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 ◽  
...  
2019 ◽  
Vol 14 (7) ◽  
pp. 1934578X1986067 ◽  
Author(s):  
Gulnara V. Giniyatullina ◽  
Oxana B. Kazakova ◽  
Irina P. Baikova ◽  
Emil Yu. Yamansarov ◽  
Ilya A. Osterman ◽  
...  

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.


Materials ◽  
2020 ◽  
Vol 13 (24) ◽  
pp. 5813
Author(s):  
Magdalena Zaremba-Czogalla ◽  
Anna Jaromin ◽  
Katarzyna Sidoryk ◽  
Agnieszka Zagórska ◽  
Marcin Cybulski ◽  
...  

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.


Author(s):  
Dungporn Teerasripreecha ◽  
Preecha Phuwapraisirisan ◽  
Songchan Puthong ◽  
Kiyoshi Kimura ◽  
Masayuki Okuyama ◽  
...  

2021 ◽  
pp. 174751982110434
Author(s):  
Van-Tai Nguyen ◽  
Minh-Quan Pham ◽  
Thi-Ha Vu ◽  
Thi-Hong-Ha Tran ◽  
Duy-Tien Doan ◽  
...  

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.


2021 ◽  
Vol 8 (5) ◽  
pp. 01-10
Author(s):  
Hassan A. Al-Shamahy

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.


2013 ◽  
Vol 14 (3) ◽  
pp. 1829-1832 ◽  
Author(s):  
Mai Mohammad Al-Oqail ◽  
Nida Nayyar Farshori ◽  
Ebtesam Saad Al-Sheddi ◽  
Javed Musarrat ◽  
Abdulaziz Ali Al-Khedhairy ◽  
...  

Author(s):  
Hassan Mohammed Al-Mahbashi ◽  
Mohammad Abobakr Al-Ghazali ◽  
Hassan A. Al-Shamahy ◽  
Azhar Azher Mohammed Al-Ankoshy

 Background and aims: Natural products, in particular plant extracts, have opened up great chance in the area of drug progress owing to their chemical variety. The Aloe genus has long been known to be used for medicinal uses in countless parts of the world. This study was planned to inspect the phytochemicals and anti-cancer capabilities of Aloe rubroviolaceae, Aloe vera and Aloe sabaea flowers. Materials and Methods: Three types of ethanolic extracts 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 ethanolic 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 applied to assess the in vitro cytotoxic activity of various 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 presents an initial screening for anti-proliferative activity of a variety of Aloe species flowers extracts on diverse cancer cell lines. Different extracts of Aloe species significantly inhibit the growth of various cancer cell lines  in a concentration-dependent manner. Advance researches are necessary to understand the possible mechanism(s) of action of these extract on a variety of cancer cells and separation of active phyto-chemicals.                   Peer Review History: Received: 18 July 2021; Revised: 17 August; Accepted: 8 September, Available online: 15 September 2021 Academic Editor:  Dr. Muhammad Zahid Iqbal, AIMST University, Malaysia, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency.  Received file:                Reviewer's Comments: Average Peer review marks at initial stage: 6.5/10 Average Peer review marks at publication stage: 7.5/10 Reviewers: Dr. U. S. Mahadeva Rao, Universiti Sultan Zainal Abidin, Terengganu Malaysia, [email protected] Dr. Nazim Hussain, BFIT, Dehradun, Uttarakhand, India, [email protected] Similar Articles: ANTIFUNGAL, CYTOTOXIC AND PHYTOTOXICITY OF AERIAL PART OF RANUNCULUS MURICATUS IN VITRO INHIBITORY ACTIVITY OF BERBERIS VULGARIS L. AGAINST LEISHMANIA TROPICA PROMASTIGOTES


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