3,3'-Diindolylmethane inhibits patient-derived xenograft colon tumor growth by targeting COX1/2 and ERK1/2

Tian, Xueli; Liu, Kang Dong; Zu, Xueyin; Ma, Fayang; Li, Zhi; Lee, Mee-Hyun; Chen, Hanyong; Li, Yan; Zhao, Yuzhou; Liu, Fangfang; Oi, Naomi; Bode, Ann M.; Dong, Zigang; Kim, Dong Joon

doi:10.1016/j.canlet.2019.01.031

Cited by 34 publications

(26 citation statements)

References 46 publications

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“…All animal experiments complied with ethical regulations and were approved by the Laboratory Animal Center of Fujian Medical University (Tian et al, 2019).…”

Section: Immunohistochemistrymentioning

confidence: 99%

Ethyl Acetate Extract of Selaginella doederleinii Hieron Induces Cell Autophagic Death and Apoptosis in Colorectal Cancer via PI3K-Akt-mTOR and AMPKα-Signaling Pathways

Wang

et al. 2020

Front. Pharmacol.

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Colorectal cancer is one type of cancer with high incidence rate and high mortality worldwide. Thus, developing new chemotherapeutic drugs is important. The Selaginella doederleinii Hieron ethyl acetate (SDEA) extract showed good anti-colon cancer effect in vitro and in vivo, but its mechanism is unclear. This study aimed to further reveal the anticolon cancer effect of SDEA and its possible mechanism. The effects on cell viability, apoptosis, autophagy, and cell cycle in colorectal cells (HT29 and HCT116) were studied using MTT assay, fluorescence microscopy, transmission electron microscopy, and flow cytometry. The mechanisms were further studied using cell transfection, Western blot, and real-time quantitative polymerase chain reaction assay. The effect of xenotransplantation in vivo was observed using immunohistochemistry. Results showed that SDEA inhibited cell proliferation and induced cell morphological changes, cell cycle arrest, autophagy, and apoptosis. It also induced loss of mitochondrial membrane potential, increased the autophagic flux, raised the ratio of Bax/Bcl-2, activated caspases, and inhibited PI3K-Akt-mTOR signaling pathways. Furthermore, SDEA inhibited the growth of xenograft tumors in a dose-dependent manner. Immunohistochemistry analysis confirmed the alteration of autophagy-and apoptosisrelated proteins and immunohistochemical microvascular density in xenografts, which were consistent with the results in vitro. Therefore, SDEA is important for developing candidate drugs against colorectal cancers.

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“…All animal experiments complied with ethical regulations and were approved by the Laboratory Animal Center of Fujian Medical University (Tian et al, 2019).…”

Section: Immunohistochemistrymentioning

confidence: 99%

Ethyl Acetate Extract of Selaginella doederleinii Hieron Induces Cell Autophagic Death and Apoptosis in Colorectal Cancer via PI3K-Akt-mTOR and AMPKα-Signaling Pathways

Wang

et al. 2020

Front. Pharmacol.

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“…DIM competitively binds the ERK docking site and inhibits cell proliferation. [62] Qiu et al (2020) have used commercially available neutral salt CF 3 SO 2 Na to synthesize DIM. CF 3 SO 2 Na generates ⋅CF 3 insitu under ultraviolet irradiation and an oxygen atmosphere.…”

Section: Anticancer Activity Of Dim In Various Cancer Cell Lines (201mentioning

confidence: 99%

“…In other mechanisms, D‐domains of phosphorylated ribosomal s6 kinase (RSK) bind with the ERK‐CD domain to mediate apoptosis. DIM competitively binds the ERK docking site and inhibits cell proliferation …”

Section: Introductionmentioning

confidence: 99%

Anticancer Activity of 3,3′‐Diindolylmethane and the Molecular Mechanism Involved in Various Cancer Cell Lines

Koli

Reena²,

Indurthi

et al. 2020

ChemistrySelect

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Indole-3-carbinol is a natural compound present in cruciferous plants, which upon digestion, converts into 3,3'-diindolylmethane (DIM) under acidic pH of the stomach. In recent years, various methods have been developed to improve the synthesis of DIM and its analogs because of different pharmacological activities like anticancer, antimicrobial, anti-inflammatory, etc. Among them, DIMs anticancer activity by modulation of protein expression in cell signaling pathways and other factors has widely studied. This review describes the antiproli-ferative activity of DIMs and its mode of action, which resulted in apoptosis in various cancerous cells. We have performed a literature search on DIMs anticancer activity over the last ten years (2011-2020) and reported in this review. Several fascinating DIM attributes against cancer suggest it as a potential candidate for further drug development programs. This review will guide the medicinal chemist to find the mechanistic pathways involved in the inhibition of proliferation in cancerous cells by novel DIMs.

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“…[13,14] 3,3′-Diindolylmethane (DIM, 1; Figure 2), found in broccoli and cabbage, demonstrated potential anticancer activity by influencing cell proliferation, cell cycle, and apoptosis through the mediation of various signaling molecules in several types of cancers without causing unwanted toxicity in normal cells. [15][16][17][18][19][20][21] DIM not only exhibited remarkable inhibition of acute lymphoblastic leukemia, breast, colon, and prostate xenograft tumor growth without causing severe toxicity in mice models, but also showed potential activity in clinical evaluations against human breast, prostate, and ovarian cancer, and vulvar intraepithelial neoplasia either alone or in combination with other anticancer agents. [22][23][24][25][26][27] Thus, DIM is a useful pharmacophore for the development of novel anticancer agents.…”

Section: Bisindole Alkaloidsmentioning

confidence: 99%

Anticancer activity of bisindole alkaloids derived from natural sources and synthetic bisindole hybrids

Zhang

2020

Archiv der Pharmazie

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The bisindole moiety, as a versatile pharmacophore, is one of the widespread heterocycles in naturally occurring and synthetic bioactive compounds. The bisindole alkaloids derived from natural sources possess structural and mechanistic diversity, and they were found to be generally more active than monoindole alkaloids against various cancer cell lines. Moreover, some bisindole alkaloids such as the tubulin inhibitors, vinorelbine and vinblastine, have already been approved for cancer therapy, suggesting that bisindole alkaloids are a significant source of anticancer agents and lead hits. Bisindole hybrids have the potential to overcome drug resistance, enhance efficiency, and reduce severe side effects. The bisindole–lactam hybrid midostaurin has already been approved for the treatment of adult patients with newly diagnosed acute myeloid leukemia who are FLT3 mutation‐positive, highlighting the importance of bisindole hybrids in the development of novel anticancer agents. In this review, we present a brief account of the bisindole alkaloids derived from nature and of synthetic hybrids with potential anticancer activity developed in the recent 10 years.

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3,3'-Diindolylmethane inhibits patient-derived xenograft colon tumor growth by targeting COX1/2 and ERK1/2

Cited by 34 publications

References 46 publications

Ethyl Acetate Extract of Selaginella doederleinii Hieron Induces Cell Autophagic Death and Apoptosis in Colorectal Cancer via PI3K-Akt-mTOR and AMPKα-Signaling Pathways

Ethyl Acetate Extract of Selaginella doederleinii Hieron Induces Cell Autophagic Death and Apoptosis in Colorectal Cancer via PI3K-Akt-mTOR and AMPKα-Signaling Pathways

Anticancer Activity of 3,3′‐Diindolylmethane and the Molecular Mechanism Involved in Various Cancer Cell Lines

Anticancer activity of bisindole alkaloids derived from natural sources and synthetic bisindole hybrids

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