scholarly journals Antiproliferative activity of extract from in vitro callus cultures of Astragalus vesicarius ssp. carniolicus (A. Kern.) Chater

Pharmacia ◽  
2021 ◽  
Vol 68 (1) ◽  
pp. 217-221
Author(s):  
Pavlinka Popova ◽  
Yancho Zarev ◽  
Rositsa Mihaylova ◽  
Georgi Momekov ◽  
Iliana Ionkova
Keyword(s):  
Enzymatic Hydrolysis ◽  
Cell Line ◽  
Antiproliferative Activity ◽  
Multidrug Resistant ◽  
Callus Cultures ◽  
Resistant Variant ◽  
Strong Activity ◽  
Etoac Extract ◽  
H Nmr

Five isoflavonoids, i.e. 5-hydroxy-7-methoxy-2’, 5’-dihydroxyisoflavone (AV4), 5, 7-dihydroxy-4’-methoxyisoflavone (AV6), 7-methoxy-5-hydroxy-4’-methoxy-2’-hydroxyisoflavone (AV7), 8-pregnyl genistein (AV9), 5,7-dihydroxy-8-pregnyl-4’-methoxy-2’-hydroxyisoflavone (AV10) and one coumarochromone – sophorophenolone (AV8) were isolated from EtOAc of in vitro callus cultures of Astragalus vesicarius ssp. carniolicus, after enzymatic hydrolysis with β-glucosidase. Their structures were tentatively elucidated by spectroscopic mean (1H NMR and HR-ESI-MS spectra). Antiproliferative activity of EtOAc extract and isolated aglycones against chemosensitive human promyelocyte cell line HL-60 and its multidrug-resistant variant HL-60/Dox was assessed in vitro. Despite the strong activity of EtOAc (IC50 8.8 µg/mL (HL-6, 72 h) to 11.8 µg/mL (HL-60/Dox, 72 h)), prenylated compound AV9 showed also antiproliferative activity – 36.1 µg/mL (HL-60 and HL-60/Dox, 72 h).

scholarly journals Uncommon Trimethoxylated Flavonol Obtained fromRubus rosaefoliusLeaves and Its Antiproliferative Activity

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Marcel Petreanu ◽  
Emili Kamila Ferreira ◽  
Ana Paula M. Sagaz ◽  
Débora B. Vendramini-Costa ◽  
Ana Lúcia T. G. Ruiz ◽  
...  
Keyword(s):  
Cell Line ◽  
Antiproliferative Activity ◽  
Glioma Cells ◽  
Cancer Cell Line ◽  
Multidrug Resistant ◽  
Spectroscopic Methods ◽  
Total Growth ◽  
Tormentic Acid ◽  
Selective Activity

This study shows the evaluation the antiproliferative effect of the extract, fractions, and uncommon compounds isolated fromR. rosaefoliusleaves. The compounds were identified by conventional spectroscopic methods such as NMR-H1and C13and identified as 5,7-dihydroxy-6,8,4′-trimethoxyflavonol (1), 5-hydroxy-3,6,7,8,4′-pentamethoxyflavone (2), and tormentic acid (3). Both hexane and dichloromethane fractions showed selectivity for multidrug-resistant ovary cancer cell line (NCI-ADR/RES) with total growth inhibition values of 11.1 and 12.6 μg/ml, respectively. Compound1also showed selective activity against the same cell line (18.8 μg/ml); however, it was especially effective against glioma cells (2.8 μg/ml), suggesting that this compound may be involved with thein vitroantiproliferative action.

scholarly journals Synthesis, DNA-binding and antiproliferative activity of N-(Nitrogen heterocyclic) norcantharidin acylamide acid

2009 ◽  
Vol 7 (3) ◽  
pp. 569-575 ◽  
Author(s):  
Wen-Zhong Zhu ◽  
Rui-Ding Hu ◽  
Qiu-Yue Lin ◽  
Xiao-Xia Wang ◽  
Xiao-Liang Zheng
Keyword(s):  
Dna Binding ◽  
Cell Line ◽  
Elemental Analysis ◽  
Antiproliferative Activity ◽  
Plasmid Dna ◽  
H Nmr ◽  
Smmc7721 Cell ◽  
Calf Thymus ◽  
Binding Experiment ◽  
Pbr322 Plasmid

AbstractTwo novel norcantharidin acylamide acids (HL1=N-pyrimidine norcantharidin acylamide acid, C12H13N3O4; HL2=N-pyridine norcantharidin acylamide acid, C13H14N2O4) were synthesized by a reaction of norcantharidin(NCTD) with 2-aminopyrimidine and 2-aminopyridine, respectively. Their structures were characterized by elemental analysis, IR, UV and 1 H NMR. Fluorescence titration and viscosity measurements indicated that HL1, HL2 and HL3 (HL3=N-phenyl norcantharidin acylamide acid, C14H15NO4) can bind calf thymus DNA via partial intercalation. The liner Stern-Volmer quenching constant Ksv values for HL1, HL2 and HL3 were 2.05 × 104 L mol−1, 1.15 × 104 L mol−1 and 8.30×103 L mol−1, respectively. Two compounds containing heterocycle of HL1 and HL2 have been found to cleave pBR322 plasmid DNA at physiological pH and temperature. The test of antiproliferation activity showed that the compounds had moderate to strong antiproliferative ability against the tested cell lines except of HL3 against the SMMC7721 cell line. The results indicated that the heterocycle attached to the norcantharidin was favorable to antiproliferative activity. This result was consistent with the DNA binding experiment.

