Current Research in Pharmaceutical Sciences

80-86

Authors: Saadiya A El-Nahas, Hoda Mahrous, Yahya Naguib, Mohammed Fathy Salem and Yossereya M Hassan

L-carnitine is a cofactor in the transfer of long-chain fatty acid allowing the β-oxidation of fatty acid in the mitochondria. It is also a known antioxidant with protective effects against lipid peroxidation. This study aimed to investigate the effect of the biosyenthesized L-carnitine from mushroom Pleurotus ostreatus against paracetamol (AA) induced hepatotoxicity and nepherotoxicity where mitochondrial dysfunction and oxidative stress are thought to be involved in AA toxicity. Forty Swiss albino male adult mice were divided into five groups. Mice were dosed with single-AA injection (500 mg/kg via the intra peritoneal route) with or without L-carnitine (500 mg/kg for 10 days starting 10 days before and after AA injection via intra peritoneal route) AA increased serum AST, ALT, serum creatinine and BUN levels significantly. Administration of biosynthesized L-carnitine from Pleurotus ostreatus significantly reduced AA-induced elevations in AST, ALT, serum createnine and BUN levels. Also histopathological examination of liver and kidney showed great improvement of AA induced necrosis and hemorrhage. These results suggested that AA results in oxidative damage in the liver and kidney with an acute effect and L-carnitine from mushroom Pleurotus ostreatus pharmacologically active and has a prominent therapeutic and protective effect against acute AA toxicity and may be of therapeutic value in the treatment and prevention of AA-induced hepatotoxicity and nephrotoxiciy.

92-98

Authors: Anand Gupta, Yogendra Mavai, Suman Jain

edicinal plants have been used in various traditional systems, as they have potential against numerous diseases. Currently, more than 200 clinically useful prescription drugs are derived from plants. Most of these were developed because of their use in traditional medicine. In several ancient systems of medicine including Ayurveda, Siddha and Unani, Ipomoea aquatic, Cinnamomum zeylanicum and Piper longum, three medicinally important herbs from mainly Asian origin has vast number of therapeutic applications including antiasthematic activity but very little information is available about their safety profile. It is a common believe that herbal products are safe because of which nobody care for the evaluation of their final preparation. We strongly recommend performing safety studies for the herbal preparations because all the extracts used are chemical in nature and there is strong possibility that these chemicals may react with each other and form some toxic compound or interact with the biomolecules. Keeping these things in mind, the present study has been envisaged and it was observed that water and chloroform extracts of Ipomoea aquatic, Cinnamomum zeylanicum and Piper longum are safe, based on the acute toxicity studies, as no abnormal changes are observed in treated animals. The combinations of both the extracts in 1:1:1 ratio are also safe and can be encapsulated into hard gelatin capsule of 000 size for human use.

45-47

Authors: Piyush Gupta, Ashish Kumar Parashar and Rajesh Kumar Nema

Solanum xanthocarpum (Solanaceae) is distributed all over India and has been used by triable as well a local people widely. Locally it is known as “Kantakari”. In present investigation the aim is to focus on the anthelmintic activity of this valuable medicinal plant Solanum xanthocarpum. Helminthiasis is a worldwide and one of the common diseases of all ages. As per WHO more than two billion people harbor this infection. From the survey of WHO only few drugs are frequently used in the treatment of helminthes in human, due to the cost and the development of resistance against these drugs. In the present work the alcoholic and aqueous extracts of Solanum xanthocarpum were evaluated for its anthelmintic activity against adult earthworms (Phertima prosthuma). The activities of the extracts were compared with standard Albendazole. Both the extracts and standard were prepared in saline water. The alcoholic and aqueous extract showed significant anthelmintic activity and it was found that the aqueous extract activity is higher than alcoholic extract.

