scholarly journals SYNTHESIS AND CHARACTERIZATION OF NOVEL ORGANOBISMUTH FOR ANTIMICROBIAL AND ANTITUMOR STUDIES

2020 ◽  
pp. 57-61
Author(s):  
DIPTI MANI TRIPATHI ◽  
RAVI KANT ◽  
KRISHNA SRIVASTAVA
Keyword(s):  
Spectral Analysis ◽  
Antitumor Activity ◽  
General Formula ◽  
Antitumor Agents ◽  
Antimicrobial Studies ◽  
Trigonal Bipyramidal ◽  
Bipyramidal Structure ◽  
Complexation Reactions

Objectives: The major objective of this manuscript is to present synthesis and biomedical screening of some organic derivatives of bismuth having general formula (R3BiL2) by the method reported and characterized with the help of M.P., elemental, I.R., and NMR spectral analysis along with their antimicrobial and in vitro antitumor activity against human breast (MCF-7) and mammary cancer (EVSA-7) cell line. Methods: All the newly organobismuth having general formula [R3BiL2] were synthesised by the method reported especially using oxidative addition and complexation reactions. Results: It was found that organobismuth compounds have trigonal bipyramidal structure as per their elemental and spectral analysis and show potentiality as antimicrobial and antitumor agents. Conclusion: The newly synthesized organobismuth(V)substituted carboxylates were fully characterized chemically to ascertain their structure by sophisticated instrumental and spectral analysis resulted as trigonal bipyramidal structure. The compounds were also screened 1st time for antitumor and antimicrobial studies. The observations clearly indicated that organobismuth carboxylates show potent antimicrobial and antitumor activity.

scholarly journals ANTITUMOR AND GASTROPROTECTIVE SCREENING OF SOME NOVEL ORGANIC DERIVATIVES OF BISMUTH

2020 ◽  
pp. 62-65
Author(s):  
DIPTI MANI TRIPATHI ◽  
RAVI KANT ◽  
KRISHNA SRIVASTAVA
Keyword(s):  
Spectral Analysis ◽  
Antitumor Activity ◽  
General Formula ◽  
Moderate Activity ◽  
Pyramidal Structure ◽  
Complexation Reactions ◽  
Derivatives Of ◽  
Mcf 7 ◽  
Potential Antitumor

Objectives: The objectives of present manuscript are to synthesize some new organic derivatives of bismuth having general formula (RBiL2; wherein R = C6F5; L = Substituted aromatic carboxylic acid), and characterized with the help of M.P., elemental, I.R., and NMR spectral analysis to ascertain the structure of novel compounds. These compounds were also characterized for their in vitro antitumor activity against human breast (MCF-7) and mammary cancer (EVSA-7) cell line along with gastroprotective (anti-ulcer) activity in rats using standard methods. Methods: All the newly organobismuth having general formula (RBiL2) were synthesised by earliar reported methods especially using redistribution and complexation reactions. The in-vitro antitumor and gastroprotective studies were performed by using standard protocols and methods. Results: It was found that the compounds were crystalline solids, air stable, and soluble in common organic solvent, have sharp melting points, and possess trigonal/pyramidal structure, exhibit higher activity than the standard ranitidine when the tests were carried out with aspirin induced and moderate activity was seen when the tests were done with ethanol induced along with potential antitumor activity against MCF-7 and EVSA-7 cell lines. Conclusion: The newly synthesized organobismuth complexes were characterized to ascertain their structure by sophisticated instrumental and spectral analysis resulted as trigonal/pyramidal structure. The compounds were also screened 1st time for gastroprotective and antitumor activity in vitro. The observations clearly indicate that organobismuth carboxylates as reported here show potential gastroprotective and antitumor activity in vitro.

scholarly journals Design, Synthesis, Molecular Modeling and Antitumor Evaluation of Novel Indolyl-Pyrimidine Derivatives with EGFR Inhibitory Activity

Molecules ◽  
2021 ◽  
Vol 26 (7) ◽  
pp. 1838
Author(s):  
Naglaa M. Ahmed ◽  
Mahmoud M. Youns ◽  
Moustafa K. Soltan ◽  
Ahmed M. Said
Keyword(s):  
Molecular Modeling ◽  
Antitumor Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Antiproliferative Activity ◽  
Antitumor Agents ◽  
Cancer Cell Lines ◽  
Normal Cells

Scaffolds hybridization is a well-known drug design strategy for antitumor agents. Herein, series of novel indolyl-pyrimidine hybrids were synthesized and evaluated in vitro and in vivo for their antitumor activity. The in vitro antiproliferative activity of all compounds was obtained against MCF-7, HepG2, and HCT-116 cancer cell lines, as well as against WI38 normal cells using the resazurin assay. Compounds 1–4 showed broad spectrum cytotoxic activity against all these cancer cell lines compared to normal cells. Compound 4g showed potent antiproliferative activity against these cell lines (IC50 = 5.1, 5.02, and 6.6 μM, respectively) comparable to the standard treatment (5-FU and erlotinib). In addition, the most promising group of compounds was further evaluated for their in vivo antitumor efficacy against EAC tumor bearing mice. Notably, compound 4g showed the most potent in vivo antitumor activity. The most active compounds were evaluated for their EGFR inhibitory (range 53–79 %) activity. Compound 4g was found to be the most active compound against EGFR (IC50 = 0.25 µM) showing equipotency as the reference treatment (erlotinib). Molecular modeling study was performed on compound 4g revealed a proper binding of this compound inside the EGFR active site comparable to erlotinib. The data suggest that compound 4g could be used as a potential anticancer agent.

