scholarly journals In-vitro and in-silico anticancer potential of taxoids from Taxus wallichiana Zucc

2019 ◽  
Vol 70 (4) ◽  
pp. 295-300
Author(s):  
Mughal Qayum ◽  
Muhammad Nisar ◽  
Abdur Rauf ◽  
Imran Khan ◽  
Waqar Ahmad Kaleem ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Docking Study ◽  
Cancer Cell Lines ◽  
Cancer Drug ◽  
Bioactive Constituents ◽  
Taxus Wallichiana

Introduction Natural products derived from medicinal plants provide beneficial cancer chemotherapeutic drugs. Bioactive constituents from plants are explored for their anticancer properties. Methods Three known compounds (deacetylbaccatin III, tasumatrol B, and taxawallin J) were isolated from Taxus wallichiana. Compounds were screened against four cancer cell lines, such as eA498, HepG2, NCI-H226, and MDR 2780AD. Cytotoxic activity was evaluated using MTT assay against cancer cell lines. Results Tasumatrol B showed good cytotoxic activity conducted for the improvement of inhibiting potential of these compounds against the cancer drug target protein (EGFR tyrosine kinase enzyme). The docking study showed that all compounds have binding affinities and interaction profile with the receptor tyrosine kinase. Discussion The study suggests that these compounds could be used for the discovery of novel inhibitors against the target receptors for the treatment of cancer.

scholarly journals Implementation of the NCI-60 Human Tumor Cell Line Panel to Screen 2260 Cancer Drug Combinations to Generate >3 Million Data Points Used to Populate a Large Matrix of Anti-Neoplastic Agent Combinations (ALMANAC) Database

2018 ◽  
Vol 24 (3) ◽  
pp. 242-263 ◽  
Author(s):  
David A. Close ◽  
Allen Xinwei Wang ◽  
Stanton J. Kochanek ◽  
Tongying Shun ◽  
Julie L. Eiseman ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Growth Inhibition ◽  
Cell Line ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Cancer Drug ◽  
Large Matrix ◽  
Data Points

Animal and clinical studies demonstrate that cancer drug combinations (DCs) are more effective than single agents. However, it is difficult to predict which DCs will be more efficacious than individual drugs. Systematic DC high-throughput screening (HTS) of 100 approved drugs in the National Cancer Institute’s panel of 60 cancer cell lines (NCI-60) produced data to help select DCs for further consideration. We miniaturized growth inhibition assays into 384-well format, increased the fetal bovine serum amount to 10%, lengthened compound exposure to 72 h, and used a homogeneous detection reagent. We determined the growth inhibition 50% values of individual drugs across 60 cell lines, selected drug concentrations for 4 × 4 DC matrices (DCMs), created DCM master and replica daughter plate sets, implemented the HTS, quality control reviewed the data, and analyzed the results. A total of 2620 DCMs were screened in 60 cancer cell lines to generate 3.04 million data points for the NCI ALMANAC (A Large Matrix of Anti-Neoplastic Agent Combinations) database. We confirmed in vitro a synergistic drug interaction flagged in the DC HTS between the vinca-alkaloid microtubule assembly inhibitor vinorelbine (Navelbine) tartrate and the epidermal growth factor-receptor tyrosine kinase inhibitor gefitinib (Iressa) in the SK-MEL-5 melanoma cell line. Seventy-five percent of the DCs examined in the screen are not currently in the clinical trials database. Selected synergistic drug interactions flagged in the DC HTS described herein were subsequently confirmed by the NCI in vitro, evaluated mechanistically, and were shown to have greater than single-agent efficacy in mouse xenograft human cancer models. Enrollment is open for two clinical trials for DCs that were identified in the DC HTS. The NCI ALMANAC database therefore constitutes a valuable resource for selecting promising DCs for confirmation, mechanistic studies, and clinical translation.

Synthesis and Сytotoxicity of A-Azepanobetulinic Acid N-Methyl-Piperazinylamide

2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1986067 ◽  
Author(s):  
Gulnara V. Giniyatullina ◽  
Oxana B. Kazakova ◽  
Irina P. Baikova ◽  
Emil Yu. Yamansarov ◽  
Ilya A. Osterman ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antibacterial Agent ◽  
Cancer Cell Lines ◽  
Beckmann Rearrangement ◽  
Betulonic Acid

The synthesis of A-azepanobetulinic acid N-methylpiperazinylamide was performed through a series of transformations (oximation, Beckmann rearrangement, reduction) of previously synthesized betulonic acid N-methylpiperazinylamide. In vitro cytotoxic activity was detected for the obtained compound against a number of cancer cell lines, and its potential was revealed as an antibacterial agent.

scholarly journals Evaluation of the In Vitro Cytotoxic Activity of Caffeic Acid Derivatives and Liposomal Formulation against Pancreatic Cancer Cell Lines

Materials ◽  
2020 ◽  
Vol 13 (24) ◽  
pp. 5813
Author(s):  
Magdalena Zaremba-Czogalla ◽  
Anna Jaromin ◽  
Katarzyna Sidoryk ◽  
Agnieszka Zagórska ◽  
Marcin Cybulski ◽  
...  
Keyword(s):  
Pancreatic Cancer ◽  
Cytotoxic Activity ◽  
Caffeic Acid ◽  
Cell Lines ◽  
Cancer Cell ◽  
Pancreatic Cancer Cell ◽  
Cancer Cell Lines ◽  
Liposomal Formulation ◽  
Caffeic Acid Derivatives

