CDKN2A-p53 mediated antitumor effect of Lupeol in head and neck cancer

Bhattacharyya, Sayantan; Sekar, Vasanthakumar; Majumder, Biswanath; Mehrotra, Debapriya G.; Banerjee, Samir; Bhowmick, Anup Kumar; Alam, Neyaz; Mandal, Gautam; Biswas, Jaydip; Majumder, Pradip K.; Murmu, Nabendu

doi:10.1007/s13402-016-0311-7

Cited by 40 publications

(23 citation statements)

References 56 publications

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“…This is an indication that lupeol is absorbed, metabolized and finally distributed in the tissues in which it can exert its beneficial effects. Several studies have shown that lupeol supplementation is able to reduce damage to organs such as kidneys (Sudhahar et al, ) and liver (Kim et al, ); to show anti‐inflammatory activities against inflammation‐related molecules such as cytokines involved in systemic inflammation such as tumor necrosis factor‐ α , interleukin‐1 β , interleukin‐2, interleukin‐4, interleukin‐6, interferon‐ γ or derivatives of arachidonic acid such as prostaglandin E2 (Siddique & Saleem, , and references therein), and anti‐cancer effects such as anti‐topoisomerase 2 (Sánchez‐Burgos et al, ); to down‐regulate pathways related to cancer development such as AKT/ERK (Liu et al, ); and to enhance expression of p53 and phase G1 cell cycle arrest (Bhattacharyya et al, ). Furthermore, lupeol shows few toxic effects associated with its consumption (Saleem, ), making it a good candidate for its potential use as a therapeutic agent.…”

Section: Discussionmentioning

confidence: 99%

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI⁺–MS/MS

Cháirez-Ramírez

Gallegos‐Infante

Moreno‐Jiménez

et al. 2018

Biomedical Chromatography

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Lupeol is a dietary triterpene that shows limited water solubility, which affects its bioavailability. It is well known that poor oral bioavailability is one of the major causes of therapeutic variability. Lupeol has been reported to have multiple biological activities;however, there are no reports about its bioavailability. Therefore, the objective of this research was to evaluate the systemic bioavailability of lupeol. An experimental strategy with three groups of female CD-1 strain mice was proposed (control, olive oil and lupeol in olive oil), at six experimental times (0.5, 2, 4, 8, 12 and 24 h) with four animals per experimental point. Mice were sacrificed for organs, urine, feces and blood collection. Lupeol was extracted from samples and analyzed by UPLC-APCI + -MS/ MS, obtaining the pharmacokinetics parameters time to peak concentration 6.444 ± 0.851 h and peak concentration 8.071 ± 2.930 μg/mL. Study of direct digestion and absorption in various organs showed important concentrations of lupeol at earlier post-administration times (stomach, 137.25 ± 19.94 ng/mg and small intestine, 99.00 ± 12.99 ng/mg). The main excretion route was fecal, with a peak at 12 h postadministration (163.28 ± 9.83 μg/mg). Absorption of lupeol by the animals was better than expected despite its nonpolar nature (extent of absorption F = 0.645 ± 0.0581).

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Section: Discussionmentioning

confidence: 99%

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI⁺–MS/MS

Cháirez-Ramírez

Gallegos‐Infante

Moreno‐Jiménez

et al. 2018

Biomedical Chromatography

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“…75,76 They have used this platform with head and neck squamous cell carcinomas (HNSCC) and colorectal carcinomas (CRC) and evaluated responses to cytotoxic and targeted therapies by immunohistochemical assessment of cell death or proliferation biomarkers as well as pharmacodynamic biomarkers. 77,78 Strong correlations between CANScript responses to cytotoxic drug regimens of docetaxel, cisplatin and 5fluorouracil (TPF) and the responses of PDX models derived from the same human tumour samples to the same chemotherapies were observed. Furthermore, following stratification of HNSCCs for KRAS mutation status, correlations between the CANScript and PDX responses were observed upon treatment with the epidermal growth factor receptor (EGFR) inhibitor cetuximab.…”

