What do we have that is new in antifungal peptides? A patent review.

Drugs used to fight fungal infections may cause toxic or adverse drug interactions. For this reason, there is an increase in the development of natural, semisynthetic and synthetic antifungal peptides. This study aimed to perform a patent review to identify the advances in peptides to treat fungal infections. In a preliminary assessment, 597 patents were identified from the database. Then, duplicated patents (62) and those with titles in disagreement with the scope of this review (196) were excluded. Then, six patents were not in English or Spanish. Following the screening, 288 patents were outside the focus of this review, according to their abstract and description. The final selection covered 45 patents.

Currently, medications used to treat fungal infections may interact negatively with other drugs or be hazardous to the host. Scientists have been looking for novel, safe and efficient antifungal drugs since the enhancement of fungal resistance. Antimicrobial peptides, as opposed to traditional antibiotics, offer a variety of antibacterial activity against bacteria, fungi, parasites, viruses and cancer cells. The production of isolated natural, semisynthetic and synthetic antifungal peptides has increased. As a result, patents are a reliable and up-to-date source of innovation. As a result, their content analysis provides crucial information for identifying trends in new medications and targeted treatment plans.

In vitro and in vivo evaluation of the delivery of topical formulations containing glycoalkaloids of Solanum lycocarpum fruits.

The glycoalkaloids solasonine (SN) and solamargine (SM) have been studied for their antiparasitic, antifungal, and anticancer properties, especially in vitro and in vivo against non-melanoma skin cancer. Thus, the alkaloidic extract of Solanum lycocarpum, which contains approximately 45% each of SN and SM, was used to define the best experimental conditions for in vitro and in vivo assays. The in vitro assays were performed with the Franz cell diffusion porcine skin model to evaluate the effects of different pHs and the presence of monoolein, ethoxydiglycol or ethanol penetration enhancers on the skin penetration and retention of SN and SM after 3, 6, 9 and 12h of exposure. The in vivo assay was performed on hairless mice with the formulation selected in the in vitro assays. The results showed that pH 6.5 was optimal for SM penetration. The formulation containing 5% alkaloidic extract, 5% propylene glycol, 5% monoolein and a hydroxyethyl cellulose gel base (Natrosol) (pH 6.5) was optimal for the delivery of SN and SM into the skin, and this formulation is potentially useful for the topical therapy of several skin disorders.

Hypoglycemic effects of Cecropia pachystachya in normal and alloxan-induced diabetic rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Leaves of Cecropia pachystachya are described in the folk medicine as possessing antitusive, expectorant, antiasthmatic and hypoglycemic effects. AIM OF THE STUDY: To investigate the hypoglycemic and antioxidant effects of methanolic extract from the leaves of Cecropia pachystachya. The total amount of phenolic and flavonoids compounds was determined and the qualitative composition of the extract was analyzed. MATERIALS AND METHODS: The hypoglycemic effect of the extract was tested in normal, glucose loading and alloxan-induced diabetic rats. The antioxidant activity was assessed by DPPH free radical scavenging and reduction power assays. The total amount of phenolic and flavonoids compounds was determined by Folin-Denis and AlCl(3) reagent method, respectively. The qualitative composition of the extract was analyzed using a HPLC-DAD system. RESULTS: The glucose tolerance test showed that in diabetic rats, the extract caused a significant hypoglycemic effect with a blood glucose reduction of 68% after 12h. The administration of the extract in alloxan-induced diabetic rats also produced a significant reduction in the blood glucose levels at all points being more pronounced at 90min (reduction of 60%). After 120min, no significant difference was observed between the blood levels of the rats treated with the extract and those treated with the standard drugs (metformin and glibenclamide). The extract also presented relevant antioxidant activity with IC50=3.1microg/ml (DPPH assay) and EC50=10.8microg/ml (reduction power). Results were compared with the reference antioxidants quercetin, rutin, and ascorbic acid. The content of flavonoids was 83mg/g plant and that of phenolics was 326mg/g plant. Chlorogenic acid and the C-glycosylated flavones, orientin and isoorientin, were identified in the extract. CONCLUSIONS: In conclusion, the findings showed that the folk medicinal plant Cecropia pachystachya possesses hypoglycemic and antioxidant effects which confirmed the traditional use of the plant in the treatment of diabetes. Chlorogenic acid and the C-glycosylated flavonoids may explain these activities.