β-Thujaplicin modulates estrogen receptor signaling and inhibits proliferation of human breast cancer cells

Ko, Jiwon; Bao, Cheng; Park, Hyun‐Chang; Kim, Minchae; Choi, Hae-Jin; Kim, Young Suk; Lee, Hong Jin

doi:10.1080/09168451.2015.1008978

Cited by 15 publications

(9 citation statements)

References 30 publications

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“…To validate our screening data,we performed second validation screening assay for the top candidates. Moreover, given the fact that HR occurs only in S and G2 phases of the cell cycle, HR levels are exquisitely sensitive to fluctuations in cell cycle progression, to demonstrate that β-thujaplicin’s HR inhibition effect is not due to the G1 or S arrest previously shown in other studies [33,38], we conducted the assays previously used in our own publication [22] to exclude cell cycle effects particularly the shift to G1 phase on HR repair by synchronizing cells using contact inhibition. As shown in Fig.…”

Section: Discussionmentioning

confidence: 79%

“…3A–C. We selected β-thujaplicin as our top candidate based on the marked suppression of HR of GFP, the existing literature reporting the biological activities and clinical usage safety of this potential candidate,and the most promising translational research potential [33–35]. …”

Section: Resultsmentioning

confidence: 99%

“…It exerts a wide variety of biologic activities, including antimicrobial, antioxidant, and antitumor activities [45]. Additionally, It has also been reported to regulate tumor growth and metastasis, β-thujaplicin’s antitumor effects have been investigated in a variety of cancer models, including models of melanoma,breast cancer,lung cancer,colon cancer,prostate cancer, and oral cancer [33–35,38,46,47]. Some studies have shown that β-thujaplicin can inhibit cancer cell proliferation by inducing the p53-independent DNA damage response, S or G1 cell cycle arrest [33,34,48].…”

Section: Discussionmentioning

confidence: 99%

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Natural product β-thujaplicin inhibits homologous recombination repair and sensitizes cancer cells to radiation therapy

et al. 2017

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Investigation of natural products is an attractive strategy to identify novel compounds for cancer prevention and treatment. Numerous studies have shown the efficacy and safety of natural products, and they have been widely used as alternative treatments for a wide range of illnesses, including cancers. However, it remains unknown whether natural products affect homologous recombination (HR)-mediated DNA repair and whether these compounds can be used as sensitizers with minimal toxicity to improve patients’ responses to radiation therapy, a mainstay of treatment for many human cancers. In this study, in order to systematically identify natural products with an inhibitory effect on HR repair, we developed a high-throughput image-based HR repair screening assay and screened a chemical library containing natural products. Among the most interesting of the candidate compounds identified from the screen was β-thujaplicin, a bioactive compound isolated from the heart wood of plants in the Cupressaceae family, can significantly inhibit HR repair. We further demonstrated that β-thujaplicin inhibits HR repair by reducing the recruitment of a key HR repair protein, Rad51, to DNA double-strand breaks. More importantly, our results showed that β-thujaplicin can radiosensitize cancer cells. Additionally, β-thujaplicin sensitizes cancer cells to PARP inhibitor in different cancer cell lines. Collectively, our findings for the first time identify natural compound β-thujaplicin, which has a good biosafety profile, as a novel HR repair inhibitor with great potential to be translated into clinical applications as a sensitizer to DNA-damage-inducing treatment such as radiation and PARP inhibitor. In addition, our study provides proof of the principle that our robust high-throughput functional HR repair assay can be used for a large-scale screening system to identify novel natural products that regulate DNA repair and cellular responses to DNA damage-inducing treatments such as radiation therapy.

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Section: Discussionmentioning

confidence: 79%

Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Natural product β-thujaplicin inhibits homologous recombination repair and sensitizes cancer cells to radiation therapy

et al. 2017

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“…Interestingly, β-thujaplicin down-regulated ERα expression, which led to cell growth inhibition. These results suggest that β-thujaplicin might be considered as a potent agent that regulates the hormone sensitive mammary tumorigenesis (Ko et al, 2015). …”

Section: Natural Xenoestrogensmentioning

confidence: 96%

Risks and benefits related to alimentary exposure to xenoestrogens

Paterni

Granchi

Minutolo

2017

Critical Reviews in Food Science and Nutrition

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Xenoestrogens are widely diffused in the environment and in food, thus a large portions of human population is worldwide exposed to them. Among alimentary xenoestrogens, phytoestrogens (PhyEs) are increasingly being consumed because of their potential health benefits, although there are also important risks associated to their ingestion. Furthermore, other xenoestrogens that may be present in food are represented by other chemicals possessing estrogenic activities, that are commonly defined as endocrine disrupting chemicals (EDCs). EDCs pose a serious health concern since they may cause a wide range of health problems, starting from pre-birth till adult lifelong exposure. We herein provide an overview of the main classes of xenoestrogens, which are classified on the basis of their origin, their structures and their occurrence in the food chain. Furthermore, their either beneficial or toxic effects on human health are discussed in this review.

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“…Furthermore, β-thujaplicin (hinokiol), one of the constituents of C . obtusa essential oil, was recently reported to suppress proliferation of breast cancer cells [ 15 ] and have anti-inflammatory effects in mice [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Effects of Essential Oil from Hinoki Cypress, Chamaecyparis obtusa, on Physiology and Behavior of Flies

Lee

Min

2015

PLoS ONE

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Phytoncides, which are volatile substances emitted from plants for protection against plant pathogens and insects, are known to have insecticidal, antimicrobial, and antifungal activities. In contrast to their negative effects on microorganisms and insects, phytoncides have been shown to have beneficial effects on human health. Essential oil from Hinoki cypress (Chamaecyparis obtusa) is mostly used in commercial products such as air purifiers. However, the physiological/behavioral impact of essential oil from C. obtusa on insects is not established. In this study, we tested the effects of essential oil extracted from C. obtusa on the physiologies and behaviors of Drosophila melanogaster and Musca domestica. Exposure to essential oil from C. obtusa decreased the lifespan, fecundity, locomotive activity, and developmental success rate of D. melanogaster. In addition, both fruit flies and house flies showed strong repellent behavioral responses to the essential oil, with duration times of about 5 hours at 70 μg/ml. These results suggest that essential oil from C. obtusa can be used as a ‘human-friendly’ alternative insect repellent.

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β-Thujaplicin modulates estrogen receptor signaling and inhibits proliferation of human breast cancer cells

Cited by 15 publications

References 30 publications

Natural product β-thujaplicin inhibits homologous recombination repair and sensitizes cancer cells to radiation therapy

Natural product β-thujaplicin inhibits homologous recombination repair and sensitizes cancer cells to radiation therapy

Risks and benefits related to alimentary exposure to xenoestrogens

Effects of Essential Oil from Hinoki Cypress, Chamaecyparis obtusa, on Physiology and Behavior of Flies

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