The reversal of antineoplastic drug resistance in cancer cells by β-elemene

Zhang, Guan‐Nan; Ashby, Charles R.; Zhang, Yun‐Kai; Chen, Zhe‐Sheng; H, Guo

doi:10.1186/s40880-015-0048-0

Cited by 34 publications

(27 citation statements)

References 63 publications

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“…1A and D). These results are consistent with those of previous studies in which β-elemene was toxic to tumor cells at high concentrations, but was non-toxic or minimally toxic to normal cells [2,5,6,11,12,14,17,22]. …”

Section: β-Elemene Reduces Human Sperm Vitality and Motilitysupporting

confidence: 83%

β-Elemene Inhibits Human Sperm Function by Affecting Sperm Vitality and Intracellular Calcium

Chen

Weng

et al. 2018

Cell Physiol Biochem

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Background/Aims: β-Elemene is a bioactive sesquiterpene compound that exhibits a potent anti-tumor effect and is used in various clinical applications. However, little is known about its effect on the male reproductive system. The objective of this study was to investigate the in vitro actions of β-elemene on human sperm function and elucidate the underlying mechanism. Methods: The cytotoxicity of β-elemene toward MCF-10A, MDA-MD-231, and A549 cells was evaluated with cell proliferation and colony formation assays. Additionally, human sperm were treated with different concentrations (0, 10, 20, 40, 80, 160, and 320 µM) of β-elemene in vitro. The characteristics in human sperm essential for fertilization, including vitality, motility, capacitation, acrosome reaction, responsiveness to progesterone, and intracellular calcium concentration ([Ca²⁺]_i) were examined with a computer-assisted sperm analysis system, chlortetracycline staining, and a fluorescent Ca²⁺ indicator. Results: A comprehensive evaluation of sperm motility, especially hyperactivated motility, revealed that treatments with 40–320 μM β-elemene decreased human sperm vitality, motility (total motility, progressive motility, and curvilinear velocity), and penetrating ability in a dose-dependent manner, but were non-toxic or minimally toxic toward MCF-10A, MDA-MD-231, and A549 cells. Although 10 and 20 μM β-elemene did not affect sperm vitality and motility, these concentrations increased the spontaneous acrosome reaction and inhibited progesterone-induced sperm functions by affecting sperm [Ca²⁺]_i. Conclusion: These results suggest that β-elemene inhibits human sperm function by affecting sperm vitality and [Ca²⁺]_i. These observations must be considered when using β-elemene to treat cancer patients who may wish to preserve their fertility.

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Section: β-Elemene Reduces Human Sperm Vitality and Motilitysupporting

confidence: 83%

β-Elemene Inhibits Human Sperm Function by Affecting Sperm Vitality and Intracellular Calcium

Chen

Weng

et al. 2018

Cell Physiol Biochem

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“…This compound showed protective effects against oxidative stress in the nematode Caenorhabditis elegans and prolonged its lifespan. [43] In addition, b-elemene proved to be highly effective as larvicidal against the mosquitoes Anopheles subpictus, Aedes albopictus, and Culex tritaeniorhynchus and safe against the non-target fish Gambusia affinis. [36] Ledol is a tertiary sesquiterpene alcohol reported for the first time in marsh rosemary (Ledum palustre L.), [37] and also extracted from the bark extracts of Calophyllum teysmannii MIQ.…”

Section: Chemical Composition Of Essential Oilsmentioning

confidence: 99%

Cytotoxic Essential Oils from Eryngium campestre and Eryngium amethystinum (Apiaceae) Growing in Central Italy

Cianfaglione

Blomme

Quassinti

et al. 2017

Chemistry & Biodiversity

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Eryngium campestre and E. amethystinum are thorny herbs belonging to the Apiaceae family and spontaneously growing in stony pastures and dry meadows, preferentially on calcareous substrates. In the Mediterranean countries, these plants have been used as a food or traditional remedies to treat various ailments. In the present work, we have analyzed the chemical composition of the essential oils distilled from the aerial parts by GC-FID and GC/MS, and evaluated their cytotoxic effects on a panel of human cancer cells, namely A375 (human malignant melanoma), MDA-MB 231 cells (human breast adenocarcinoma), and HCT116 cells (human colon carcinoma), by the MTT assay. Furthermore, the Eryngium essential oils were evaluated for antioxidant and acetylcholinesterase (AChE) activities. The two essential oils were rich in sesquiterpene hydrocarbons, with germacrene D as the major compound, accompanied by allo-aromadendrene, β-elemene, spathulenol, and ledol. They turned out to be highly cytotoxic on the tumor cells, with IC values (1.65 - 5.32 and 1.57 - 2.99 μg/ml for E. amethystinum and E. campestre, respectively) comparable or close to those of the anticancer drug cisplatin. The E. amethystinum essential oil exhibited a moderate antioxidant activity, whereas that of E. campestre a weak AChE inhibition.

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“…β-Elemene is less cytotoxic and could enhance the sensitivity to radiotherapy and chemotherapy. 36,37 Although the inhibition of PKM2 could lead to inhibition of cancer cell proliferation, most of cancer cells could survive by another compensatory glutaminolysis way. 38 Whether β-elemene can overcome this problem needs further examination.…”

Section: Discussionmentioning

confidence: 99%

Beta‐elemene inhibits breast cancer metastasis through blocking pyruvate kinase M2 dimerization and nuclear translocation

Pan

Wang

Huang

et al. 2019

J Cellular Molecular Medi

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Pyruvate kinase M2 (PKM2), playing a central role in regulating aerobic glycolysis, was considered as a promising target for cancer therapy. However, its role in cancer metastasis is rarely known. Here, we found a tight relationship between PKM2 and breast cancer metastasis, demonstrated by the findings that beta‐elemene (β‐elemene), an approved drug for complementary cancer therapy, exerted distinct anti‐metastatic activity dependent on PKM2. The results indicated that β‐elemene inhibited breast cancer cell migration, invasion in vitro as well as metastases in vivo. β‐Elemene further inhibited the process of aerobic glycolysis and decreased the utilization of glucose and the production of pyruvate and lactate through suppressing pyruvate kinase activity by modulating the transformation of dimeric and tetrameric forms of PKM2. Further analysis revealed that β‐elemene suppressed aerobic glycolysis by blocking PKM2 nuclear translocation and the expression of EGFR, GLUT1 and LDHA by influencing the expression of importin α5. Furthermore, the effect of β‐elemene on migration, invasion, PKM2 transformation, and nuclear translocation could be reversed in part by fructose‐1,6‐bisphosphate (FBP) and L‐cysteine. Taken together, tetrameric transformation and nuclear translocation of PKM2 are essential for cancer metastasis, and β‐elemene inhibited breast cancer metastasis via blocking aerobic glycolysis mediated by dimeric PKM2 transformation and nuclear translocation, being a promising anti‐metastatic agent from natural compounds.

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The reversal of antineoplastic drug resistance in cancer cells by β-elemene

Cited by 34 publications

References 63 publications

β-Elemene Inhibits Human Sperm Function by Affecting Sperm Vitality and Intracellular Calcium

β-Elemene Inhibits Human Sperm Function by Affecting Sperm Vitality and Intracellular Calcium

Cytotoxic Essential Oils from Eryngium campestre and Eryngium amethystinum (Apiaceae) Growing in Central Italy

Beta‐elemene inhibits breast cancer metastasis through blocking pyruvate kinase M2 dimerization and nuclear translocation

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