Normal Vascular Reactivity Is Restored by Apigenin in Diabetic Rats

Abstract

Objective: Diabetes is a disease whose complications have serious implications for the health of sufferers; one of the most serious such complications is the deterioration of vascular reactivity. Apigenin is a natural flavonoid with PKC inhibiting and antioxidant properties. In this study, the impact of apigenin on vascular reactivity deterioration was investigated.Methods: Insulin resistance (IR) and insulin deficiency (ID) were induced by fructose and streptozotocin respectively. The isolated aortae vasoconstriction response to phenylephrine (PE) and potassium chloride (KCl) in addition to the vasodilation response to acetylcholine (ACh) and sodium nitroprusside (SNP) were tested.Results: IR and ID were associated with significantly exaggerated vasoconstriction to KCl and PE while significantly impaired vasodilation to ACh. Response to SNP was not significantly affected by both IR and ID. In vitro incubation with apigenin (7 7µM) for 20 min restored normal responses to PE, KCl and ACh in aortae isolated from insulin-resistant or insulin-deficient rats. Incubation for one hour with the PKC stimulant, phorbol 12-myristate 13-acetate (PMA, 800 nM) resulted in aortic impairment similar to that seen in aortae isolated from IR and ID animals. Incubation with both apigenin prevented PMA-induced exaggerated vasoconstriction response to both PE and KCl.Conclusion: Apigenin alleviates vascular exaggerated vasoconstriction and impaired dilation associated with diabetes or PKC activated.

Structure-Based Drug Design Method: Molecular Docking Study and Pharmacophore Modelling of Apigenin as an Antimalarial

“…Ligandscout 4.4 was used to load each complex into the structure-based perspective. The development of the pharmacophore and its 2D depiction were then used to interpret and evaluate the results after the interaction had been studied by selecting the yellow box [6,[14][15][16].…”

“…A natural substance called apigenin (API), which belongs to the flavone subclass of flavonoids, is found in many plants, including celery, parsley, grapes, chamomile, onions, maize, tea, sugar, and sprouts. Numerous pharmacological effects of API include anti-inflammatory, antidiabetes, vasodilators, anticoagulant, antidiabetic, anti-cancer, and antimalarial properties [4][5][6].…”