Synthesis and antiproliferative activity of novel 4-azasteroidal-17-hydrazone derivatives

2019 ◽  
Vol 43 (3-4) ◽  
pp. 130-134
Author(s):  
Shao-Rui Chen ◽  
Hao Wu ◽  
Hai-Yan Zhao ◽  
Yu-Mei Zhang ◽  
Peng-Qi Li ◽  
...  
Keyword(s):  
Cell Line ◽  
Antiproliferative Activity ◽  
Normal Cell ◽  
Spectroscopic Data ◽  
Human Lung ◽  
Positive Control ◽  
Mucosal Cell ◽  
Human Gastric Adenocarcinoma ◽  
Normal Human

A new series of 4-azasteroidal-17-hydrazone derivatives have been synthesized from androstenedione. Their structures were characterized by analysis and spectroscopic data. The antiproliferative activity of synthesized compounds against three cancer cells (human lung adenocarcinoma, human oesophageal cervical cancer, human gastric adenocarcinoma) and a normal cell line (human gastric mucosal) was investigated. The studies show that the compound bearing a naphthyl group displayed the same antiproliferative activity in vitro against tested cells as cis-platin did (a positive control). Most of the compounds show very weak toxicity towards normal human gastric mucosal cell line.

scholarly journals HPLC-DAD Analysis, Antileishmanial, Antiproliferative, and Antibacterial Activities ofLacistema pubescens: An Amazonian Medicinal Plant

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Josiane Mello da Silva ◽  
Luciana Maria Ribeiro Antinarelli ◽  
Nícolas de Castro Campos Pinto ◽  
Elaine Soares Coimbra ◽  
Elaine Maria de Souza-Fagundes ◽  
...  
Keyword(s):  
Antiproliferative Activity ◽  
Methanolic Extract ◽  
Indigenous Communities ◽  
Antibacterial Activities ◽  
Peritoneal Macrophages ◽  
Jurkat Cells ◽  
Hexane Fraction ◽  
Strong Activity ◽  
Cytotoxicity Activities

Species of the genusLacistemaare traditionally used by Brazilian and Peruvian indigenous communities. The present study investigated thein vitroantileishmanial activity against severalLeishmaniaspecies, cytotoxicity in murine peritoneal macrophages, antiproliferative activity against HL60 and Jurkat cells, and antibacterial activities against seven bacteria strains of the aerial parts of the methanolic crude extract and fractions ofLacistema pubescens. In addition, their chemical profile was also evaluated. Hexane fraction showed the most significant IC50values against all promastigotes ofLeishmaniaspecies tested, except forL. chagasi(IC50= 4.2 µg/mL forL. majorand IC50= 3.5 µg/mL forL. amazonensis). This fraction also exhibited a strong activity against amastigotes ofL. amazonensis(IC50= 6.9 µg/mL). The antiproliferative activity was also observed for methanolic extract and hexane fraction with IC50= 47.2 µg/mL and IC50= 39.7 µg/mL for HL60, respectively. Regarding the antimicrobial activity, the overall antibacterial activity was not very significative. Phytol and sitosterol were identified in the methanolic extract. Additionally, previous studies also revealed the presence of those compounds in the hexane fraction. Among other compounds, phytol and sitosterol were probably involved in the antileishmanial and cytotoxicity activities observed in this study.

Mouse Myeloma Cell Line Sp2/0 Multidrug-Resistant Variant as Parental Cell Line for Hybridoma Construction

2003 ◽  
Vol 22 (5) ◽  
pp. 321-327 ◽  
Author(s):  
Marina B. Melixetian ◽  
Maria A. Pavlenko ◽  
Elena V. Beriozkina ◽  
Zoya V. Kovaleva ◽  
Elena A. Sorokina ◽  
...  
Keyword(s):  
Cell Line ◽  
Myeloma Cell ◽  
Multidrug Resistant ◽  
Parental Cell ◽  
Parental Cell Line ◽  
Myeloma Cell Line ◽  
Resistant Variant ◽  
Mouse Myeloma Cell ◽  
Mouse Myeloma Cell Line ◽  
Mouse Myeloma

scholarly journals Sulphamoylated estradiol analogue induces antiproliferative activity and apoptosis in breast cell lines

2012 ◽  
Vol 17 (4) ◽  
Author(s):  
Michelle Visagie ◽  
Thandi Mqoco ◽  
Anna Joubert
Keyword(s):  
Estrogen Receptor ◽  
Epithelial Cell ◽  
Cell Line ◽  
Cell Density ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Breast Adenocarcinoma ◽  
Epithelial Cell Line ◽  
Antimitotic Activity

