To investigate the Nephroprotective activity of ethanol extract of Ficus dalhousiae on Gentamicin induced nephrotoxicity in male Wistar rats. In this model of nephrotoxicity, 30 adult male wistar rats (150- 200gms) were evenly divided into 5 groups. Group-1 and Group-2 served as untreated and model controls respectively, while Group-3, 4 and 5 were the treatments groups which were simultaneously treated with standard, 200 and 400 mg/kg extract respectively, after each dose gentamicin (80 mg/kg, i.p.) for 10 day . On 11 th day, blood samples for biochemical parameters, while the rats kidneys for histology were obtained under inhaled diether anaesthesia. Gentamicin treatment caused nephrotoxicity as evidenced by marked elevation in blood urea, uric acid and creatinine. Co-administration of extract with Paracetanmol decreased rise in blood urea, uric acid and creatinine. Apart from these, histopathological changes also showed the protective nature of extract against Gentamicin induced necrotic damage of renal tissues. It was observed that the ethanol extract of conferred nephroprotective activity by histopathological and biochemical observation against Gentamicin induced nephrotoxicity in rats. In the near future could constitute a lead to discovery of a novel drug for treatment of drug induced nephrotoxicity. Key words: Ficus dalhousiae, Gentamicin, nephrotoxicity KEY WORDS: Naltrexone, oxycodone, bulk dosage form
2.
DETERMINATION OF ESCITALOPRAM OXALATE AND ETIZOLAM IN TABLET DOSAGE FORMS BY RP-HPLC METHOD
M. Suresh Babu*, K.Sushmitha, P.Hima Sree, N.Sai Teja, P.G.S.Prakash
A simple and selective LC method is described for the determination of Escitalopram oxalate and Etizolam in tablet dosage forms. Chromatographic separation was achieved on a c18 column using mobile phase consisting of a mixture of 30 volumes of ammonium acetate buffer, 40 volumes of acetonitrile and 30 volumes of Methanol with detection of 238 nm. Linearity was observed in the range 60-140 μg/ml for Escitalopram oxalate (r2 =0.999) and 6-14 μg /ml for Etizolam (r2 =0.996) for the amount of drugs estimated by the proposed methods was in good agreement with the label claim. The proposed methods were validated. The accuracy of the methods was assessed by recovery studies at three different levels. Recovery experiments indicated the absence of interference from commonly encountered pharmaceutical additives. The method was found to be precise as indicated by the repeatability analysis, showing %RSD less than 2. All statistical data proves validity of the methods and can be used for routine analysis of pharmaceutical dosage form. KEY WORDS: Liquid chromatography (LC), RSD Relative standard deviation, r2 correlation coefficient.
3.
HEPATO AND NEPHROPROTECTIVE ACTIVITY OF ETHANOL EXTRACT OF SEBASTIANA CHAMAELEA ON PARACETAMOL INDUCED NEPHROTOXICITY IN MALE WISTAR RATS
To investigate the hepato and nephroprotective activity of ethanol extract of Sebastiana chamaelea on Paracetamol induced nephrotoxicity in male Wistar rats. In this model of nephrotoxicity, 30 adult male wistar rats (150-200gms) were evenly divided into 5 groups. Group-1 and Group-2 served as untreated and model controls respectively, while Group-3, 4 and 5 were the treatments groups which were simultaneously treated with standard, 2 0 0 and 400 mg/kg e x t r a c t respectively, after each dose of Paracetamol (200 mg/kg, i.p. for 3 days) from4 to 14 days . On 11 th day, blood samples for biochemical parameters, while the rats kidneys for histology were obtained under inhaled diether anaesthesia. Paracetamol treatment caused hepato a n d nephrotoxicity as evidenced by marked elevation in blood urea, uric acid and creatinine, bilirubin. Co-administration of e x t r a c t with Paracetanmol decreased rise in blood urea, uric acid and creatinine, bilirubin. Apart from these, histopathological changes also showed the protective nature of extract against Paracetamol induced necrotic and hepatic damage of renal and hepatic tissues. It was observed that the ethanol extract of conferred nephroprotective and hepatoprotective activities by histopathological and biochemical observation against Paracetamol induced nephrotoxicity and hepatotoxicity in rats. In the near future could constitute a lead to discovery of a novel drug for treatment of drug induced nephrotoxicity and hepato toxicity. KEY WORDS: Sebastiana chamaelea, Paracetamol induced nephrotoxicity, hepato and nephroprotective activity
4.
PHYTOCHEMICAL AND PHARMACOLOGICAL STUDIES ON WHOLE PLANT OF UTRICULARIA RETICULATA
Sarath Lal P.S,* Ajith Kumar. P, Ayshath Nafiya, Ayshath Shamseera.K, C. K. Khadeejath Thahira, Manasa.
