In vivo Evaluation of Antiproliferative Activity of a Novel Benzimidazole De-rivative Against Daltons Lymphoma Ascitic in Swiss Albino Mice
Keywords:Antiproliferative activity, Benzimidazole, DAL, Haematological parameters
The present work was to evaluate the antiproliferative activity of a novel benzimidazole derivative, [N-[3-chloro-2-oxo-4-(2-hydroxyphenyl)-4-oxoazetidin-1yl]-2-(2-methyl-1H-benzimidazol-1-yl)acetamide] against tumour induced in female Swiss albino mice. The effective dose of the test compound was determined as 10 mg/kg body weight. Two doses of the test compound were used for the evaluation. 5- Fluorouracil at a dose of 20 mg/kg body weight was used as the standard. Derived, haemotological and biochemical parameters were evaluated. RBC, Hb level, platelet count and packed cell volume that reduced significantly in cancer control group became normal after treatment with test drug. WBC count that increased significantly in DAL control group became normal by treatment with test drug. The results strongly support the antiproliferative activity of novel benzimidazole derivative [N-[3-chloro-2-oxo-4-(2-hydroxyphenyl)-4-oxoazetidin-1yl]-2-(2-methyl-1H-benzimidazol-1-yl)acetamide] against cancer induced female Swiss albino mice.
Walia, R., Hedahitulla, M., Naaz, S.F., Iqbal, K., Lamba, H.S., 2011. Benzimidazole derivatives- An Over-view. Int. j. pharm. chem. biol. sci. 1 (3), 565-74.
Soderlind, K.J., Gorodetsky, B.,Singh, A.K., Bachur, N.R., Miller,G.G., Lown, J.W., 1999. Bis-benzimidazole anticancer agents: Targeting human tumour helicases. Anticancer Drug Des. 14, 19–36.
Kapuriya, K., Ganure, A., Davda S., Kitawala, M., Topiya, H., 2013. Benzimidazole: A promising Lead for Anticancer Drug Design. UJP. 02(03), 57-62.
Kumar, K., Awasthi, D. Lee, S.Y., Cummings, J.E., Knudson, S.E., Slayden, R.A., Ojima, I., 2013. Benzimi-dazole- based antibacterial agents against Francisella tularensis. Bioorg. Med. Chem. 21, 3318–3326.
Mentese, E., Bektas, H., Ulker, S., Bekircan, O., Kahveci, B., 2014. Microwave-assisted synthesis of new benzimidazole derivatives with lipase inhibition activity. J. Enzyme Inhib. Med. Chem., 29, 64–68.
Vel??k, J., Baliharová, V., Fink-Gremmels, J., Bull, S., Lamka, J., Skálová, L., 2004. Benzimidazole drugs and modulation of biotransformation enzymes. Res. Vet. Sci., 76, 95–108.
Janupally, R., Jeankumar, V.U., Bobesh, K.A., Soni, V., Devi, P.B., 2014. Structure-guided design and de-velopment of novel benzimidazole class of compounds targeting DNA gyrase B enzyme of Staphylococcus aureus. Bioorg. Med. Chem., 22, 5970–5987.
Tonelli, M., Paglietti, G., Boido, V., Sparatore, F., La Colla, P.,Loddo, R., 2008. Antiviral activity of ben-zimidazole derivatives. I. Antiviral activity of 1-substituted-2-[(benzotriazol-1/2-yl) methyl] benzimida-zoles. Chem. Biodivers., 5, 2386–2401.
Vitale, G., Corona, P., Loriga, M., Carta, A., Paglietti, G., Loddo, R, 2010. Styryl benzimidazoles. Synthesis and biological activity. Med Chem., 6(3), 70–78.
Tonelli, M., Simone, M., Tasso, B., Novelli, F., Paglietti, 2010. Antiviral activity of benzimidazole deriva-tives. II. Antiviral activity of 2-phenylbenzimidazole derivatives. Bioorg. Med. Chem., 18, 2937–2953.
Vitale, G., Corona, P., Loriga, M., Carta, A., Farci, P., Marongiu, M.E. 2012. 5-Acetyl-2-arylbenzimidazoles as antiviral agents. Eur. J. Med. Chem., 53(4), 83–97.
Tonelli, M., Novelli, F., Tasso, B., Sparatore, F., Sanna, G., Giliberti, G., 2014. Antiviral activity of benzimidazole derivatives. III. Novelanti-CVB-5, anti-RSV and anti-Sb-1 agents. Bioorg. Med. Chem., 22, 4893–4909.