Pancreatic cancer belongs to the most aggressive group of cancers, with very poor prognosis. Therefore, there is an important need to find more potent drugs that could deliver an improved therapeutic approach. In the current study we searched for selective and effective caffeic acid derivatives. For this purpose, we analyzed twelve compounds and evaluated their in vitro cytotoxic activity against two human pancreatic cancer cell lines, along with a control, normal fibroblast cell line, by the classic MTT assay. Six out of twelve tested caffeic acid derivatives showed a desirable effect. To improve the therapeutic efficacy of such active compounds, we developed a formulation where caffeic acid derivative (7) was encapsulated into liposomes composed of soybean phosphatidylcholine and DSPE-PEG2000. Subsequently, we analyzed the properties of this formulation in terms of basic physical parameters (such as size, zeta potential, stability at 4 °C and morphology), hemolytic and cytotoxic activity and cellular uptake. Overall, the liposomal formulation was found to be stable, non-hemolytic and had activity against pancreatic cancer cells (IC50 19.44 µM and 24.3 µM, towards AsPC1 and BxPC3 cells, respectively) with less toxicity against normal fibroblasts. This could represent a promising alternative to currently available treatment options.

Straightforward synthesis of a novel ring-fused pyrazole-lactam and in vitro cytotoxic activity on cancer cell lines

2016 ◽  
Vol 117 ◽  
pp. 1-7 ◽  
Author(s):  
G. Bertuzzi ◽  
E. Locatelli ◽  
D. Colecchia ◽  
P. Calandro ◽  
B.F. Bonini ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines

scholarly journals In vitro antiproliferative/cytotoxic activity on cancer cell lines of a cardanol and a cardol enriched from Thai Apis mellifera propolis

2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Dungporn Teerasripreecha ◽  
Preecha Phuwapraisirisan ◽  
Songchan Puthong ◽  
Kiyoshi Kimura ◽  
Masayuki Okuyama ◽  
...  
Keyword(s):  
Apis Mellifera ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines

scholarly journals Synthesis of pyrophosphate analogues and their cytotoxic activities

2021 ◽  
pp. 174751982110434
Author(s):  
Van-Tai Nguyen ◽  
Minh-Quan Pham ◽  
Thi-Ha Vu ◽  
Thi-Hong-Ha Tran ◽  
Duy-Tien Doan ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Lines ◽  
Dipolar Cycloaddition ◽  
Cytotoxic Activities ◽  
Cycloaddition Reactions

Six pyrophosphate analogues are prepared from zerumbone, murrayafoline A, acridone, and 4-hydroxycoumarin via 1,3-dipolar cycloaddition reactions. Their in vitro cytotoxic activity is evaluated against HepG2, LU-1, and HeLa cancer cell lines. Among them, diisopropyl ((ethoxy((4-((1-methoxy-3-methyl-9 H-carbazol-9-yl)methyl)-1 H-1,2,3-triazol-1-yl)methyl)phosphoryl)methyl)phosphonate (6a) and diisopropyl ((ethoxy((4-(((3-methyl-9 H-carbazol-1-yl)oxy)methyl)-1 H-1,2,3-triazol-1-yl)methyl)phosphoryl)methyl)phosphonate (6b) are found to show activity against HepG2, LU-1, and HeLa cancer cell lines, with IC50 values ranging from 7.31 to 17.88 μM.

scholarly journals Cytotoxic Activities in Vitro of Flower Extracts of Three Species of Aloe Growing in Yemen: Aloe Rubroviolaceae, Aloe Vera and Aloe Sabaea, against Eleven Types of Cancer Cell Lines

2021 ◽  
Vol 8 (5) ◽  
pp. 01-10
Author(s):  
Hassan A. Al-Shamahy
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Aloe Vera ◽  
Cancer Cell Lines ◽  
Myelogenous Leukemia ◽  
Methanolic Extracts

Background and aims: Natural products, especially plant extracts, have opened up great opportunities in the field of drug progress due to their chemical variety. The genus Aloe has long been used for medicinal uses in countless parts of the world. This study was designed to investigate the phytochemicals and anti-cancer capabilities of Aloe rubroviolaceae, Aloe vera and Aloe sabaea flowers. Materials and Methods: The methanolic extracts of three types of plants traditionally used in Yemen to treat a variety of diseases have been tested in vitro for their potential anticancer activity on different human cancer cell lines. The cytotoxic activity of the methanolic extracts of tested plants was determined using eleven strains of human cancer cells, namely: MCF-7 (breast cancer), PC-3 (prostate cancer), HEP-2 (human epithelial carcinoma), MNFS-60 (myelogenous leukemia), CACO (intestinal cancer), A-549 (lung adenocarcinoma), HeLa (cervical cancer), RD (rhabdomyosarcoma),HepG2 (hepatocellular carcinoma), HCT-116 (colon cancer), and CHO-K1 (Chinese hamster ovary). A colorimetric sulforhodamine B assay was used to evaluate the in vitro cytotoxic activity of different extracts. Growth inhibition of 50% (IC50) for each extract was calculated from the optical density of treated and untreated cells. Doxorubicin, a broad-spectrum anticancer drug was used as a positive control. Results: More interesting cytotoxic activity was observed for Aloe vera extract more than Aloe sabaea and Aloe rubroviolaceae, extract. Conclusions: This study provides a preliminary screening for anti-proliferative activity of various Aloe species flowers extracts on different cancer cell lines. Different extracts of Aloe species significantly inhibit the growth of various cancer cell lines in a concentration-dependent manner. Further investigations are required to understand the possible mechanism(s) of action of these extract on various cancer cells and isolation of active phyto-chemicals.

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