53-57

Authors: Sunil Sangare, Nidhi Jain, A K Pathak

The purpose of this project work to develop a antibacterial patch that may stick to the wounds, providing protection against bacterial infection without disturbing the healthy tissues present around the wound. As there is no external agent that can heal the wound, as body has its own wound healing mechanism, only thing that can be done is protecting the wounds against bacteria so healing can be fast. Here is film is prepared using neomycin antibacterial agent and using polymer gelatin that too has anti bacterial effect. The neomycin patch will be biocompatible material without given any side effect to the applied natural systems. The incorporation of PEG with gelatin has the aim of developing a material that would have good mechanical strength, be thermally stable on human body, and have good swelling property and effective water absorption capacity. The prepared will enhance both the rapidity of healing including reducing infection, pain, and scarring. An improved dressing also will reduce cost by improving the rate of wound healing and shorter the duration the treatment.

61-67

Authors: Pradeep K Sharma, Yogendra Mavai, Suman Jain

Medicinal plants have been used in various traditional systems, as they have potential against numerous diseases like cardiovascular disease. Currently, more than 200 clinically useful prescription drugs are derived from plants. Most of these were developed because of their use in traditional medicine. In several ancient systems of medicine including Ayurveda, Siddha and Unani, Achyranthus aspera & Murraya koenigii, two medicinally important herb from mainly Asian origin has vast number of therapeutic applications including hypolipidemic activity but very little information is available about their safety profile. It is a common believe that herbal products are safe because of which nobody care for the evaluation of their final preparation. We strongly recommend performing safety studies for the herbal preparations because all the extracts used are chemical in nature and there is strong possibility that these chemicals may react with each other and form some toxic compound or interact with the biomolecules. Keeping these things in mind, the present study has been envisaged and it was observed that water and chloroform extracts of Achyranthus aspera & Murraya koenigii are safe, based on the acute toxicity studies, as no abnormal changes are observed in treated animals. The combinations of both the extracts in 1:1 ratio are also safe and can be encapsulated into hard gelatin capsule of 000 size for human use.

7-9

Authors: B K Sarkar, K G Vasanthakumar, P Madhavikutty and V C Deep

Current scenario lead to change in life style which has resulted in the increased production of free radicals which raise the oxidative stress and also play an important role in the immune system dysfunction. Hence there is need of a safe and effective antioxidant. In this regard Varatika Bhasm was screened for the free radical scavenging activity. Various antioxidant assay methods were used for this purpose such as hydroxyl radicals, super oxide radical scavenging activity and nitric oxide radical inhibition. Ascorbic acid (AA) was used as the standard antioxidant for the free radical scavenging assays. The study was carried out for different concentrations of drug in suspension form. The result of antioxidant activities shows significant scavenging of hydroxyl and super oxide radical with the minimum IC50 values of 54.8±0.53 mcg/ml and 91.21±0.22 mcg/ml respectively. Result of study suggested that Varatika Bhasm have excellent antioxidant activity against the different in vitro antioxidant models.

15-27

Authors: Nitendra K Sahu, Kamlendra S Bhadoriya, Mukesh C Sharma and D V Kohli

The QSAR studies were performed on a series of thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline to find out the structural requirements of their antimalarial activities. The 2D-QSAR studies were performed using three methods: MLR, giving r2 = 0.7808, q2 = 0.6492 and pred_r2 = 0.9044; the PLS, with r2 = 0.7785, q2 = 0.6420 and pred_r2 = 0.7181; and PCR, giving r2 = 0.7393, q2 = 0.6222 and pred_r2 = 0.9135. The QSAR models showed that the LUMOEnergy, SdsCHE-index and Quadrupole1 played an important role in determining biological activities. The 3D-QSAR studies were performed using the stepwise variable selection k-nearest neighbor molecular field analysis (kNN-MFA) approach; q2 of 0.7107and pred_r2 of 0.8521 were obtained. The results of the present study may be useful for the designing of more potent analogues as antimalarial agents.

