Polar fraction from Parkinsonia aculeata aerial parts extract improves imbalanced metabolic profile and reduces proinflammatory interleukin levels in white adipose tissue in obese rats induced by western diet.

ETHNOPHARMACOLOGICAL RELEVANCE: Parkinsonia aculeata L. (Cesalpineaceae) is a medium tree found in the Xingó region (semi-arid area) in Northeast of Brazil, recognised by local population as an antidiabetic agent. According information from local community, the commonly traditional preparation is prepared as an infusion of the aerial part of the plant and consumed over the day to manage diabetes-related complications. Previous studies have described Parkinsonia aculeate as a product with both hypoglycemic and hypotriglyceridemic effects. AIM OF THE STUDY: The objective of this study was to evaluate the effects of polar fraction obtained from the hydroethanolic extract of Parkinsonia aculeata (PfrHEPA) on the lipid profile of animals that consumed a westernized diet. MATERIALS AND METHODS: Thirty-six Wistar rats (45-55 g) were fed either with standard control(C) or westernized diet(W) for 120 days. The food intake, body weight evolution and body size were also analyzed. From 120 to 150 days, they were orally treated according to their group with vehicle (distillated water, 10 mL/kg), PfrHEPA at three doses (35, 70 and 140 mg/kg/day) or Gemfibrozil (140 mg/kg/day) for 30 days. RESULTS: The animals fed with westernized diet showed dyslipidemia when compared to animals receiving a standard diet. Treatment with PfrHEPA (140 mg/kg), even with the continued consumption of westernized diet by animals (from 120 to 150 days) promoted a significant reduction in total cholesterol, LDL and triglyceride levels, in relation to untreated W group. PfrHEPA 140 mg/kg reduced the key serum lipids and glycaemia as well as inflammatory cytokines known as important risk factors of cardiovascular diseases. CONCLUSIONS: The observed evidence may contribute to the control of metabolic parameters as dyslipidemia corroborating the ethnopharmacological information concerning the antihyperlipidemic and hypoglycemic activities of P. aculeata.

Poly-ε-Caprolactone Microsphere Polymers Containing Usnic Acid: Acute Toxicity and Anti-Inflammatory Activity.

Usnic acid (UA) has been studied by its pharmacological properties; however, it presents moderate toxicity, low solubility, and absorption by biological membranes. The aim of this study was to develop poly-ε-caprolactone microsphere polymers containing UA (UA-micro) and evaluate their acute toxicity and anti-inflammatory activity. The microspheres were prepared by multiple emulsion technique (water/oil/water) and characterized by the encapsulation efficiency, particle size, polydispersity index, and zeta potential. The acute toxicity of UA and UA-micro (25-50 mg/kg; p.o.) was evaluated in mice. The anti-inflammatory activity of UA and UA-micro was evaluated by subcutaneous air pouch and carrageenan-induced paw edema in rat, with measurement of inflammatory cytokines and MPO levels. The UA presented encapsulation efficiency of 97.72%, particle size of 13.54 micrometers, polydispersity index of 2.36, and zeta potential of 44.5 ± 2.95 mV. The UA-micro presented lower acute toxicity (LD50 value up to 2000 mg/kg; p.o.) when compared to UA. UA-micro and UA (25 mg/kg) significantly reduced paw volume and decreased MPO levels, whereas only UA-micro (50 mg/kg) reduced significantly IL-1ß, TNF-α, and NO levels in inflammatory exudate. These results suggest that controlled release systems, as microspheres, can be a promising alternative to reduce the toxicity of UA, making it a viable compound for inflammation therapy.