Targeting hepatocellular carcinoma with piperine by radical-mediated mitochondrial pathway of apoptosis: An in vitro and in vivo study

Gunasekaran, Vetrichelvi; Elangovan, Kannan; Devaraj, S. Niranjali

doi:10.1016/j.fct.2017.03.029

Cited by 59 publications

(33 citation statements)

References 42 publications

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“…Ginger is traditionally used in tea and as "trikatu" as a therapeutic decoction to improve the immunity, metal detoxification, digestion, and fight against the cold inflammation in Indian continent [56][57][58][59][60]. High doses of antioxidants have been shown to inhibit the growth of different rodent and human cancer cells in vivo and in vitro [61][62][63][64][65]. Dose-dependent effect of antioxidant (prooxidant and antioxidant theory) of the known "antioxidants" on normal and cancer cell is still not well established [66].…”

Section: Discussionmentioning

confidence: 99%

Correlation of Antioxidant and Antiproliferative Activity of Amla and Ginger

Kulsum¹,

Suresh²,

Mehta

2018

Asian J Pharm Clin Res

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Objective: Our study focused on evaluating the anticancer property of ascorbic acid and aqueous extract of amla and ginger.Methods: Antioxidant capacity of ascorbic acid, aqueous extract of amla, and ginger was obtained by 2,2-diphenyl-1-picrylhydrazyl method and total antioxidant capacity (TAC). Vero cell line, PA-1, Cal-27, Cal-27 CisR, and DysMSCTR16 cell lines were treated with antioxidants to evaluate its antiproliferative property using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Colony and spheroid formation assays were also carried out in the presence of extracts to assess its role in anticancer stem cell activity.Results: Two volumes of amla 5 µl (~0.016 g) and 25 µl (~0.08 g) and ginger 5 µl (~0.02 g) and 25 µl (~0.1 g) showed TAC activity equivalent to 0.25 mM and 2 mM ascorbic acid, respectively. Amla and ascorbic acid showed significant antiproliferative property in normal (Vero) p=0.05, cancer (PA-1, Cal-27) p=0.005, and resistant (Cal-27 CisR) p=0.05 cell lines and ginger extract in Vero and Cal-27 cell lines (p=0.05). In PA-1 and Cal-27 CisR cell line, ginger extract showed proliferative activity (p=0.005). Antioxidants showed no antiproliferative activity in DysMSCTR16 cells. Amla extract and ascorbic acid showed significant inhibitory effect on spheroid (p=0.005) and colony formation capacity (p=0.0005) among dysplastic, cancer, and resistant cell lines. Ginger showed inhibitory effect (p=0.05) only in colony formation capacity. Conclusion:Overall, we found a strong correlation between antioxidant and antiproliferative activity of ascorbic acid, amla, and ginger. Amla and ascorbic acid proved to be effective in controlling cell proliferation and self-renewal properties of cancer cells. However, ginger was found to have selective and less antiproliferative effect in comparison to amla.

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Section: Discussionmentioning

confidence: 99%

Correlation of Antioxidant and Antiproliferative Activity of Amla and Ginger

Kulsum¹,

Suresh²,

Mehta

2018

Asian J Pharm Clin Res

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“…We added 0.01% w/v sodium azide to the release media as a preservative. At 6,8,12,24,48, and 72 h, a 2 mL aliquot was withdrawn, filtered through a 0.45-mm Millipore filter, and measured at 342 ± 0.05 nm against the blank cuvette. We maintained sink conditions by adding an equal volume of fresh buffer with each sampling.…”

