Abstract

Calotropis procera is traditionally used for treating many diseases including ulcers and tumors. It was thus deemed of interest to investigate and compare the antiulcer and cytotoxic activities of C. procera leaf, flower, and fruit extracts in an attempt to verify its traditional uses. Phytochemical studies on the fruits, flowers, and leaves of C. procera, collected from the desert of Saudi Arabia, led to the isolation of one new lignan 7′-methoxy-3′-O-demethyl-tanegool-9-O-β-d-glucopyranoside and five known compounds from the flowers, four compounds from leaves, and a flavonoid glycoside and a lignan glycoside from the fruits. The structures of compounds were determined by spectroscopic techniques. Ethanol extracts of the three parts of C. procera were evaluated for their antiulcer activity and we found that the leaf extract possessed a powerful antiulcer activity which could be considered as a promising drug candidate. All the extracts and the isolated compounds were evaluated for their cytotoxic activity against MCF-7, HCT-116, HepG-2, and A-549 human cancer cell lines. Compound 2 was highly active on all the cell lines, whereas compounds 5 and 11 were more selective on colon and liver cell lines. Compound 10 demonstrated a significant activity on liver and lung cancer cell lines.

Highlights

  • Calotropis procera (Cp) is a xerophytic perennial shrub native to tropical and subtropical Africa and Asia and common in the Middle East [1]

  • The decoction of the aerial parts of Cp is commonly used in Saudi Arabian traditional medicine for the treatment of a variety of diseases including fever, tumors, joint pain, ulcer, muscular spasm, and constipation [1,2,3]

  • All the extracts and the isolated compounds were evaluated for their cytotoxic activity against MCF7, HCT-116, HepG-2, and A-549 human cancer cell lines and we found that compound 2 showed significant activity on all the tested cancer cell lines, while compounds 5 and 11 exhibited strong activity against colon and liver cancer cell lines

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Summary

Introduction

Calotropis procera (Cp) is a xerophytic perennial shrub native to tropical and subtropical Africa and Asia and common in the Middle East [1]. It is known in Arabic as Ushar, found in northern and southern Hijaz, in the central region, and in southern and northeastern regions of Saudi Arabia. Different parts of Cp had been widely used in traditional medicine due to its pharmacologically active compounds found in all the plant’s parts, flowers, roots, and leaves, and its milky latex which is an exudate from damaged and broken leaves and stems. The whole parts of Cp have been investigated previously for its phytoconstituents, which revealed the presence of cardenolides, anthocyanins, and triterpenoids [6]

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