Abstract

Natural products are important sources for drug discovery, especially anti-tumor drugs. β-Elemene, the prominent active ingredient extract from the rhizome of Curcuma wenyujin, is a representative natural product with broad anti-tumor activities. The main molecular mechanism of β-elemene is to inhibit tumor growth and proliferation, induce apoptosis, inhibit tumor cell invasion and metastasis, enhance the sensitivity of chemoradiotherapy, regulate the immune system, and reverse multidrug resistance (MDR). Elemene oral emulsion and elemene injection were approved by the China Food and Drug Administration (CFDA) for the treatment of various cancers and bone metastasis in 1994. However, the lipophilicity and low bioavailability limit its application. To discover better β-elemene-derived anti-tumor drugs with satisfying drug-like properties, researchers have modified its structure under the premise of not damaging the basic scaffold structure. In this review, we comprehensively discuss and summarize the potential anti-tumor mechanisms and the progress of structural modifications of β-elemene.

Highlights

  • Cancer generally refers to various malignant tumors and is characterized by deregulated cellular behavior [1]

  • Interferences with the polymerization and decomposition of microtubules are a vital target for tumor drug therapy. β-Elemene injection effectively inhibits hepatoma HepG2 cell proliferation and arrests the cell cycle at the S phase associated with downregulating alpha-tubulin and inhibiting microtubular polymerization [28]

  • These effects were confirmed in the human hepatoma cancer HepG2 cells and breast cancer cell lines (Bcap37 and MBA-MD-231) [90,91]. These findings indicate that β-elemene in combination with autophagy inhibitors is a feasible way for the therapy of cancer

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Summary

Introduction

Cancer generally refers to various malignant tumors and is characterized by deregulated cellular behavior [1]. Radiotherapy, and chemotherapy are currently the main treatments for cancer, which can effectively kill cancer cells and cause serious adverse reactions due to the intervention affecting normal cells. Because the threelung olefinic bonds play important roles in cancer, liver cancer, esophageal cancer, its anti-tumor activity, the researchers have modified its structure under thecancer, premise nasopharyngeal cancer, brain and of for adjuvant treatment esophageal cancer retaining the basic scaffoldofstructure and the double bonds, including introducing hydrobone metastasis; intervention, intracavitary and gastric cancer to improve symptoms chemotherapy, carcinoma hydrothorax philic moieties like hydroxyl and amino groups to improve its and water solubility. Side effects ally loss of appetite; decreased he-modified tion; its mild digestiveunder tract reaction in its anti-tumor activity, the researchers have structure the premise moglobin; decreased leukocytes of retaining the basic scaffold structure and the double bonds, including introducing.

The Inhibition of Tumor Cell Proliferation and Growth
The Induction of Cell Apoptosis
The Inhibition of Tumor Cell Invasion and Metastasis
The Reverse of Multidrug Resistance
Enhancement of the Chemoradiotherapy Sensitization
The Activation of Protective Autophagy
The Regulation of the Immune System
Reduction
Chemical structures of β-elemene derivatives
Halogenated Derivatives of β-Elemene
Chemical structures of β-elemene oxidation derivatives
The chlorination and the chemical related products
Chemical
10. Chemical
Ester Derivatives of β-Elemene
Amino Acid Derivatives of β-Elemene
Glycoside Derivatives of β-Elemene
NO-Donating Derivatives of β-Elemene
Conclusions
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