The chemotherapeutic effect of β-2-himachalen-6-ol in chemically induced skin tumorigenesis

Daaboul, Hamid Elia; Dagher, Carole; Taleb, Robin I.; Bodman‐Smith, Kikki; Shebaby, Wassim N.; El‐Sibai, Mirvat; Mroueh, Mohamad; Daher, Costantine F.

doi:10.1016/j.biopha.2018.04.027

Cited by 19 publications

(12 citation statements)

References 45 publications

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“…Oridonin, a natural tetracycline diterpenoid, isolated from Rabdosia rubescens, suppresses cell proliferation and increases G2/M cell cycle arrest via inhibiting PI3K-Akt pathway and upregulating p21 and p53 in cancer cells such as in esophageal cancer [82] and oral squamous cell carcinoma cells [83]. Deguelin treatment in human gastric cancer cells [84], β-2-himachalen-6-ol treatment of skin carcinogenesis mouse model [85], Valtrate treatment in human breast cancer cells [86] and Aloperine treatment in prostate cancer cells [87] reduce tumor growth and cell survival by inhibiting PI3K-Akt pathway and upregulating p21 expression. Chemicals that have been shown to induce p21 expression in cancer research are listed in Table 2.…”

Section: P21 As a Target In Cancer Treatmentmentioning

confidence: 99%

p21 in Cancer Research

Shamloo

Usluer

2019

Cancers

264

139

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p21 functions as a cell cycle inhibitor and anti-proliferative effector in normal cells, and is dysregulated in some cancers. Earlier observations on p21 knockout models emphasized the role of this protein in cell cycle arrest under the p53 transcription factor activity. Although tumor-suppressor function of p21 is the most studied aspect of this protein in cancer, the role of p21 in phenotypic plasticity and its oncogenic/anti-apoptotic function, depending on p21 subcellular localization and p53 status, have been under scrutiny recently. Basic science and translational studies use precision gene editing to manipulate p21 itself, and proteins that interact with it; these studies have led to regulatory/functional/drug sensitivity discoveries as well as therapeutic approaches in cancer field. In this review, we will focus on targeting p21 in cancer research and its potential in providing novel therapies.

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Section: P21 As a Target In Cancer Treatmentmentioning

confidence: 99%

p21 in Cancer Research

Shamloo

Usluer

2019

Cancers

264

139

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“…Moreover, it has been reported that the antitumor activity of these compounds was associated with the induction of apoptosis through caspase-3 activation and the inhibition of DNA. [15][16][17][18] Meanwhile, the literature survey revealed that semicarbazone and thiosemicarbazone derivatives have demonstrated great promise in pharmacological and industrial chemistry. [19] Also, they have been widely used as useful intermediates to produce heterocyclic compounds (such as thiazoles and 4-thiazolidinones) and as ligands in metal-complexes synthesis because of their excellent chemical properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Thiazole Analogs with Both Anti‐Proliferative and Mechanistic Analyses and Molecular Docking Studies

et al. 2022

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Herein, we report the synthesis of a novel series of βhimachalene derivatives, including semicarbazones, thiosemicarbazones, and thiazoles. The structures of these compounds were elucidated by NMR, IR, and HRMS analysis methods. The in vitro antitumor activity of these compounds was evaluated by the MTT assay against four human cancer cell lines, such as fibrosarcoma (HT-1080), breast adenocarcinoma (MCF-7 and MDA-MB-231), and lung carcinoma (A-549), and the results indicated that all compounds showed moderate to significant cytotoxic activities against all cancer cell lines with IC 50 values ranging from 7.19 � 0.30 to 50 μM. The mechanism of action of the most cytotoxic compounds 2 b and 7 b suggested that they induced apoptosis through caspase-3/7 activation, and elicited G2/M-phase arrest with the loss of mitochondrial membrane potential in HT-1080 cells. The molecular docking showed that compounds 2 b and 7 b activated the caspase-3 by forming a stable protein-ligand complex.

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“…More recently, β‐2‐himachalen‐6‐ol ((Figure 1): A‐1) and 2‐himachelen‐7‐ol ((Figure 1): A‐2) showed promising cytotoxic activity against B16‐F‐10, Caco‐2, MB‐MDA‐231 and A‐549 cells. In the same way, the mechanism of action study showed that these products induced apoptosis through the activation of caspase‐3 in renal cell carcinoma (HaCaT‐ras) ((Figure 1): A‐1) or ((Figure 1): A‐2), associated with the ability to interact with DNA [6–8] …”

Section: Introductionmentioning

confidence: 87%

“…In the same way, the mechanism of action study showed that these products induced apoptosis through the activation of caspase-3 in renal cell carcinoma (HaCaT-ras) ((Figure 1): A-1) or ((Figure 1): A-2), associated with the ability to interact with DNA. [6][7][8] Nowadays, heterocyclic compounds carrying oxygen and nitrogen are an important class of compounds with interesting biological and pharmacological activities, due to their similarity with various bioactive molecules of natural origin. [9][10][11] Among these compounds, substituted thiazolidin-4-ones mediated significant antiproliferative effects, studies concerning structure-activity relationships have shown that the cytotoxic potency of compounds was highly dependent on the types and patterns of N-substitution on the thiazolidin-4-one ring.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Biological and Computational Assessment of New Thiazolidin‐4‐one Derivatives as Potential Anticancer Agents Through the Apoptosis Pathway

et al. 2022

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A variety of novel thiazolidin‐4‐one himachalene derivatives were designed and synthesized through hetero‐cyclization of thiosemicarbazone analogs that have previously exhibited strong anticancer activity. The synthesized products 2 a–4 f were completely characterized by 1H NMR, 13C NMR, IR, and HRMS and were later submitted for in vitro evaluation of their anticancer activity and cytotoxicity on a panel of four human cancer cell lines ( i.eHT‐1080, MCF‐7, A‐549, and MDA‐MB‐231). Most of the evaluated compounds showed potent antiproliferative activities against the four human cancer cell lines with tested IC50 values ranging from 5.25±0.32 to 9.26±0.73 μM. The mechanism of action revealed that compounds 2 b and 4 b induced caspase‐3/7‐activated apoptosis and cell cycle arrest in the G0/G1 stage in HT‐1080 and A‐549 cells. Furthermore, molecular docking studies were conducted to evaluate the binding affinities and the possible binding modes of the top‐performing compounds 2 b and 4 b. This was later supported by Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) analysis predicting their prospective pharmacological profiles. The outcome of this study supports the validity of our strategy and presents 2 b and 4 b as a pattern for the discovery of novel cancer therapeutics.

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The chemotherapeutic effect of β-2-himachalen-6-ol in chemically induced skin tumorigenesis

Cited by 19 publications

References 45 publications

p21 in Cancer Research

p21 in Cancer Research

Synthesis and Biological Evaluation of Novel Thiazole Analogs with Both Anti‐Proliferative and Mechanistic Analyses and Molecular Docking Studies

Design, Synthesis, Biological and Computational Assessment of New Thiazolidin‐4‐one Derivatives as Potential Anticancer Agents Through the Apoptosis Pathway

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