Current Research in Pharmaceutical Sciences

108-113

Authors: Neha Sahu, Jagdish K Sahu and Atul Kaushik

Triazole is an entity which is being synthesized in many of its derivative form from past few years; the entity is major source of interest for many of medicinal chemist to explore its various pharmacological potentials. Various methods for synthesizing triazoles are discussed with their chemistry. Studying this chemistry different substituted and fused compounds of triazole are analyzed here for varying pharmacological activities. In present article we review the chemistry of triazole and its pharmacological actions as antihelmintics, anticancer, antifungal and anti-inflammatory agent by studying its various synthesized derivatives.

122-131

Authors: H K Sharma and V Alagarsamy

In this study we aimed to fix Rungia repens (L) Nees botanical identity, macroscopical, microscopical diagnostic characters and to isolate the bio-active principle responsible for biological actions shown by ethyl acetate and methanol extracts. Bioactive compounds were isolated by running column chromatography, characterized and percentage of activity of bioactive principle was calculated. Microscopical study reveals the characteristic nature of stomata, trichome, leaf mid rib and stem. The extracts were found to be non toxic upto the dose of 3000 mg/kg of Rungia repens ethyl acetate extract (RREAE) and methanolic extract (RRME) respectively. RREAE and RRME produced a significant and dose dependent inhibition of analgesic, anti inflammatory and antipyretic activity. Bioactive principle isolated was a flavonoid luteolin shows maximum activity equal to that of standard drug. We believe that the antipyretic, analgesic, and anti-inflammatory activity of the RREAE and RRME were due to its bioactive principle flavonoid luteolin present in the extract.

138-143

Authors: Asheesh Singh, Amit Jain and Bhawna Mishra

A QSAR study on 4-benzylideneamino-benzenesulfonamide & 4-phenyliminomethyl-benzenesulfonamides derivatives as selective cyclooxygenase-2 (COX-2) & COX-1 inhibitors was performed with 21 (16 training + 5 test) compounds. Molecular modeling studies were performed using Chemoffice 6.0 supplied by cambridgesoft. The sketched structures were subjected to energy minimization and the lowest energy structure was used to calculate the physiochemical properties. The regression analysis was carried out using a computer program called VALSTAT. The best models were selected from the various statistically significant equations. The substitution Different monosubstituents preferably at the 3- or 4-position of the phenyl ring had the greatest influence on selectivity (COX-1 & COX-2). Replacement of the 4-hydroxy moiety with an electron withdrawing group such as 4-fluoro, 4-methoxycarbonyl, or 4-nitro substituents increased inhibitory potency and selectivity. However, 3-nitro substituent resulted in loss of inhibitory potency. On the other hand, the 4-N, N-dimethylamino substituent exhibited potent and selective inhibition of cyclooxygenase. Among these compounds with monosubstituted at the para-position, cyclooxygenase the inhibitory selectivity order was 4-F > 4-CO2Me > 4-NMe2 > 4-NO2 > 4-OH > unselective 3-NO2. The analysis resulted in QSAR equation, which suggests that, n=16, r=0.880, r2=0.774, adjusted squared multiple R=0.713, Standard error of estimate(s) = 0.106 & validated r2 (q2) =0.671. This study can help in rational drug design of new cyclooxygenase-2 inhibitor with predetermined affinity.

148-153

Authors: Veerendra Sharma, Pooja Sinoriya and S C Mehta

To investigate the anticonvulsant and CNS depressant activity of methanolic extracts of whole plant of Sida acuta and Sida rhombifolia in mice. The methanolic extract of whole plant of Sida acuta (MESA) and Sida rhombifolia (MESR) (100, 200 and 400 mg/kg, p.o.) was studied for its anticonvulsant effect on maximal electroshock (MES) induced seizures and Pentylenetetrazole (PTZ) induced seizures and CNS depressant activity at the same dose level using traction test, rota rod and locomoter activity in mice. MESA and MESR at dose 100, 200 and 400 mg/kg significantly reduced the duration of the seizures as compared to control group. In CNS depressant activity and the mean time duration on rotating rod was significantly decreased (P<0.0001) and decline in motor co-ordination.

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.