Section: Recent Advances In Pde-based Platformsmentioning

confidence: 99%

Patient-derived explants (PDEs) as a powerful preclinical platform for anti-cancer drug and biomarker discovery

et al. 2020

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Preclinical models that can accurately predict outcomes in the clinic are much sought after in the field of cancer drug discovery and development. Existing models such as organoids and patient-derived xenografts have many advantages, but they suffer from the drawback of not contextually preserving human tumour architecture. This is a particular problem for the preclinical testing of immunotherapies, as these agents require an intact tumour human-specific microenvironment for them to be effective. In this review, we explore the potential of patient-derived explants (PDEs) for fulfilling this need. PDEs involve the ex vivo culture of fragments of freshly resected human tumours that retain the histological features of original tumours. PDE methodology for anti-cancer drug testing has been in existence for many years, but the platform has not been widely adopted in translational research facilities, despite strong evidence for its clinical predictivity. By modifying PDE endpoint analysis to include the spatial profiling of key biomarkers by using multispectral imaging, we argue that PDEs offer many advantages, including the ability to correlate drug responses with tumour pathology, tumour heterogeneity and changes in the tumour microenvironment. As such, PDEs are a powerful model of choice for cancer drug and biomarker discovery programmes.

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“…head and neck, colorectal, prostate, pancreatic, and cervical cancer (Liu et al, 2015;Bhattacharyya et al, 2017;Emanuele et al, 2018;Wang et al, 2018b) inhibiting metastasis BCL2, CLAUDIN1, MMP2/9, MTCO2, NFKB, RELA, TP53…”

Section: Phenolic Acidsmentioning

confidence: 99%

Mapping Pharmacological Network of Multi-Targeting Litchi Ingredients in Cancer Therapeutics

Cao

Han

et al. 2020

Front. Pharmacol.

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Considerable pharmacological studies have demonstrated that the extracts and ingredients from different parts (seeds, peels, pulps, and flowers) of Litchi exhibited anticancer effects by affecting the proliferation, apoptosis, autophagy, metastasis, chemotherapy and radiotherapy sensitivity, stemness, metabolism, angiogenesis, and immunity via multiple targeting. However, there is no systematical analysis on the interaction network of "multiple ingredients-multiple targets-multiple pathways" anticancer effects of Litchi. In this study, we summarized the confirmed anticancer ingredients and molecular targets of Litchi based on published articles and applied network pharmacology approach to explore the complex mechanisms underlying these effects from a perspective of system biology. The top ingredients, top targets, and top pathways of each anticancer function were identified using network pharmacology approach. Further intersecting analyses showed that Epigallocatechin gallate (EGCG), Gallic acid, Kaempferol, Luteolin, and Betulinic acid were the top ingredients which might be the key ingredients exerting anticancer function of Litchi, while BAX, BCL2, CASP3, and AKT1 were the top targets which might be the main targets underling the anticancer mechanisms of these top ingredients. These results provided references for further understanding and exploration of Litchi as therapeutics in cancer as well as the application of "Component Formula" based on Litchi's effective ingredients.

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CDKN2A-p53 mediated antitumor effect of Lupeol in head and neck cancer

Abstract: Together, our data indicate that Lupeol may orchestrate a bifurcated regulation of neoplastic growth and apoptosis in head and neck cancers and may serve as a promising agent for the management of tumors that have progressed on a platinum-based treatment regimen.

Cited by 40 publications

References 56 publications

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI⁺–MS/MS

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI⁺–MS/MS

Patient-derived explants (PDEs) as a powerful preclinical platform for anti-cancer drug and biomarker discovery

Mapping Pharmacological Network of Multi-Targeting Litchi Ingredients in Cancer Therapeutics

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CDKN2A-p53 mediated antitumor effect of Lupeol in head and neck cancer

Abstract: Together, our data indicate that Lupeol may orchestrate a bifurcated regulation of neoplastic growth and apoptosis in head and neck cancers and may serve as a promising agent for the management of tumors that have progressed on a platinum-based treatment regimen.

Cited by 40 publications

References 56 publications

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI+–MS/MS

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI+–MS/MS

Patient-derived explants (PDEs) as a powerful preclinical platform for anti-cancer drug and biomarker discovery

Mapping Pharmacological Network of Multi-Targeting Litchi Ingredients in Cancer Therapeutics

Contact Info

Product

Resources

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Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI⁺–MS/MS

Absorption and distribution of lupeol in CD‐1 mice evaluated by UPLC–APCI⁺–MS/MS