Anticancer activity of THMPP: Downregulation of PI3K/ S6K1 in breast cancer cell line

Tapak dara or Madagascar Periwinkle (Catharanthus roseus [L] G.Don), a natural plant, is empirically reported to have promising anticancer activity. To elucidate its mechanism, a research was conducted to investigate the possible ethanol extract of C. roseus in inducing apoptosis on breast cancer cell line (T47D). Antioxidant activity of C. roseus was investigated as well. Sub-G1 flowcytometric apoptotic analysis result showed that extract of C. roseus at 6.25 μg/mL induced apoptosis for 26.365%. Increasing extract concentration resulted an increasing apoptotic level as well, extract at concentration of 12.5 μg/mL induced apoptosis for 22.235%. Meanwhile doxorubicin at concentration of 10 μg/mL induced apoptosis for 36.055%. The antioxidant activity was determined by using in vitro assay: inhibition of 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity. Antioxidant activity of C. roseus extract were compared to quercetin and butylated hydroxyanisol (BHA), as positive controls. The results showed that DPPH IC50 of C. roseus extract, quercetin and BHA were 358.411 μg/mL, 19.200 μg/mL and 94.178 μg/mL, respectively. We suggest that C. roseus extract had a potential anticancer activity by inducing apoptosis.Key words : antioxidant, DPPH, Catharanthus roseus, apoptosis, breast cancer, T47D

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Anticancer Activity of Holothuria atra Extracts on the Triple-Negative Breast Cancer Cell Line MDA-MB-231

SSRN Electronic Journal ◽

10.2139/ssrn.3892194 ◽

2021 ◽

Author(s):

Kunwadee Noonong ◽

Laphatrada Yurasakpong ◽

Kanta Pranweerapaiboon ◽

Suksit Nobsathian ◽

Kulathida Chaithirayanon

Keyword(s):

Breast Cancer ◽

Anticancer Activity ◽

Cell Line ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Triple Negative Breast Cancer ◽

Breast Cancer Cell Line ◽

Triple Negative ◽

Cancer Cell Line ◽

Holothuria Atra

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ENZYME-ENHANCED EXTRACTION OF CAMPTOTHECIN AND ITS ANTICANCER ACTIVITY ON BREAST CANCER CELL LINE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i6.26333 ◽

2018 ◽

Vol 11 (6) ◽

pp. 468

Author(s):

Sujatha Natarajan ◽

Sangilimuthu Alagar Yadav

Keyword(s):

Breast Cancer ◽

Anticancer Activity ◽

Cell Line ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Endophytic Fungi ◽

Breast Cancer Cell Line ◽

Cancer Cell Line ◽

Vero Cells ◽

Extraction Yield

Objective: Camptothecin (CPT) is an alkaloid produced by endophytic fungi, and it acts against colon, uterine, and lung cancers as drug. Macerating enzyme cellulase is used to increase the extraction yield of CPT. The cytotoxicity and anticancer activity of CPT are being studied to aid in discovering its beneficial properties and its use as a lead compound in pharmacological industries.Methods: In this work, the extraction of CPT from the endophytic fungi is enhanced using the crude enzyme cellulase obtained from Aspergillus niger. CPT was extracted from A. niger by two ways such as using macerating enzyme cellulase (CWME) and without macerating enzyme (CWOME). High-performance liquid chromatography (HPLC) was carried out to characterize the extracted CPT against standard CPT. The yields of CPT extracted both ways were compared. Cytotoxicity of the extracted CPTs was studied against Vero cells. The anticancer activity of CPT was tested against the breast cancer cell line (MCF7).Results: The extracted compound was confirmed to be CPT using HPLC. The yield of CPT extracted with enzyme was more than that extracted without enzyme. The extracted CPT was found to be safe up to 1000 μg/ml against Vero cells. The IC50 value of the CWME was found to be 62.5 μg/ml compared to the CWOME (IC50 125 μg/ml) against the MCF7 cell line, thus inferring that the anticancer activity of CWME was higher than that of CWOME.Conclusion: Thus, it can be concluded that cellulase helps to increase the extraction yield of CPT from A. niger. CPT is safe against normal cell line and exhibits anticancer properties against MCF7.

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Design and synthesis of tri-substituted imidazole derivatives as CD73 inhibitors for their anticancer activity

Letters in Drug Design & Discovery ◽

10.2174/1570180818666210604113849 ◽

2021 ◽

Vol 18 ◽

Author(s):

Abhishek Ghara ◽

Ganesh Sakharam Andhale ◽

Gurubasavaraja Swamy Purawarga Matada ◽

Prasad Sanjay Dhiwar

Keyword(s):

Breast Cancer ◽

Clinical Trials ◽

Small Molecules ◽

Anticancer Activity ◽

Cell Line ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Breast Cancer Cell Line ◽

Cancer Cell Line ◽

Imidazole Derivatives

Background: US-FDA-approved monoclonal antibodies focus different biological targets related to immuno-oncology and small molecules which are in clinical trials target different immune-oncology aspects. Some small molecules targeting CD73 are in the different phases of clinical trials. Presently, several imidazoles such as Dacarbazine, Zoledronic acid, Mercaptopurine, etc. are being used in the treatment of various cancers. Hence, we explored the cytotoxicity studies of substituted tri-phenyl imidazoles against breast cancer cell line followed by virtual studies. Methods: We performed molecular docking, ADMET, and molecular properties studies for 68 designed imidazole derivatives using Accelrys Drug Discovery Studio 3.5 software. The binding modes of the designed compounds were studied against CD73 protein (PDB Code: 4H1S). ADMET solubility, BBB penetration, hepatotoxicity, PPB binding, polar surface area also studied to obtain the compounds with best pharmacokinetic properties. The breast cancer cell line MDA-MB-231 was treated with these synthesized compounds and IC50 was evaluated by MTT assay method. Results: Molecular docking studies indicate that the selected 14 compounds show good binding at the active site of CD73 by forming H-bond with amino acid residues. Substituted tri-phenyl imidazole derivatives showed anticancer activity against breast cancer cell line. Particularly, compounds 3a and 3h with electron donating group at 2nd and 3rd position with the p-substitutions of chloro and nitro group showed significant anticancer activity. Conclusion: Based on the in-silico studies fourteen imidazole derivatives were synthesized and evaluated against breast cancer cell line. Compounds 3a and 3h significantly inhibited the growth of MDA-MB-231 cell line. From the in vitro enzyme inhibition studies, only 3h showed significant inhibition.

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