32-34

Authors: D Kumar, H V Hegde, P A Patil, R K Joshi, A K Sharma and S Roy

A formulation of Andrographis paniculata is widely used by traditional healers for the treatment of fever in rural northern Karnataka. The present study was undertaken to evaluate the safety and efficacy of the formulation milk induced pyrexia model. After 1 hr intraperitonial administration of milk, decoction was given in the oral dose of 0.7 ml/kg, which, were shown to be significant in reducing reduced the elevated body temperature of rabbit.

191-196

Authors: Gagandip Singh and Manish K Gupta

The contemporary therapeutic demand is to develop a new antimalarial agent with a novel mode of action. Recently, the Plasmodium protein farensyltransferase (Pf-PFT) has been suggested as a viable target to develop new and alternative antimalarial agent. The present work describes the homology modeling of Pf-PFT and docking study to provide a structural basis for the design of new Pf-PFT inhibitors and antimalarial agents. Homology model of Pf-PFT was developed using X-ray structure of Rat-PFT. The sequence alignment was done using ClustalW. The homology model of Pf-PFT was generated using Modeller 9v7. The outliers were identified using PROCHECK and were minimized by energy minimization. The docking study of two potent Pf-PFT inhibitors (BMS-214662 and SCH66336) were performed using GOLD5.0.1 software. The Pf-PFT is a heterodimeric protein which consist of α and β chains. The sequences of target and template were aligned using ClustalW and refined manually. Twenty five models of Pf-PFT were developed and the model with least objective function was selected for validation with PROCHECK and WHATIF. The docking of BMS-214662 and SCH66336 at substrate binding site of Pf-PFT identified important ligand-receptor interactions. Both inhibitors coordinated with zinc cofactor and adopt the conformations sufficient to inhibit substrate-Pf-PFT binding. A 3D-conformation of Pf-PFT was developed and validated by standard protocol. The docking study highlighted the crucial amino acid residues involved in drug-receptor interactions. The Pf-PFT model may be useful to design and develop new Pf-PFT inhibitors and anti-malarial agents.

203-209

Authors: Charushila Jaiswal, Y Verma, A B Shrivastav

72 male albino rats of the Wistar strain were randomly divided into 6 groups. Rats of control group I was fed with standard feed and water through out of experiment. Group II rats were treated with of E. coli (0.3 ml) by intra-peritoneal (I/P) inoculation, before 24 hrs of both sacrifices i.e.on 15th and 30th day of experiment. Group III was treated with chlorpyrifos reconstituted with 2 ml soya oil @10.6mg/kg b.wt. orally daily for 30 days. Group IV was treated with chlorpyrifos same as group III and I/P inoculation of E. coli (0.3 ml) was same as group II. Group V was treated with chlorpyrifos same as group III with α-tocopherol (VE) @150mg/kg b.wt. 30 minutes before the administration of CPF. Group VI was treated with chlorpyrifos same as group IV with Vitamin E @150mg/kg b.wt. 30 minutes before administration of CPF. This regimen was administered orally for the period of 30 days. At the time of sacrifice blood sample was collected i.e. on day 15th and 30th of the experiment. Oxidative stress was evaluated by measuring erythrocyte osmotic fragility test using different salt concentrations. The study showed that α-tocopherol protects erythrocyte osmotic fragility induced by repeated CPF exposure and E. coli infection in albino rats.

215-218

Authors: Mahendra Patel, Ashish K Parashar, MradulaTiwari, Arti J Majumdar, Rajesh K Nema

A simple, precise and economical procedure for the simultaneous estimation of Phenylephrine Hydrochloride (PHE) and Benzyl Alcohol (BEN) in formulation has been developed. PHE is a Vasocostracting agentandBEN is a Local anaesthetic agent. The absorbance values 229.6 nm and 274.2 nm of first derivative spectrum was used for the estimation of PHE and BEN, respectively without mutual interference. This method obeyed beer’s law in the concentration range of 25-250 μg/ml and 0.125-1.5 mg/ml forPHE and BEN respectively, in Methanol: Water (1:1) ratio.The slope and intercept for PHE were -0.001 and -0.008 and for BENwere -0.028 and -0.001 respectively as determined by the method of least squares. The results were found satisfactory and reproducible. The method was applied successfully for the estimation of PHE and BEN simultaneously in dosage form without the interference of common excipients.