Section: In Vitro Drug Releasementioning

confidence: 99%

“…At the pharmacological level, Pip improves the bioavailability of drugs, either synthetic or natural, when combined [13,14], and has anti-inflammatory [15], neuroprotective [16], and anti-oxidant effects [17]. Anti-tumor effects have been reported in several cancers both in vitro and in vivo, including melanoma, breast, ovarian, colon, lung, liver, and prostate [18][19][20][21][22][23][24]. Despite these fascinating properties, Pip has not yet been used clinically due to its inherent limitations in regards to solubility, site-specific targeting, and bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

et al. 2020

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Targeted drug delivery offers great opportunities for treating cancer. Here, we developed a novel anticancer targeted delivery system for piperine (Pip), an alkaloid prodrug derived from black pepper that exhibits anticancer effects. The tailored delivery system comprises aggregated hydroxyapatite nanoparticles (HAPs) functionalized with phosphonate groups (HAP-Ps). Pip was loaded into HAPs and HAP-Ps at pH 7.2 and 9.3 to obtain nanoformulations. The nanoformulations were characterized using several techniques and the release kinetics and anticancer effects investigated in vitro. The Pip loading capacity was >20%. Prolonged release was observed with kinetics dependent on pH, surface modification, and coating. The nanoformulations fully inhibited monolayer HCT116 colon cancer cells compared to Caco2 colon cancer and MCF7 breast cancer cells after 72 h, whereas free Pip had a weaker effect. The nanoformulations inhibited ~60% in HCT116 spheroids compared to free Pip. The Pip-loaded nanoparticles were also coated with gum Arabic and functionalized with folic acid as a targeting ligand. These functionalized nanoformulations had the lowest cytotoxicity towards normal WI-38 fibroblast cells. These preliminary findings suggest that the targeted delivery system comprising HAP aggregates loaded with Pip, coated with gum Arabic, and functionalized with folic acid are a potentially efficient agent against colon cancer.

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“…Furthermore, it has well-characterized anti-inflammatory (10) and antitumor effects in numerous types of cancer, including breast, lung and liver cancer, and lymphoma (11)(12)(13)(14). Piperine has been reported to dose-dependently (15)(16)(17)(18)(19)(20) regulate cell growth and differentiation via the Akt/JNK/MAPK pathway (21), and can increase cytokine production via the mTOR signaling pathway (22).…”

Section: Introductionmentioning

confidence: 99%

Wnt/β‑catenin signaling modulates piperine‑mediated antitumor effects on human osteosarcoma cells

Yang

et al. 2020

Mol Med Report

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The plant extract piperine is used as a traditional Chinese medicine due to its anti-inflammatory effects and efficacy against numerous types of cancer. The aim of the present study was to investigate the antitumor mechanism of piperine in human osteosarcoma U2OS and 143B cell lines. The effects of piperine on cell apoptosis and invasion of human osteosarcoma cells were assessed using flow cytometry and Transwell assays. Moreover, western blotting was used to measure the effects of piperine on the protein expression levels of the metastasis markers matrix metalloproteinase-2 (MMP-2) and vascular endothelial growth factor (VEGF). In addition, the involvement of the Wnt/β-catenin signaling pathway in modulating the effects of piperine was examined via western blot analysis. The results of MTT and Transwell invasion assays indicated that piperine treatment dose-dependently reduced U2OS and 143B cell viability and invasion. Furthermore, a significant reduction was identified in MMP-2, VEGF, glycogen synthase kinase-3β and β-catenin protein expression levels, as well as the expression levels of their target proteins cyclooxygenase-2, cyclin D1 and c-myc, in U2OS cells after piperine treatment. In addition, similar results were observed in 143B cells. Therefore, the present study demonstrated the efficacy of piperine in osteosarcoma, and identified that the Wnt/β-catenin signaling pathway may modulate the antitumor effects of piperine on human U2OS and 143B cells.

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Targeting hepatocellular carcinoma with piperine by radical-mediated mitochondrial pathway of apoptosis: An in vitro and in vivo study

Cited by 59 publications

References 42 publications

Correlation of Antioxidant and Antiproliferative Activity of Amla and Ginger

Correlation of Antioxidant and Antiproliferative Activity of Amla and Ginger

Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

Wnt/β‑catenin signaling modulates piperine‑mediated antitumor effects on human osteosarcoma cells

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