International Journal of Pharmaceutical Sciences and Drug Research

100-104

Authors: Babu A, Sheik Noor Mohamed M, Jaikumar K, Anand D, Saravanan P*

Traditional healers possess a rich knowledge on the use of medicinal plants for the treatment of various diseases. Enicostemma axillare (Lam). Raynal is one plant, used by healer to treat gastric cancer or ulceration. We assessed the phytochemical components of leaf extract for its antibacterial activity, to add value and provide an evidence-base for their traditional use. The antibacterial potential of the leaf extract was tested against Helicobacter pylori using agar well diffusion method. The minimum inhibitory concentration (MIC) of ethanol extract exhibited the (MIC) against H. pylori ranged from 200µg/ml - 250µg/ml followed by chloroform extract. Gas chromatography and mass spectrum (GC-MS) analysis confirms the occurrence of different components in the ethanol and chloroform leaf extract of the studied species.

113-117

Authors: Anantha Padmanabhan S, John Wyson W, Marimuthu S, Saravanan P, Anand D*

Microbial community has been a major part in the drug industry. They are known for their effectiveness and do not cause any undesirable effects. Exploitation of bacteria could be fruitful for mankind. Bacteria play a major role in producing useful bioactive compounds. HSV-1 infection causes 80% of oral lesions. A majority of the population is infected by at least one herpes subtype of HSV-1 before adulthood. The infection in some cases does not produce any symptoms. Drugs for HSV-1 are becoming suppressive. In the present study, isolation of endophytic bacteria was carried out from medicinal plant. A grown bacterium was identified and confirmed using molecular 16S rRNA sequencing followed by extraction of bioactive compounds using solvents. Twelve bioactive compounds were then investigated for in vitro cytotoxicity assay and in vitro antiviral assay. Chloroform extract was found to be effective in inhibiting the virus.

126-133

Authors: S. G. Dhage, G. K. Lohiya, Y. M. Charde*, J. G. Avari

Certain problems regarding the drugs like high first pass metabolism, also the bioavailability of the certain drugs varies due to instability in acidic environment of stomach. Hence, to resolve such problems the drug should be incorporated in the microspheres for sustained release using a suitable polymer. Natural polymer like chitosan gained great interest in pharmaceutical sector because of its advantages like biodegradability, biocompatibility, non-toxicity, non-immunogenicity and low cost. In the present study, formulation and evaluation of polymeric microspheres of Atorvastatin Calcium was carried out and the release profile of such drug using the alginate and chitosan was studied. Microspheres were prepared for sustained release of drug using chitosan and alginate polymers by ionotropic gelation method. Microspheres were spherical in shape, having good flow properties and further its encapsulation efficiency, swelling index, micromeritic study, in- vitro drug release study and stability studies were performed in order to characterize microspheres. Three different concentrations of sodium alginate (1%, 2% and 3%) were used. The higher encapsulation efficiency was observed as the concentration of alginate increased. This is due to the greater availability of active calcium binding sites in the polymeric chains and consequently the greater degree of cross linking. The highest encapsulation efficiency (88.36) was achieved with 2% w/v sodium alginate in combination with 3% chitosan (F6). Among the prepared formulations with respect to the entrapment efficiency, swelling studies and in vitro drug release, the alginate-chitosan microspheres prepared by ionotropic gelation using calcium chloride found to be better than ionically cross linked alginate spheres alone. Therefore, dual cross-linked, microspheres are promising carrier for sustained release of drug.

139-144

Authors: Debarshi Kar Mahapatra1*, Devashish Das2, Ruchi Shivhare3

Cancer is the second leading causes of mortality across the planet which has had affected millions. In spite of massive efforts in producing new molecules and chemotherapeutic approaches for managing cancer, it continued to be the global threat. Small hybrid molecules have gained popularity in chemotherapy due to their potential and smart characteristics in modulating biological targets. The present research attempts in developing few novel hybridized derivatives of murrayanine (an active carbazole derivative) by the semi-synthetic approach to form substituted thiazole linked murrayanine-Schiff’s base derivatives. The protocol involved murrayanine 1 as the template material for constructing a hybridized Schiff’s base intermediate 3, which further by Hantzch’s cyclization was subsequently converted to various hybridized thiazoles analogs 5a-5f. The purity of the synthesized compounds was ascertained by sophisticated analytical techniques. The anti-cancer potential was screened against breast cancer cell lines; MCF-7 and MDA-MB-231 by Sulforhodamine B (SRB) assay. The compound 5b displayed most potent anti-proliferative activity with IC50 values of 23.41μM against MCF-7 cell line and 32.15μM against MDA-MB-231 cell line. It has been observed that analogs having electron withdrawing substituents exhibited pronounced anticancer activity. The docking study was performed by Autodock Vina where the results were found to be in full agreement with the cytotoxic study, depicting that the probable cytotoxic outcome by EGFR inhibitory mechanism. The study revealed the potential of novel hybridized derivatives as active anti-breast cancer candidates. The research will encourage (medicinal) chemists in rationally designing of semi-synthetic analogs of a heterocyclic prototype having pronounced anti-cancer activity.