DOI: http://dx.doi.org/10.18203/2319-2003.ijbcp20174385

Evaluation of antioxidant activity of ormeloxifene: in vitro study

Vinay M., Seethalakshmi S., Vijay Kumar

Abstract


Background: Ormeloxifene (Centchroman) is a Selective Estrogen Receptor Modulator (SERM) which acts as estrogen antagonist and having anti progestogenic activity also. It is being used in the management of dysfunctional uterine bleeding and as nonhormonal oral contraceptive. It is also being investigated for the indications such as osteoporosis, breast and endometrial carcinoma. In this study, we have evaluated the Antioxidant potential of drug by using DPPH and NO synthase Assay. It was found that ormeloxifene has significant antioxidant activity which could be cause for its use in various gynaecological and other conditions.

Methods: In this study, we have demonstrated in vitro antioxidant activity of ormeloxifene. DPPH and NO synthase assay tests were done for different concentrations of ormeloxifene.

Results: In our study, it showed that the free radical scavenging activity of ormeloxifene was less in lower concentration and increased in the higher concentration in DPPH assay. The free radical scavenging activity of drug ormeloxifene was 22% at 100µg/ml and 27% for the concentrations of 1000µg/ml in DPPH assay. No scavenging activity was 3% at 100µg/ml and 11% at 1000µg/ml.

Conclusions: The invitro antioxidant analysis of ormeloxifene, was proved to be a potent antioxidant.


Keywords


DPPH (1,1-diphenyl-2-picrylhydrazy) assay, Nitric oxide synthase assay, Ormeloxifene, Selective estrogen receptor modulator

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References


Chang BY, Kim SA, Malla B, Kim SY. The effect of selective estrogen receptor modulators (SERMs) on the tamoxifen resistant breast cancer cells. Toxicol Res. 2011;27:85-93.

Kriplani A, Kulshrestha V, Agarwal N. Efficacy and safety of ormeloxifene in management of menorrhagia: A pilot study. J Obstet Gynaecol Res. 2009;35:746-52.

Singh MM. Centchroman, a selective estrogen receptor modulator, as a contraceptive and for the management of hormone-related clinical disorders. Med Res Rev. 2001;21:302-47.

Hormones and related drugs. In: Tripathi KD, editor. Essentials of Medical Pharmacology, 7th edition. New Delhi: Jaypee Brothers Medical Publishers; 2014:327.

Hormones and Hormone Antagonists. In: Sharma HL & Sharma KK, editors. Principles of Pharmacology, 2nd edition. New Delhi: Paras Medical Publishers; 2011:587.

Yohozowa T, Chen CP, Dong E, Tanaka T, Nonaka GT. Studies on the inhibitory effect of tannins and flavonoids against radical. Biochemical Pharmacology; 1998:212-242.

Alderson WK, Cooper CE, Knowels RG. Nitric oxide synthesis, structure, function and inhibition. Journal of Biologycal Chemistry; 2001:593-615.

Dhawan BN, Srimal.RC. Anti-inflammatory and some other pharmacological effects of 3,4-trans-2,2-dimethyl-3-phenyl4-[p-(B-pyrrolidinoethoxy)-phenyl]-7-methoxy-chroman (Centchroman). Br. J.Pharmac. 1973;49:64-73.

Khalid Rahman. Studies on free radicals, antioxidants and co-factors. Clinical Interventions in Aging. 2007;2(2):219-23.

Kedare SB, Singh RP. Genesis and development of DPPH method of antioxidant assay. J Food Sci Technol. 2011;48(4):412-22.

Marinova G, Batchvarov V. Evaluation of the methods for determination of the free radical scavenging activity by DPPH. Bulg J Agric Sci. 2011;17(1):11-24.

Patel RM, Patel NJ. In vitro antioxidant activity of coumarin compounds by DPPH, super oxide and nitric oxide free radical scavenging methods. J Adv Pharm Educ Res. 2011;1:52-68.