ABSTRACT “Utricularia reticulata” is a medium to large sized probably annual carnivorous plant which is used by the tribes for the treatments of ulcers, wound healing, and neutralizing venoms of snakes, spiders, eye diseases. The study highlights the antibacterial studies of the plant thereby increasing the utilization of this commonly available plant for its medicinal property. The whole plants were collected, dried and subjected to successive solvent extraction. The phtyochemical and pharmacological studies were carried out. Further the extracts were tried for antioxidant activity and antimicrobial studies. Ethyl acetate extracts were shown significant antioxidant and antibacterial properties. Inspite of the data reveled form phytochemical screening and literature survey the phytoconstituents like alkaloids, glycosides, phenolic and flavonoids, flavonones, terpenoids and sterols present in the plant were responsible for the activities. Keyword: Utricularia reticulata, antioxidant, antibacterial.
5.
FORMULATION AND EVALUATION OF FAST DISINTEGRATING TABLETS OF DICLOFENAC SODIUM USING TREATED BANANA POWDER
Nisha K.V*, Ronald Peter, P. Ajith Kumar, Amaldev S., Ayshath Rabiya , Muhammed Nuhman N. P., Subair M. A.
ABSTRACT The purpose of this research project was to prepare fast disintegrating tablets of Diclofenac sodium, an NSAID drug by direct compression method using natural superdisintegrant (treated banana powder) and evaluate their various in-vitro properties. Diclofenac sodium was chosen as the drug with an aim to develop fast disintegrating tablets by direct compression method, which disintegrates quickly and have a release of drug faster than conventional tablets. A natural superdisintegrant (treated banana powder) with different concentrations were used in the development of formulations by direct compression method. The prepared tablets were evaluated for pre and post compression parameters like angle of repose, bulk density, tapped density, drug content, wetting time, in-vitro disintegration time, in-vitro dissolution studies. KEY WORDS: Diclofenac sodium, treated banana powder, superdisintegrant, fast disintegrating tablet
6.
PHARMACOGNOSTIC, PHYTOCHEMICAL, ANTIOXIDANT AND ANTI-INFLAMMATORY STUDIES ON THE LEAVES OF CHASSALIA CURVIFLORA
Sreepriya T K*, Alan Jacob*, P. Ajith Kumar, Anusree K P, Asiyath Shabana K J, Juzaira T P, Meenu Aleyas
ABSTRACT Chassalia curviflora is an evergreen shrub grows in tropical region. It is endemic to East Asia. It has potential uses like anti hypertensive, anti bacterial and traditionally used for eye infection, ear infection and insect bites. The present study highlights the phytochemical and invitro pharmacological studies of various extracts of Chassalia curviflora. The phytochemical screening of the plant extracts shows the presence of various chemical constituents. The chloroform extract shows potent antioxidant and anti-inflammatory activity when compared to other extracts. The presence of chemical constituents such as alkaloids, phenolics, flavanoids and saponins may be responsible for the anti oxidant and anti-inflammatory activities. KEYWORDS: Chassalia curviflora, antioxidant, anti inflammatory.
7.
SYNTHESIS, CHARACTERIZATION, INSILICO PREDICTION AND ANTI MICROBIAL ACTIVITY OF CHALCONE DEIVATIVES
ABSTRACT A novel series of six different derivatives of some NSAID chalcones were synthesized and characterized by physical & spectral interpretations like m.p., FT-IR & H1 NMR are confirmed. The derivatives of some NSAID chalcones were prepared from chalcone derivatives and hydrazine. The initial compounds for synthesizing derivatives are paracetamol ,aspirin and different aldehydes. The synthesized compounds are useful as a lead compounds for various diseases like antiulcer, antitumour, herbicidal, antifungal activites some infectious diseases. The derived chalcone pyrazoline derivatives were characterized by thin layer chromatography, infrared spectroscopic and NMR methods. The biological activity was tested and found to have anti-microbial activity against bacteria like E.coli (Gram negative organism), Pseudomonas aeuroginosa (Gram negative organism), Staphylococcus aureus (Gram positive organism) and Fungal Organism of Sacchromyces Species, Aspergillus Niger, Candida Albicans using filter-paper disc method. Most of the compounds exhibit mild to moderate anti bacterial activity as well as anti fungal activity against all the microbes tested. Key Words: NSAID chalcones, insilico prediction, antimicrobial activity
8.
