ArticleScientific reports2017
Targeting P-glycoprotein: Investigation of piperine analogs for overcoming drug resistance in cancer.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 57 papers, 1 of them a synthesis that pooled it.
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Who cites it
57 citing papers in PubMed, 1 synthesis or guideline pooled it, 119 citations in OpenAlex.
- A Systematic Review of the Anti-seizure and Antiepileptic Effects and Mechanisms of Piperine.Central nervous system agents in medicinal chemistry · 2025Pooled it
- Synthesis and Assessment of the Enantioselectivity in Antitumor Activity of a Library of Novel Chiral Flavone Derivatives.ChemMedChem · 2026Article
- Recent advances in piperine and its derivatives as potential anticancer agents.RSC medicinal chemistry · 2026Review
- Total Synthesis of Piperine and Derivatives: Antimicrobial and Cytotoxic Activities.ACS omega · 2026Article
- Adaptogenic and Neuroprotective Effects of the Thai Herbal Formula AYW-KK-04 Against Chronic Stress-Induced Cognitive Impairment.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Article
- Review
- Integrated molecular and ADME-toxicity profiling identifies PGV-5 and HGV-5 as potential agents to counteract multidrug-resistant (MDR) cancer.Scientific reports · 2025Article
- Therapeutic spectrum of Piperine in ischemic stroke: a literature review.Molecular biology reports · 2025Review
- Article
- Investigations on genomic, topological and structural properties of diguanylate cyclases involved inCurrent research in structural biology · 2025Article
- The Role of Elacridar, a P-gp Inhibitor, in the Re-Sensitization of PAC-Resistant Ovarian Cancer Cell Lines to Cytotoxic Drugs in 2D and 3D Cell Culture Models.International journal of molecular sciences · 2025Article
- Efficient Synthesis of Mannopyranoside-based Fatty Acyl Esters: Effects of Acyl Groups on Antimicrobial Potential.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Article
- Post-genomic illumination of paclitaxel biosynthesis.Nature plants · 2024Review
- Modulation of Multidrug Resistance Transporters by Food Components and Dietary Supplements: Implications for Cancer Therapy Efficacy and Safety.Current issues in molecular biology · 2024Review
- Amorphous Polymer-Phospholipid Solid Dispersions for the Co-Delivery of Curcumin and Piperine Prepared via Hot-Melt Extrusion.Pharmaceutics · 2024Article
- Marine Prostanoids with Cytotoxic Activity from OctocoralMarine drugs · 2024Article
- Sorafenib and Piperine co-loaded PLGA nanoparticles: Development, characterization, and anti-cancer activity against hepatocellular carcinoma cell line.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Article
- Evaluation of Antitumor Activity of Xanthones Conjugated with Amino Acids.International journal of molecular sciences · 2024Article
- Ethosomes for Curcumin and Piperine Cutaneous Delivery to Prevent Environmental-Stressor-Induced Skin Damage.Antioxidants (Basel, Switzerland) · 2024Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
P-glycoprotein (P-gp) is a drug transporter that effluxes chemotherapeutic drugs and is implicated in the development of resistance of cancer cells to chemotherapeutic drugs. To date, no drug has been approved to inhibit P-gp and restore chemotherapy efficacy. Moreover, majority of the reported inhibitors have high molecular weight and complex structures, making it difficult to understand the basic structural requirement for P-gp inhibition. In this study, two structurally simple, low molecular weight piperine analogs Pip1 and Pip2 were designed and found to better interact with P-gp than piperine in silico. A one step, acid-amine coupling reaction between piperic acid and 6,7-dimethoxytetrahydroisoquinoline or 2-(3,4-dimethoxyphenyl)ethylamine afforded Pip1 and Pip2, respectively. In vitro testing in drug resistant P-gp overexpressing KB (cervical) and SW480 (colon) cancer cells showed that both analogs, when co-administered with vincristine, colchicine or paclitaxel were able to reverse the resistance. Moreover, accumulation of P-gp substrate (rhodamine 123) in the resistant cells, a result of alteration of the P-gp efflux, was also observed. These investigations suggest that the natural product analog - Pip1 ((2E,4E)-5-(benzo[d][1,3]dioxol-5-yl)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1 H)-yl)penta-2,4-dien-1-one) - is superior to piperine and could inhibit P-gp function. Further studies are required to explore the full potential of Pip1 in treating drug resistant cancer.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.