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Antioxidant and cytotoxic activity of polyphenolic compounds isolated from the leaves of Leucenia leucocephala.Haggag EG, Kamal AM, Abdelhady MI, El-Sayed MM, El-Wakil EA, Abd-El-Hamed SS Department of Pharmacognosy, Faculty of Pharmacy, Helwan University, Cairo, Egypt. Context: Cancer is a serious clinical problem to the health care system. Anticancer drugs have been extracted from plants containing phenolic compounds. Leucenia species (Fabaceae) contain a variety of bioactive components of numerous biological and pharmacological properties. Objective: This study explored the constitutive polyphenols of Leucenia leucocephala Lam. growing in Egypt and evaluated the antioxidant and cytotoxic activity. Materials and methods: Chemical structures of the isolated compounds from the leaves of L. leucocephala were established by spectral techniques (UV, (1)H, and (13)C NMR, MS). Results: Chromatographic separation of 80% MeOH extract of the leaves of L. leucocephala have resulted in a novel flavonoid-galloyl glycoside [myricetin 3-O-(2',3'4'-tri-O-galloyl)-α-l-rhamnopyranoside] with three known polyphenolic compounds isolated for the first time from this species (apigenin 7-O-β-d-glucuronopyranoside methyl ester, luteolin 7-O-β-d-glucuronopyranoside methyl ester, and 1,3,6-tri-O-galloyl-β-d-glucopyranose) and seven known previously isolated compounds. Also, 80% methanol extract exhibited high antioxidant activity (SC(50) = 3.94 µg/ml), which is correlated with its phenolic content. The extract also showed cytotoxic activity against Hep G2 (IC(50) value 1.41 µg/ml) confirming its anticancer activity against hepatocellular carcinoma. Among the tested compounds (4-8) for antioxidant property, compound 7 was the most active compound (SC(50) = 2.49 µg/ml). Also compounds 7 and 8 exhibited high cytotoxic activity (IC(50) = 2.41 and 2.81 µg/ml, respectively). Discussion and conclusion: These findings demonstrate that the leaves of L. leucocephala contain a considerable amount of polyphenolic compounds with high antioxidant properties, thus it has great potential as a source for natural health products. Published 21 October 2011 in Pharm Biol, 49(11): 1103-13. Articles on Pharmacy published 21 October 2011: Determination of tadalafil and N-desmethylsibutramine in health and dietary supplements using ultra-performance liquid chromatography (UPLC) coupled with quadrupole-time-of-flight mass spectrometry (Q-TOF MS). Food Addit Contam Part A Chem Anal Control Expo Risk Assess, 28(11): 1475-82. The adulteration of dietary supplements with drugs is potentially dangerous for human health. In this study, a method was used to test simultaneously for the presence of three synthetic PDE-5 inhibitors (sildenafil, vardenafil and tadalafil), and sibutramine and its two major metabolites (N-desmethylsibutramine and N-didesmethylsibutramine) using ultra-performance liquid chromatography (UPLC) coupled with quadrupole-time-of-flight mass spectrometry (Q-TOF MS) in dietary supplements. This ... [Abstract] [Full-text] A 5-HT(2C) receptor antagonist potentiates a low dose amphetamine-induced conditioned place preference. Neurosci Lett. This study was designed to determine whether a 5-HT(2C) receptor antagonist could induce a conditioned place preference indicative of reward and/or abuse potential. Here, we present the first evidence that a selective 5-HT(2C) receptor antagonist, 6-chloro-5-ethoxy-N-(pyridin-2-yl)indoline-1-carboxamide hydrochloride (CEPC), can potentiate a low dose (0.5mg/kg) amphetamine-induced positive conditioned place preference (CPP). CEPC did not produce any CPP given alone at doses of either 2.0 or ... [Abstract] [Full-text] M3-receptor activation counteracts opioid-mediated apneusis, but the apneusis per se is not necessarily related to an impaired M3 mechanism in rats. Life Sci, 89(19): 685-90. A protocol for the classification of powder compression characteristics. Eur J Pharm Biopharm. In this paper, a structured protocol for powder compression analysis as a test to assess the mechanical properties of particles in a formulation development programme is presented. First, the sequence of classification steps of the protocol is described, and secondly, the protocol is illustrated using compression data of six powders of two model substances, sodium chloride and mannitol. From powder compression data, a set of compression variables are derived, and by using critical values of ... [Abstract] [Full-text] Abstract Objective: To examine treatment patterns and costs among patients with fibromyalgia prescribed pregabalin or tricyclic antidepressants (TCAs). Methods: Using the LifeLink™ Health Plan Claims Database, patients with fibromyalgia (International Classification of Diseases, Ninth Revision, Clinical Modification code 729.1X) newly prescribed (index date) TCAs (n = 898) were identified and propensity score-matched (PSM) with patients newly prescribed pregabalin ... [Abstract] [Full-text] Rational design of 2-pyrrolinones as inhibitors of HIV-1 integrase. Bioorg Med Chem Lett, 21(22): 6724-7. HIV-1 integrase is an essential enzyme for viral replication and a validated target for the development of drugs against AIDS. With an aim to discover new potent inhibitors of HIV-1 integrase, we developed a pharmacophore model based on reported inhibitors embodying structural diversity. Eight compounds of 2-pyrrolinones fitting all the features of the pharmacophore query were found through the screening of an in-house database. These candidates were successfully synthesized, and three of them ... [Abstract] [Full-text] Fingerprinting of sildenafil citrate and tadalafil tablets in pharmaceutical formulations via X-ray fluorescence (XRF) spectrometry. J Pharm Biomed Anal. The production of counterfeited drugs is a criminal problem that carries serious risks to public health in the worldwide. In Brazil, Viagra(®) and Cialis(®) are the most counterfeit medicines, being used to inhibit the phosphodiesterase type 5 (PDE-5), treating thus, problems related to erectile dysfunction. X-ray fluorescence (XRF) is a suitable technique to control the quality of new pharmaceutical formulations and distinguish between authentic and counterfeit tablets. XRF has advantageous ... [Abstract] [Full-text] Bone targeting for the treatment of osteoporosis. J Control Release. Osteoporosis represents a major public health burden especially considering the aging populations worldwide. Drug targeting will be important to better meet these challenges and direct the full therapeutic potential of therapeutics to their intended site of action. This review has been organized in modules, such that scientists working in the field can easily gain specific insight in the field of bone targeting for the drug class they are interested in. We review currently approved and emerging ... [Abstract] [Full-text] © 2008-2013 Pharmacy Research Today. All Rights Reserved. |
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