SYNTHESIS OF THE 2, 4, 6-TRISUBSTITUTED PYRIMIDINES AND SCREENING OF ANTI-BACTERIAL ACTIVITY
ABSTRACT Aim of the study is to synthesize some new 2, 4, 6-trisubstituted pyrimidines by conventional method. All the synthesized compounds were characterized by FT-IR and1H-NMR spectral studies and the structures were established. All the synthesized compounds were predicted for biological properties by using PASS computer programme and screened for Anti-Bacterial activity in Staphylococcus aureus&E.coliby using Ciprofloxacin as standard. From the results of Anti-bacterial activity, it was clear that the compounds SB-4, SB-5, SB-8 & SB-9 exhibit significant activity in comparison with that of standard. This may be due to the presence of electron donating groups like Nitro group at position -6 of the parent molecule. Key Words: 2,4,6-Trisubstituted Pyrimidines, anti-bacterial activity
9.
FORMULATION OF CRYSTALLO-CO-AGGLOMERATES OF TELMISARTAN: STUDY OF EFFECT OF POLYMERS ON DRUG RELEASE
Chaithanya .A.P*, Ajith Kumar. P, Ayishath Shabna, Mohammed Dilkush K.A, Mohammed Munawar, Moideen Farhan
ABSTRACT The present work is aimed to formulate spherical agglomerates of telmisartan by crystallo-co-agglomeration technique and enhance the micromeritic properties, solubility and dissolution rate of telmisartan, a poorly water soluble anti-hypertensive drug. Chloroform-water system containing PEG 6000 & HPMC in different concentration was used as the crystallization medium. Chloroform act as good solvent and bridging liquid for telmisartan and water as bad solvent. The agglomerates were characterized to various physicochemical evaluations such as practical yield, drug content, particle size, FTIR spectroscopy, scanning electron microscopy, micromeritic properties and solubility analysis. The dissolution studies were carried out using PBS of pH 7.4 as dissolution media maintained at 37.5°C for 70 minutes. The dissolution data demonstrate that the rate of drug release is dependent upon the nature and concentration of polymer used in the formulation. Formulation TP2 (combination of telmisartan and PEG 6000) in the ratio 1:1.5 was selected as an optimum formulation which showed better results with respect to drug release, solubility and micromeritics when compared to other formulation. Key Words: Telmisartan, Crystallo-co-agglomerates, PEG6000, HPMC.
10.
SYNTHESIS AND EVALUATION OF ANTI MICROBIAL ACTIVITY OF 2-METHYLAMINO BENZIMIDAZOLE DERIVATIVES
Seethalakshmi, Asmath Maziyuna fabin, Muhammed Anas, Muhammed Sabith B, K, Arun Ramachandran*, Ajith Kumar P
ABSTRACT Substituted 2-methylamino benzimidazoles were synthesized by refluxing 2-methylamino benzimidazole with urea and thiourea in presence of methanol. Synthesis of 2-methylamino benzimidazole from o-phenylene diamine by refluxing with glycine in presence of HCl. The structures of final synthesized compounds were assigned on the basis of IR spectral data. All the newly synthesized compounds were screened for their in-vitro antimicrobial activity against various species of bacteria by cup plate method. The zone of inhibition exhibited by all the derivatives at a concentration of 250μg and 500μg was compared to that of standard ciprofloxacin at a concentration of 5μg. The compounds were good antibacterial agents against the tested organisms when compared to the standard ciprofloxacin. Key Words: Benzimadazole, o-phenylene diamine, glycine, antimicrobial.
11.
SYNTHESIS AND ANTI INFLAMMATORY ACTIVITY OF SOME NEW PRENYLATED 5, 7-DIHYDROXY FLAVONOID ANALOGS
ABSTRACT 5,7-dihydroxy-2[2-(3-methylbut-2-en-1-yl)phenyl]-2,3-dihydro-4H-1-benzopyran-4-onewere prepared with different chloro phenyl acetic acid under mild conditions to give corresponding prenylated flavones, the title compounds in good yields. Lead compound synthesized were characterized by physical (Rf values, Melting point, Molecular weight, Molecular formula) and spectral data (1H NMR, IR, Mass spectra). In carageenan induced paw edema compounds 4,7,10 significantly inhibited the edema in a dose dependent manner. The paw volume in rats pretreated with lower dose of compounds 4,7,10 (100 mg/kg/day), higher dose of compounds 4,7,10 (200 mg/kg/day) and indomethacin (10 mg/kg/day) at 2nd hr were found to be 0.191  0.0061 ml, 0.158  0.0042** ml and 0.1369  0.0054** ml. Key Words: prenylated 5,7-dihydroxy flavonoid, anti inflammatory activity.
12.
FORMULATION AND EVALUATION OF NATURAL BINDING AGENTS IN MORINGA OLIEFERA TABLET
Prothibha Das, P Ajith Kumar, Anushree, Sruthina, Sharafudeen B M, Junaid Abdulla.