AbstractResearch into potential anticancer agents has shown that 2-methoxyestradiol exerts antiproliferative activity in vitro and in vivo in an estrogen receptor-independent manner. Due to its limited biological accessibility and rapid metabolic degradation, several new analogues have been developed in recent years. This study investigated the in vitro effects of a novel in silicodesigned compound (C16) in an estrogen receptor-positive breast adenocarcinoma epithelial cell line (MCF-7), an estrogen receptor-negative breast adenocarcinoma epithelial cell line (MDA-MB-231) and a nontumorigenic breast cell line (MCF-12A). Light microscopy revealed decreased cell density, cells blocked in metaphase and the presence of apoptotic characteristics in all three cell lines after exposure to C16 for 24 h. Polarizationoptical transmitted light differential interference contrast revealed the presence of several rounded cells and decreased cell density. The xCELLigence real-time label-independent approach revealed that C16 exerted antiproliferative activity. Significant inhibition of cell growth was demonstrated after 24 h of exposure to 0.2 μM C16 in all three cell lines. However, the non-tumorigenic MCF-12A cell line recovered extremely well after 48 h when compared to the tumorigenic cell lines. This indicates that C16 acts as an antiproliferative agent, possesses antimitotic activity and induces apoptosis in vitro. These features warrant further investigation.

Polyethylene Oxide-Polystyrene Oxide Triblock Copolymers as Biological-Responsive Nanocarriers.

2012 ◽  
Vol 1468 ◽  
Author(s):  
Adriana Cambón ◽  
Ana Rey-Rico ◽  
Silvia Barbosa ◽  
Jose Brea ◽  
M. I. Loza ◽  
...  
Keyword(s):  
Cell Line ◽  
Polyethylene Oxide ◽  
Triblock Copolymers ◽  
Styrene Oxide ◽  
Temporal Stability ◽  
Tumor Cell Line ◽  
Micelle Formation ◽  
Multidrug Resistant ◽  
Drug Release Profile

ABSTRACTThe present work presents the synthesis, characterization and evaluation of the biocompatibility and ability to dissolve and chemically protect the anticancer drug doxorubicin (DOXO) of two polyethylene oxide-polystyrene oxide triblock copolymers, EO33SO13EO33 and EO38SO10EO38, where EO and SO denote the ethylene oxide and styrene oxide blocks, respectively. Block copolymer length and SO/EO ratio were selected with the objective of ensuring an optimal compromise between chain solubility, micelle formation ability and core size for enhanced drug solubilization. The temporal stability of the drug-loaded micelles and drug release profile were also analyzed as well as their efficacy as an antitumoral polymeric formulation in vitro by using a multidrug resistant ovarian tumor cell line (NCI-ADR-RES), with the special aim of analyzing the possible capability of both copolymers as potential P-glycoprotein efflux (P-gp) pump inhibitors to enhance DOXO accumulation in this cell line.

scholarly journals Benzophenone Derivatives Showed Dual Anti-Inflammatory and Antiproliferative Activities by Inhibiting COX Enzymes and Promote Cyclin E Downregulation

2022 ◽  
Author(s):  
Laís Folquitto ◽  
Thiago de Souza ◽  
Jaqueline Januario ◽  
Isadora Nascimento ◽  
Brenda Brandão ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Cell Line ◽  
Cell Lines ◽  
Antiproliferative Activity ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Antiproliferative Activities ◽  
Mcf 7

Considering the promising antitumor effects of compounds with dual anti-inflammatory and antiproliferative activities, thus benzophenones analogs (2-7) were evaluated on in vivo antiinflammatory assay and molecular docking analysis. Those with the best molecular docking results were in vitro evaluated on cyclooxygenase (COX) enzymes and tested regarding antiproliferative activity. All derivatives displayed in vivo anti-inflammatory activity. Among them, the substances 2’-hydroxy-4’-benzoylphenyl-β-D-glucopyranoside (4), 4-hydroxy-4’-methoxybenzophenone (5) and 4’-(4’’-methoxybenzoyl)phenyl-β-D-glucopyranoside (7) showed the best values of Glide Score in COX-2 docking evaluation and 4 and 5 selectively inhibited COX-2 and COX-1 in vitro enzymatic assay, respectively. Thus, 4 and 5 were tested against breast cancer (MCF-7, MDA‑MB-231, Hs578T) and non-small-cell-lung cancer (A549) cell lines. The estrogen-positive MCF-7 cell line was more responsive compared to other tested cell lines. They induced cell cycle arrest at G1/S transition in MCF-7 cell line once there was an increase in G0/G1 population with concomitant reduction of S population. The antiproliferative activity of these substances on MCF-7 was associated with their ability to inhibit cyclin E expression, a critical regulator of G1/S transition. Taken together, the data indicate that 4 and 5 have dual anti-inflammatory and antiproliferative activities and support further studies to evaluate their antitumor potential.

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