134-141

Authors: Ashish Kumar Parashar and Rajesh Kumar Nema

Drug delivery to brain is still a challenging task due to the presence of the blood–brain barrier (BBB), a very restrictive barrier mainly composed of tightly sealed endothelial cells. The anatomy and physiology of BBB strictly regulates the brain access and clearance of endogenous and exogenous molecules from the systemic circulation. It is estimated that more than 98% of the new discovered central nervous system (CNS) potential drugs does not cross the BBB, failing to achieve therapeutic concentration within the brain parenchyma. Recent developments in the field of molecular biology enabled scientists to better understand the BBB and thus delivery of drugs to the brain, particularly under different pathological conditions. The aims of this Review are to outline current research in the field of brain barriers, the main advances made since 2000, the barriers to progress, and to recommend research priorities and the resources needed to advance the field. Applications of nanotechnology in drug transport, receptor-mediated targeting and transport, and finally cell-mediated drug transport will be discuss in the review. The challenge of delivering an effective dose of drug to the brain is formidable; solutions will likely involve multiple strategies that take into account the novel drug delivery systems as well as BBB biology.

149-152

Authors: Sweeti Jain, Minakshi Sharma, Rachana A Giri and A K Pathak

The aim of the study was to evaluate comparative antioxidant activity of different extract of Andrographispaniculata(AP) and Asparagus racemosus(AR). Simultaneously to observe the antioxidant effect of polyherbal formulation of both plant. In present study alcoholic and water extract of both plants was prepared and antioxidant activity was measured by nitric oxide scavenging activity and TBARS method (in vitro) and lipid peroxidation method (in vivo). Results indicate 1) Alcoholic extract of AR is more active than its aqueous extract. 2) Aqueous extract of AP is more active than its alcoholic extract. 3) Mixture of both alcoholic extract (polyherbal) show the high antioxidant activity compare to solo extract.

160-165

Authors: Ruchi Bhatia, Priyanka Rathore and Satish Nayak

A series of 1, 2, 4 triazole derivatives were synthesized and evaluated for their anti-inflammatory activity by paw edema test. All the synthesized compounds were in good agreement with spectral and physical data. Most of the compounds synthesized were active and the most potent synthesized compounds showed greater % inhibition than the standard drug ibuprofen. Conclusions could be drawn from the synthesized compounds that sulfonyl group plays an important role in anti-inflammatory activity. The Cut off LD50 was found to be 500mg/kg for all synthesized compounds when given orally.

171-176

Authors: A J Majumdar, A K Parashar and N K Jain

The unfolding development in the field of medical sciences have revolutionized the research in the field of advanced drug delivery. Sustained release or controlled release of drug delivery systems are designed to achieve a prolonged therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose. These products have been formulated for oral, injectable, and topical use. Several desirable therapeutic advantages can be achieved by using controlled released systems. Since the frequency of drug administration is reduced, patient compliance can be improved. The blood level oscillation characteristic of multiple dosing of conventional dosage forms are reduced, because a more even blood level is maintained. A less obvious advantage, implicit in the design of sustained release forms, is that the total amount of drug administered can be reduced; thus maximizing availability with a minimum dose.

180-185

Authors: Nidhi Jain and A K Pathak

Type 2 diabetes has become a global epidemic. Modern medicines, despite offering a variety of effective treatment options, can have several adverse effects. Ayurveda, a science that uses herbal medicines extensively, originated in India. From ancient times, some of these herbal preparations have been used in the treatment of diabetes. This paper reviews the accumulated literature for two Indian herbs that have antidiabetic activity and that have been scientifically tested. The name of these herbs, are Cucurbita maxima and Legenariasiceraria have been reported to be beneficial for treating type 2 diabetes. Mechanisms such as the stimulating or regenerating effect on beta cells or extra pancreatic effects are proposed for the hypoglycemic action of these herbs.