Piperlongumine inhibits migration and proliferation of castration-resistant prostate cancer cells via triggering persistent DNA damage

Zhang, Ding-fang; Yang, Zhi-Chun; Chen, Jianqiang; Jin, Xiangxiang; Qiu, Yinda; Chen, Xiaojing; Shi, Hongyi Adrian; Liu, Zhiguo; Wang, Minshan; Liang, Guang; Zheng, Xiaohui

doi:10.1186/s12906-021-03369-0

Cited by 16 publications

(5 citation statements)

References 40 publications

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“…In their study, Zhang et al [ 82 ] explored the anticancer activity and mechanisms of action of PL against CRPC in terms of DNA damage and repair processes and demonstrated that PL has an IC 50 of 6.75, 8.42, 8.73, and 68.62 μM in PC3 cells, DU145 cells (cells that are derived from bone and brain metastasis of CRPC), WPMY-1 cells, and LO2 cells. The results showed that PL exhibits anticancer activity in a dose-dependent manner (1, 2, and 4 μM) and is stronger against CRPC cells compared to taxol, cisplatin (DDP), doxorubicin (Dox), or 5-fluorouracil (5-FU), with fewer side effects in normal cells.…”

Section: Resultsmentioning

confidence: 99%

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The Antitumor Activity of Piplartine: A Review

Duarte,

Gomes,

Nunes

et al. 2023

Pharmaceuticals

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Cancer is a worldwide health problem with high mortality in children and adults, making searching for novel bioactive compounds with potential use in cancer treatment essential. Piplartine, also known as piperlongumine, is an alkamide isolated from Piper longum Linn, with relevant therapeutic potential. Therefore, this review covered research on the antitumor activity of piplartine, and the studies reported herein confirm the antitumor properties of piplartine and highlight its possible application as an anticancer agent against various types of tumors. The evidence found serves as a reference for advancing mechanistic research on this metabolite and preparing synthetic derivatives or analogs with better antitumor activity in order to develop new drug candidates.

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Section: Resultsmentioning

confidence: 99%

“…Furthermore, PL treatment (1, 2, and 4 μM) induced apoptosis in DU145 cells, with a concomitant increase in p53 expression. Finally, PL treatment triggered persistent DNA damage and caused strong DNA damage responses in CRPC cells [ 82 ].…”

Section: Resultsmentioning

confidence: 99%

The Antitumor Activity of Piplartine: A Review

Duarte,

Gomes,

Nunes

et al. 2023

Pharmaceuticals

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“…In a previous study on lung cancer cells (A549 and NCI-H460) treated with 20 µ m PL for 24 h, DAPI staining revealed an increase in apoptotic bodies, demonstrating that PL induces apoptosis in lung cancer cells ( 40 ). Similarly, in PL (1, 2, and 4 µ m)-treated DU145 prostate cancer cells, Annexin V-PI staining reveals a dose-dependent increase in apoptosis ( 41 ). The aforementioned studies support the present findings that PL induced apoptosis in melanoma cells.…”

Section: Discussionmentioning

confidence: 98%

Piperlongumine induces apoptosis via the MAPK pathway and ERK‑mediated autophagy in human melanoma cells

Jeon,

Choi,

Han

et al. 2023

Int J Mol Med

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Piperlongumine (PL) is an amide alkaloid with diverse pharmacological effects against cancer, bronchitis and asthma; however, research on its efficacy against melanoma is lacking. The present study investigated the anticancer effects of PL on A375SM and A375P human melanoma cells. PL decreased the survival rate of A375SM and A375P cells, as shown by MTT assay, increase of apoptotic cells by DAPI staining. And PL induced apoptosis by decreasing the expression of the anti-apoptotic protein Bcl-2 and increasing that of the pro-apoptotic proteins cleaved-PARP and Bax. PL also induced apoptosis in A375SM and A375P cells via the MAPK pathway, increasing expression of the MAPK pathway proteins, phosphorylated-(p-ERK), p-JNK p-p38. These proteins were confirmed by western blot. In addition, A375SM and A375P cells treated with PL showed an increased number of acidic vesicular organelles by acridine orange staining. Also, autophagy induced by the expression of 1A/1B-light chain 3, Beclin 1and mTOR was investigated through western blot. When PL was applied following treatment with autophagy inhibitors 3-methyladenine and hydroxychloroquine, autophagy exhibited a cytoprotective effect against apoptosis in MTT assay. Pretreatment of A375P cells with the ERK inhibitor PD98059 and the JNK inhibitor SP600125 followed by treatment with PL confirmed that apoptosis and autophagy were mediated via the MAPK/ERK pathway by western blot. In summary, the present study provided empirical evidence supporting the anticancer effects of PL on human melanoma cells and indicated the potential of PL as a treatment for melanoma.

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“…In addition, piperlongumine was found to exhibit promise anti-cancer activities in various cancers. In castration-resistant prostate cancer cells, DNA could be damaged persistently by piperlongumine treatment to inhibit proliferation, migration, and invasion of prostate cancer cells [ 239 ]. Apoptosis and cell cycle arrest can also be induced by piperlongumine in gastric, cervical, and colorectal cancer cells [ 240 ].…”

Section: Phytochemicals Targeting Ros and Autophagy For Cancer Therapymentioning

confidence: 99%

Targeting the Interplay of Autophagy and ROS for Cancer Therapy: An Updated Overview on Phytochemicals

Dong

Luo

et al. 2023

Pharmaceuticals

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Autophagy is an evolutionarily conserved self-degradation system that recycles cellular components and damaged organelles, which is critical for the maintenance of cellular homeostasis. Intracellular reactive oxygen species (ROS) are short-lived molecules containing unpaired electrons that are formed by the partial reduction of molecular oxygen. It is widely known that autophagy and ROS can regulate each other to influence the progression of cancer. Recently, due to the wide potent anti-cancer effects with minimal side effects, phytochemicals, especially those that can modulate ROS and autophagy, have attracted great interest of researchers. In this review, we afford an overview of the complex regulatory relationship between autophagy and ROS in cancer, with an emphasis on phytochemicals that regulate ROS and autophagy for cancer therapy. We also discuss the effects of ROS/autophagy inhibitors on the anti-cancer effects of phytochemicals, and the challenges associated with harnessing the regulation potential on ROS and autophagy of phytochemicals for cancer therapy.

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Piperlongumine inhibits migration and proliferation of castration-resistant prostate cancer cells via triggering persistent DNA damage

Cited by 16 publications

References 40 publications

The Antitumor Activity of Piplartine: A Review

The Antitumor Activity of Piplartine: A Review

Piperlongumine induces apoptosis via the MAPK pathway and ERK‑mediated autophagy in human melanoma cells

Targeting the Interplay of Autophagy and ROS for Cancer Therapy: An Updated Overview on Phytochemicals

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