at the dose of 40 mg/kg by 70.8% in the in vivo assay.

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