Ke, Y., Zhi, X., Yu, X., Ding, G., Yang, C., Xu, H., 2014, 2015. Combinatorial synthesis of benzimidazole-azo-phenolderivatives as antifungal agents. Comb. Chem. High Throughput Screen, 17, 89–95. Molecules, 20 15222
Achar, K.C.S., Hosamani, K.M., Seetharamareddy, H.R., 2010. In vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives. Eur. J. Med. Chem., 45, 2048–2054
Datar, P.A., Limaye, S.A., 2015. Design and Synthesis of Mannich bases of Benzimidazole Derivatives as Analgesic Agents. Anti-Inflamm. Anti-Allergy Agents Med. Chem, 14, 35–46.
Shingalapur, R.V., Hosamani, K.M., Keri, R.S., Hugar, M.H., 2010. Derivatives of benzimidazole pharmacophore: Synthesis, anticonvulsant, antidiabetic and DNA cleavage studies. Eur. J. Med. Chem., 45, 1753–1759.
Dona S.N., Suresh, K.A., Chakraborty, K., Valluru, L., 2018. In vitro Antiproliferative effect of Marine Macroalgae on different Human Cancer Cell lines. Int. j. pharm. drug. anal. 6 (2), 342-51.
Arul. K., Anton Smith. A., 2016. Evaluation of Anti Neoplastic Activity of a New 1, 2, 4 - Triazole Derivative Against Dalton’s Lymphoma Ascitic in Mice. Transylvanian Review, 24(5), 478- 482.
Ecobichon, D.J., The basis of toxicology testing, 2nd ed. 43-60, (1997)
Jaslin, E.J., Padmaja, V., 2015. Anticancer activity of Coleus vettiveroids K.C Jacob against Dalton’s ascitic lymphoma. International. Journal of trends in pharma. and life sciences., 1(5), 553-557.
Sathyanarayanan, L., Shinnathambi, Anilmozi, Chidhambranthan, N., 2006. Anticarcinogenic activity of Leptadenia reticulata against Dalton’s ascitic lymphoma. Iranian Journal of Pharmacology and Therapeutics. 6, 133-136.
Mahender Mohan. V., Murugan., Geetha, K. M., Mahesh Kumar, K, 2018 Synthesis Of Bis - [2-(Chloroethyl) Amino] Acetamido - 4 - Substituted Phenyl Thiazole Derivatives as Possible Antioxidant and Alkylating Anticancer Agents. Int. j. pharm. drug. anal. 6(3), 352 – 360.
Jacqueline, M.H., Darius, J.N., Mathew, J.M., Ronald, D.B., 1998. Blood lipid profile in children with acute lymphoblastic leukemia. Cancer. 83(2), 379 – 384.
Ronald, A.S., 1995. Disease of white blood cells. Wildman’s Clinical Interpretation of Laboratory Tests. 10th ed. 164.
Viroj, W., 2001. High serum alkaline phosphatase levels, a study in 181 Thai adult hospitalized patients. BMC Family Practice, 2(2), 293-309.
Intyre, M.C., Rosalki, S., (1991), Biochemical investigations in the management of Liver Disease. In: Oxford Text book of Clinical Hepatology, Oxford University Press, Chennai. 293-309.
Santhosh, K.H., Senthil, K.N., Reghu, C.H., 2007. Antitumor activity of Methanolic extract of Hypericum hookerianum on EAC cell line in swiss albino mice. J. Pharmacological. Sci. 103, 354- 359.
William, A.S., Hariharan, M., 2013. Production of Methioninase from Serratia marcescens isolated from soil and its anticancer activity against Dalton’s Lymphoma Ascites (DLA) and Ehrlich Ascitic carcinoma (EAC) in Swiss albino mice. Trop. J. Pharmaceut. Res. 5, 13, 699 – 704.
Bhaskar, V.H., Rajalakshmi, V., 2010. Antitumor activity of aqueous extract of Biophytum sensitivum Linn. Ann. Biol. Res. 1(3), 76-80.
Aravind, S., Joseph, M.M., Varghese, S., Balaram, P., Sreelekha, T.T., 2012. Antitumor and immune potentially activity of Polysacharide PS Tool isolated from the seed kernal of Tamarindus indica: An in vivo study in mice. Sci. World J. 1-14.
Patel, M.S., Antala, B.V., Dowerah, E., Senthilkumar, R., Lahlean, M., 2014. Antitumor activity of Pogostemos benghalensis Linn. on Ehrlich Ascites Carcinoma tumor bearing mice. J. Canc. Res. Therapeut. 4, 10, 1071 – 1075.
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