Abstract

Problem statement: Natural products have long been a fertile source of cure for cancer, which is projected to become the major cause of death in this century. Major classes of anticancer compounds include alkaloids, terpenoids, flavonoids and lignans. We have chosen terpenoids (bacosides) because terpenoids like taxol are currently being used in cancer chemotherapy. The anticancer activity of Bacoside A (containing Bacoside A3) isolated from the whole plant of plant Bacopa monnieiri (Linn.) was evaluated in in vitro and in vivo experimental models. Approach: The Bacoside A was isolated from ethyl acetate insoluble fraction (BM-2B) of chloroform: Methanol (2: 1) (BM-2) extract of B. monnieiri whole plant. The cytotoxicity (in vitro) of Bacoside A (BM2BF8-BSD) was carried out by means of MTT assay using MCF-7 (Human breast cancer), HT-29 (Human colon adeno carcinoma) and A-498 (Human kidney carcinoma) cell lines. The in vivo anticancer activity of Bacoside A was evaluated against Ehrlich Ascites Carcinoma (EAC) tumor bearing mice. Results: The Bacoside A (31.38 %) rich fraction, coded BM-2B containing Bacoside A3 (8.09 %) was showing potent cytotoxicity. Oral administration of BM-2B to tumor bearing mice at the dose of 250 and 500 mg kg-1 body weight for 10 days, showed significant reduction in percent increase in body weight, tumor volume, packed cell volume, viable tumor cell count and increased non-viable cell count when compared to the untreated mice of the EAC control group. The restoration of hematological parameters towards normalcy was also observed. Conclusion: The results suggests that the Bacoside A (31.38 % Bacoside A containing 8.09 % Bacoside A3) rich fraction (BM-2B) exhibits significant anticancer activity in both in vitro and in vivo experimental models.

Highlights

  • Natural products have long been a fertile source of cure for cancer, which is projected to become the major cause of death in this century

  • Isolation and characterization of major terpenoids or Bacosides (Bacoside A): As per High Performance Liquid Chromatography (HPLC) analysis, fraction Bacoapa mannieiri whole plant (BM)-2B was rich in Bacoside A (31.38 %)

  • In vivo anticancer activity: Animals: The ascitic antitumor studies induced by Ehrlich ascites carcinoma (EAC) tumor cells were carried out by using healthy adult Swiss albino mice weighing 20-25 g

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Summary

INTRODUCTION

Natural products have long been a fertile source of cure for cancer, which is projected to become the major cause of death in this century. The Bacopa monnieiri (Scrophulariaceae) whole plant constitutes the well known drug brahmi. It is astringent, laxative, carminative, digestive, depurative, cardiotonic, diuretic, bronchodilatory, emmenogogue, febrifuge and tonic. The triterpenoids reported from this plant Bacopa monnieiri are bacogenin A1, bacogenin A2 (an isomer of A1), bacogenin A3 and bacogenin A4 (embelin lactone) and known betulic acid and betulinic acid (Rastogi and Mehrotra, 1993). In the present study, we investigated the anticancer properties of major terpenoids Bacoside A (containing Bacoside A3) isolated from the whole plant of Bacopa monnieiri (Linn.) against Ehrlich ascites carcinoma (EAC) tumor bearing mice. Each fraction was filtered, concentrated and dried at reduced pressure and temperature using rotary evaporator, which yielded 75 g dark green colored BM-1A, 30 g green colored BM-1B, 115 g greenish brown BM-2A, 410 g brown colored BM-2B , 157 g brown colored BM-3A and 240 g colored brown BM-3B

MATERIALS AND METHODS
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