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The novel Piperine derivative YL-1-9 exhibits anti-breast Cancer effects by inducing apoptosis via the p53/p21
Chongyun Zhou1, Jiayun Wang1, Lili Zhou1
1Jiangsu Key Laboratory for Screening of Marine Pharmaceutical Active Molecules, School of Pharmacy, Jiangsu Ocean University, Lianyungang 222000, PR China.
Abstract:
The tumor suppressor protein p53 plays a crucial role in the pathogenesis of breast cancer; however, its function is often compromised due to MDM2 overexpression or mutations in the p53 gene, which occurs in approximately 30-35 % of breast cancer cases. Piperine, a natural bioactive compound, has shown potential in inhibiting breast cancer cell growth by upregulating p53 expression. However, its clinical application is hindered by poor bioavailability, potential toxicity, and the risk of undesirable drug interactions. In the present study, a novel derivative of Piperine, YL-1-9, was synthesized and evaluated for its anticancer activity against breast cancer. YL-1-9, a bicyclic amide derivative of Piperine, was evaluated for antitumor effects both in vitro and in vivo using MTT assays and the chick embryo chorioallantoic membrane (CAM) model. Further investigations into its effects on breast cancer cell clonogenicity, adhesion, invasion, and migration were conducted through colony formation assays, EdU assays, cell adhesion and invasion studies, and wound healing experiments. Western blot analysis was performed to elucidate the effects of YL-1-9 on the cell cycle and apoptosis, which were further validated using YO-PRO-1 and propidium iodide dual staining. YL-1-9 significantly inhibited breast cancer cell proliferation, adhesion, invasion, and migration, while inducing cell cycle arrest and promoting apoptosis. Mechanistically, YL-1-9 downregulated critical proteins in the CDK4/6-cyclin D-Rb-E2F pathway and the Caspase 3/Bax/Bcl-2 apoptosis signaling pathway. These findings position YL-1-9 as a promising candidate for breast cancer therapy; however, further clinical studies are necessary to fully assess its therapeutic potential.
Insights
A new Piperine derivative, YL-1-9, shows significant anticancer effects against breast cancer by inhibiting cell growth, migration, and inducing apoptosis. This compound offers a promising therapeutic avenue, pending further clinical evaluation.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Breast cancer pathogenesis involves the tumor suppressor protein p53, often compromised by MDM2 overexpression or p53 gene mutations in 30-35% of cases.
- Piperine, a natural compound, inhibits breast cancer growth by upregulating p53, but faces clinical limitations due to poor bioavailability and potential toxicity.
- A novel Piperine derivative, YL-1-9, was synthesized to overcome these limitations and enhance anticancer activity.
Purpose of the Study:
- To evaluate the in vitro and in vivo anticancer activity of the novel Piperine derivative, YL-1-9, against breast cancer.
- To investigate the effects of YL-1-9 on key breast cancer cell behaviors including proliferation, clonogenicity, adhesion, invasion, and migration.
- To elucidate the molecular mechanisms underlying YL-1-9's anticancer effects, focusing on cell cycle regulation and apoptosis signaling pathways.
Main Methods:
- In vitro and in vivo antitumor effects were assessed using MTT assays and the chick embryo chorioallantoic membrane (CAM) model.
- Cellular effects were evaluated through colony formation, EdU, cell adhesion, invasion, and wound healing assays.
- Western blot analysis, YO-PRO-1, and propidium iodide staining were used to determine effects on cell cycle and apoptosis.
Main Results:
- YL-1-9 significantly inhibited breast cancer cell proliferation, adhesion, invasion, and migration.
- The compound induced cell cycle arrest and promoted apoptosis in breast cancer cells.
- Mechanistically, YL-1-9 downregulated key proteins in the CDK4/6-cyclin D-Rb-E2F and Caspase 3/Bax/Bcl-2 signaling pathways.
Conclusions:
- YL-1-9 demonstrates potent anticancer activity against breast cancer, targeting proliferation, metastasis, and apoptosis.
- The compound's mechanism involves modulation of cell cycle and apoptosis regulatory proteins.
- YL-1-9 represents a promising therapeutic candidate for breast cancer, warranting further clinical investigation.
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