International Journal of Pharmaceutical Sciences and Drug Research

68-74

Authors: Syed Waseem Bihaqi1*, Suhaib Ibrahim Alkhamaiseh2¬, Manisha Tiwari3

The herbal medicinal plant, Convolvulus pluricaulis: a rasayana drug has been primarily advocated for use in mental stimulation and rejuvenation therapy. In ancient systems of Indian medicine, Ayurveda, the plant is also known by the name Shankhpushpi and has been shown to act as a prominent memory improving drug, a psychostimulant and tranquiliser. The plant displays its biological activity due to the presence of several alkaloids, flavanoids and coumarins as active chemicals. Previous reports by us and others have demonstrated beneficial effect of extracts of this plant in an in-vitro and in-vivo models of Alzheimer’s disease (AD). Justification of its potential for an ancient brain tonic has been provided recently by clinical studies on polyherbal formulation of this plant. This review attempts to compile information on Convolvulus Pluricaulis in order to establish this herbal drug as a potent natural therapeutic agent to combat AD related symptoms.

83-86

Authors: Md. Anisur Rahman*, Mohammed Faisal Bin Karim, Tirtha Nandi, Kazi Imran Adib, Roksana Parvin, Md. Shahriar Mahmud

This research work was carried out to determine whether the film coating is effective to prevent the photolytic degradation of Metoprolol tartrate which is known to have photosensitivity. For this purpose, two randomly selected brands of two different pharmaceutical companies were chosen i.e. Brand A and Brand B. These two brands were exposed to different lighting conditions (normal light, direct sunlight as well as two incandescent lights i.e. 25 watt bulb, 40 watt bulb). Potency tests were performed using UV spectroscopy which showed gradual decline in potency of the tablets under aforesaid lighting conditions and the potency degradations were found 11.48%, 12.92%, 22.62%, 16.87% for Brand A and 14.74%, 14.24%, 10.88%, 18.10% for Brand B under 25 watt bulb, 40 watt bulb, direct sunlight and normal room light respectively. So this study reveals that the both brands containing metoprolol tartrate showed significant light sensitivity even though they are coated and protective opaque packaging is highly recommended for their protection.

91-97

Authors: Rasikkumar M. Ravani*, Laxman J. Patel

Synthesis of novel quinazoline derivatives was performed from reaction of N-benzoyl substituted piperazine-1-carbothioamide with 4-(2-chlormethyl) quinazoline-4-yloxy phenyl benzamide derivatives and screened for their in vitro cytotoxic activity by MTT assay. The cell lines used were MCF 7 (Breast cancer cell), HCT 15 (Colon cancer cell line), and VERO (Normal epidermal kidney cell). Result of screening on cell line showed moderate to good cytotoxic activity for all the compounds. Compound GNU 02 (IC50 = 7.94 µM, MCF), GNU 12 (IC50 = 8.43 µM, HCT) and GNU 25 (IC50 = 9.41 µM, HCT) was found to be most active compared to standard gefitinib (IC50 = 1.51 µM HCT, IC50 =22.37 µM MCF). Structure activity relationship of synthesized analogs suggested that the attachment of electron withdrawing groups like Nitro, Chloro gave better cytotoxic activity then unsubstituted phenyl and electron donating groups. Activity by substituted piperazine at 2nd position of thiazole linked with quinazoline scaffold gave better activity in the order of H > CH3 > C6H5. Our findings may impart new direction to medicinal chemists and biochemists for further investigations of quinazoline-thiazole containing cytotoxic agents.

103-110

Authors: M. A. Reynoso1, A. Daud1, M. M. Belizán2, A. Sánchez Riera1, N. R. Vera2*

Ziziphus mistol Griseb. (Rhamnaceae), popularly known as “mistol,” is widely distributed throughout Perú, Bolivia, Paraguay and Argentina. Its fruit is consumed in different forms in several argentinean communities and used against biliary colic, dysentery, cold stomach and diseases of the respiratory system characterized by pain and inflammation. The present study was carried out to investigate the medicinal properties and safety of Ziziphus mistol (mistol) fruits ethanol and aqueous extracts and arrope. Antinociceptive activity was assessed using the formalin, acetic acid-induced writhing and tail-flick tests in rats. Anti-inflammatory effects were determined through carrageenan induced edema test and cotton pellet-induced granuloma formation, in rats. The safety was evaluated with test of acute toxicity (48 hours) and sub-chronic toxicity (91 days). All extracts (1,000 mg/kg b.w.) showed significant inhibition (P <0.05) in the three model of pain experimentally induced in comparison to control. In a combination test using naloxone, diminished analgesic activity of aqueous extract and arrope were observed, indicating that their antinociceptive activity is connected with the opioid receptors. At dose 1000 mg/kg bw, the aqueous extract and arrope showed higher anti-inflammatory activity than the ethanol extract, in carrageenan and cotton pellet granuloma model used. In the acute toxicity study, a single dose of 4000 and 8000 mg/kg b.w., produced no mortality and no clinical signs of disease were observed after 48 hours. In the sub-chronic toxicity study the extracts no caused significant visible signs of toxicity, nor mortality for 91 consecutive days of treatment. Extracts and arrope of Z. mistol fruits could be good source of antinociceptive and anti-inflammatory agents because of its good activity and safety.

117-120

Authors: Thomas SK, George RE, Kunjumon M, Thankamani VI*

Alstonia venenata R. Br. belonging to the family Apocynaceae is a tall evergreen shrub distributed throughout Peninsular India. Stem-bark, root-bark, fruits and leaves are used by many tribal communities and also in Ayurveda. The study investigates the phytochemical composition of hexane, butanol, methanol and water extracts of Alstonia venenata fruits and flowers as well as the TLC profile of hexane extracts of fruits and flowers. Quantitative data of the wet and dry weight, yields from different solvent fractions and percentage yields were noted. The phytochemical analysis revealed the presence of secondary metabolites such as alkaloids, steroids, terpenoids, saponins, flavonoids, tannins and phenolic compounds from the various extracts. Alkaloids were present in all the fractions tested. Methanol extracts of fruits and flowers showed the presence of major phytoconstituents. TLC profile of hexane extracts of fruits and flowers were developed using anisaldehyde sulphuric acid/ceric sulphate (steroids/terpenoids) and Dragendorff’s spray reagents (alkaloids). Petroleum ether: Chloroform: Methanol (5: 4.5: 0.5) showed good resolution for the hexane extracts of fruit and flower when treated with Dragendorff’s spray reagent. Petroleum ether: Chloroform (1:1) was best for the hexane exacts of flowers and fruits when sprayed with ceric sulphate spray reagent.