A study was carried out to investigate the efficiency of different natural binding agent such as gum of Okra fruit, gum of Hibiscus flower, gummy exudates of Moringa tree and gum of Aloe-Vera in Moringa oleifera tablet. Moringa oleifera is widely used for both nutrition and medicinal activity. The physical parameters used were weight variation, harness, friability, disintegration time and antimicrobial assay. The results of this study showed that Aloe-Vera gum produced tablet with higher hardness, disintegration time and increased antimicrobial activity. In conclusion, Aloe-Vera gum has good tablet binding properties and could be employed as a substitute for more expensive binders in fast or immediate release tablet.
13.
PHARMACOGNOSTIC STUDIES AND EVALUATION OF ANTIOXIDANT, ANTI-INFLAMMATORY ACTIVITY OF VARIOUS EXTRACTS OF CHASSALIA CURVIFLORA (WALL.) THWAITES ROOT
Sreepriya T.K, Bindu.K, Sarath Lal, Ajith Kumar. P, Alan Jacob
The roots of the plant Chassalia curviflora (Rubiaceae) have been used by Kani tribes for the treatment of colic pain and to heal wounds and pimples. Oil boiled with the juice of the leaves is used for eye and ear disease, ulcer and sore throat. Decoction of root is given as a remedy in phlegm, rheumatism and pneumonia. The work highlights pharmacognostic studies and evaluation of antioxidant, anti-inflammatory activity of various extracts of the roots of plant Chassalia curviflora. The pharmacognostic studies like loss on drying, ash values total ash value, extractive values, crude fibre content were done on the plant proved to be a tool for the authentication and identification of the plant The antioxidant activity studies using Iron chelating assay, DPPH radical scavenging assay and total antioxidant assay showed that ethyl acetate extract could be a promising source of natural antioxidants. The anti inflammatory activities by inhibition of protein denaturation and proteinase inhibitory assay showed ethyl acetate extract to possess potent anti inflammatory activity. Thus the roots of the plant Chassalia curviflora can be suggested to be used in diseases like phlegm, rheumatism and pneumonia due to its antioxidant and anti inflammatory properties. Key words: Chassalia curviflora, antioxidant, anti inflammatory
14.
SYNTHESIS OF SOME PYRIMIDINE DERIVATIVES AND EVALUATION OF THEIR ANTIBACTERIAL ACTIVITES
Sebastin V, Aneesh K.A, Sarath Lal P.S, P. Ajith Kumar, Jawad C
Antimicrobial agents play key role in the management of infections. Challenges faced by the chemists to develop a wide spectrum antimicrobial agent were the antibiotic resistance occurred due to the misuse of these agents. Pyrimidine is prevalent in numerous natural products and posses a wide range of biological activities. The work includes the synthesis of some 1,3-dihydro pyrimidine derivatives from different substituted aldehydes. Pyrimindine derivatives (6a,6b,6d) were synthesized from different aromatic aldehydes and screened for their antimicrobial properyies in gram positive (Bacillus subtitis, Staphylococous aureus) and gram negative (Pseudomonas aeruginosa, Escherichia coli) organisms at concentration 400μg/disc and 200μg/disc. The compound 6b (phenyl derivative) have significant antimicrobial properties than other synthesized derivatives. Key words: Purines, Pyrimidines, substituted aldehydes, antibacterial.
15.
INVITRO AND INVIVO ANTICANCER ACTIVITY OF METHANOL EXTRACT OF NYMPHOIDES KRISHNAKESARA VAR.BISPINOSA
ABSTRACT Worldwide cancer is the major cause of death. Millions of people died due to different types of cancer such as lung cancer, liver cancer, breast cancer, stomach cancer, blood cancer etc. Couples of therapies like chemotherapy, radiation, surgery and targeted therapy are available with some detrimental effect. Natural phytochemicals are prominent strategy for prevention, treating, and curing cancer. There are many plants (phytochemicals) possess anti-cancer activity that exhibits additive or synergistic activity. Generally these phytochemicals treat cancer by different mechanisms like augmenting apoptosis, cell cycle arrest, targeting to some specific cancer inducing proteins, increasing cytotoxicity etc. In this study a methanol extractfrom whole plant Nymphoides krishnakesara Var. Bispinosa male and female plantswere evaluated for in vitro anticancer activity by MTT cell viability assay and in vivo anticancer activity by DAL (Dalton’s Ascites Lymphoma) Induced Anticancer Study.The viability of cells were evaluated byMTT assay method.These studies indicates positive anticancer activity of the extractNymphoides krishnakesara Var. Bispinosa male and female (whole plant) by invitro as well as in vivo study. Key Words: MTT (3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide), DAL (Dalton’s Ascites Lymphoma), synergistic, anticancer.