Acta Pharmaceutica 

About: Acta Pharmaceutica is an academic journal published by De Gruyter Open. The journal publishes majorly in the area(s): Medicine & Drug delivery. It has an ISSN identifier of 1330-0075. It is also open access. Over the lifetime, 1096 publications have been published receiving 21626 citations.

Biological activities of isatin and its derivatives.

Abstract: Isatin is an endogenous compound identified in humans that possesses a wide range of biological activities. Isatin has anxiogenic, sedative, anticonvulsant activities and acts as a potent antagonist on atrial natriuretic peptide receptors in vitro. A series of p-substituted isatin semicarbazones have shown anticonvulsant activity in MES, scPTZ and scSTY tests. Various isatin-N-Mannich bases of isatin-3-thiosemicarbazones have shown antiviral and tuberculostatic activity. Methisazone is an effective compound against variola and vaccinia viruses. The N-dimethyl and morpholino derivative of 5-methyl isatin and trimethoprim exhibited an EC50 of more than 4.3 and 17.7 mg mL(-1), respectively. Isatin (3-o-nitrophenyl) hydrazone has shown activity against Walker carcinoma-256. Various substituted indolinones showed antitubercular activity against M. tuberculosis H37Rv with MIC ranging from 10-20 microg mL(-1). Isatin derivatives of Mannich bases had fibrinolytic, muscle relaxant, antiallergic, immunosuppressant, and antithrombotic activity. Isatin showed cardioinhibitory effect on frog heart, and hypotensive, respiratory depression and antidiuretic effects.

Anticonvulsant activity of Schiff bases of isatin derivatives.

Abstract: Schiff bases of N-methyl and N-acetyl isatin derivatives with different aryl amines have been synthesized and screened for anticonvulsant activities against maximal electroshock (MES) and subcutaneous metrazole (ScMet). N-methyl-5-bromo-3-(p-chlorophenylimino) isatin (2) exhibited anticonvulsant activity in MES and ScMet with LD50 > 600 mg kg(-1), showing better activity than the standard drugs phenytoin, carbamazepine and valproic acid. Thus, compound 2 may be chosen as a prototype for development of new anticonvulsants.

Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib

Abstract: The aim of the present study was to investigate the potential of nanoemulsion formulations for transdermal delivery of celecoxib (CXB). The in vitro skin permeation profile of optimized formulations was compared with CXB gel and nanoemulsion gel. Significant increase in the steady state flux (Jss), permeability coefficient (Kp) and enhancement ratio (Er) was observed in nanoemulsion formulations T1 and T2 (p < 0.05). The highest value of these permeability parameters was obtained in formulation T2, which consisted of 2% (m/m) of CXB, 10% (m/m) of oil phase (Sefsol 218 and Triacetin), 50% (m/m) of surfactant mixture (Tween-80 and Transcutol-P) and 40% (m/m) water. The anti-inflammatory effects of formulation T2 showed a significant increase (p < 0.05) in inhibition after 24 h compared to CXB gel and nanoemulsion gel on carrageenan-induced paw edema in rats. These results suggested that nanoemulsions are potential vehicles for improved transdermal delivery of CXB.

Antioxidant and free radical scavenging potential of Citrullus colocynthis (L.) Schrad. methanolic fruit extract

Abstract: Citrullus colocynthis (L.) Schrad. (Cucurbitaceae) is a medicinal plant traditionally used as an abortifacient and to treat constipation, oedema, bacterial infections, cancer and diabetes. Preliminary phytochemical screening of the plant showed the presence of large amounts of phenolics and flavonoids. Subsequent quantification showed the presence of 0.74% (m/m) phenolics (calculated as gallic acid) and 0.13% (m/m) flavonoids calculated as catechin equivalents per 100 g of fresh mass. The presence of phenolic compounds prompted us to evaluate its antioxidant activity. In the present study, methanolic fruit extract of C. colocynthis was screened to evaluate its free radical scavenging effect. The highest antioxidant and free radical scavenging ability of the fruit extract was observed at a concentration of 2500 microg mL(-1).

Quantitative analysis of the flavonoids in raw propolis from northern Croatia

Abstract: Spectrometric analyses of flavonoids in twenty propolis samples collected from ten different geographic localities in northern Croatia using two complementary methods, are reported. Flavones and flavonols were determined using aluminum chloride and expressed as quercetine equivalent while flavanones were determined using 2,4-dinitrophenylhydrazine and expressed as naringenin. Contents of flavones and flavonols were similar for most samples and ranged from 2 to 2.3%, except for one sample with a concentration of 1.3% and one sample in which it was not possible to detect flavones and flavonols. The content of flavanones in propolis samples is very variable. 55% of samples contain flavanons between 15 and 24% and 45% of samples between 4 and 14%. Total levels of flavonoids in raw propolis samples ranged between 5 and 26%; for the majority of samples (75%), the total level of flavonoids ranged between 15 and 25.9%. The high variability of flavanone concentration will affect biological activity of propolis preparations.