scholarly journals Design, synthesis and pharmacological evaluation of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives as antitumor agents: in vitro and in vivo antitumor activity, cell cycle arrest and apoptotic response

RSC Advances ◽  
2018 ◽  
Vol 8 (43) ◽  
pp. 24376-24385 ◽  
Author(s):  
Wen-Bin Kuang ◽  
Ri-Zhen Huang ◽  
Yi-Lin Fang ◽  
Gui-Bin Liang ◽  
Chen-Hui Yang ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Quinoline Derivatives ◽  
Apoptotic Response ◽  
Design Synthesis ◽  
Cycle Arrest ◽  
In Vivo Antitumor Activity ◽  
Combination Principle

A series of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives were designed and synthesized as antitumor agents under the combination principle. The antitumor activity and mechanisms were then evaluated.

scholarly journals Screening of Antibacterial, Thrombolytic, Membrane Stabilizing, Anti-inflammatory and Antitumor Activity of Citrus assamensis Leaf Extracts

2018 ◽  
Vol 10 (2) ◽  
pp. 195-210
Author(s):  
M. Shahriar ◽  
M. A. Bhuiyan ◽  
M. S. Rana
Keyword(s):  
Antitumor Activity ◽  
Antitumor Agents ◽  
Chloroform Extract ◽  
Haemolytic Activity ◽  
Hypotonic Solution ◽  
Leaf Extracts ◽  
Thrombolytic Activity ◽  
Anti Inflammatory

The methanol, ethanol and chlorofom leaf extracts of Satkara, Citrus assamensis (family: Rutaceae), were subjected to in vitro anti-bacterial, thrombolytic, membrane stabilizing and in vivo anti-inflammatory and antitumor activity tests. The chloroform extract of C. assamensis showed the most important spectrum of activity against Bacillus subtilis, Bacillus cereus, Sarcina lutea among 6 gram positive and against 11 gram negative bacteria at the concentration of 1000 μg/disc, while the range of zones of inhibition were within 7-16 mm. Among the tested three extracts CHCl3 extract showed potent thrombolytic activity and hypotonic solution induced haemolytic activity where the percentages of inhibition were found to be 35% and 55% respectively. All the extracts established significant (p<0.05) anti-inflammatory effect by regulating biphasic inflammatory process induced by carrageenan. The leaf extract dose-dependently and significantly decreases the number of EAC cell count and inhibition of cell growth in comparison to the EAC control and standard. The results obtained in the present study indicate that, C. assamensis leaf can be a potential source of anti-bacterial, thrombolytic, membrane stabilizing, anti-inflammatory and antitumor agents.

scholarly journals Chemical Characterization of the Lichen-symbiont Microalga Asterochloris erici and Study of Its Cytostatic Effect on the L929 Murine Fibrosarcoma Cell Line

2021 ◽  
Author(s):  
M. Concepción Matesanz ◽  
Mercedes Villa-Carvajal ◽  
Javier Linares ◽  
Sonia Morante-Zarcero ◽  
Isabel Sierra ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Chemical Characterization ◽  
Human Consumption ◽  
Cytostatic Effect ◽  
In Vitro Biocompatibility ◽  
Murine Fibrosarcoma ◽  
Terrestrial Lichen

New resources of food, pharmaceuticals or biotechnological products are needed. The huge biodiversity of aero-terrestrial lichen-symbiont microalgae remains unexplored. Viability of these for human consumption demands the demonstration of the absence of toxic effects. In vitro biocompatibility of crude homogenates of axenic microalga Asterochloris erici, symbiotic in the lichen Cladonia cristatella, was analyzed after treatment of cultured L929 fibroblasts with different doses of microalgal homogenates. The results show that crude homogenates of A. erici do not induce fibroblast cytotoxicity but seem to have some cytostatic effect inducing slight cell cycle alterations and intracellular reactive oxygen species (ROS) increase at the highest dose. Carotenoid analysis demonstrates high content of lutein, a xanthophyll with antioxidant and cytostatic properties in vivo. These findings confirm that Asterochloris erici can be considered suitable for the development of alimentary or pharmaceutical applications. The cytostatic effects should be further investigated for antitumor agents.

scholarly journals Synthesis and structural characterization of Pd(II) complexes derived from perimidine ligand and their in vitro antimicrobial studies

2013 ◽  
Vol 1047 ◽  
pp. 48-54 ◽  
Author(s):  
Mohammad Azam ◽  
Ismail Warad ◽  
Saud I. Al-Resayes ◽  
Nabil Alzaqri ◽  
Mohammad Rizwan Khan ◽  
...  
Keyword(s):  
Structural Characterization ◽  
Antimicrobial Studies

scholarly journals Recent Advances in Improved Anticancer Efficacies of Camptothecin Nano-Formulations: A Systematic Review

Biomedicines ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 480
Author(s):  
Maryam Ghanbari-Movahed ◽  
Tea Kaceli ◽  
Arijit Mondal ◽  
Mohammad Hosein Farzaei ◽  
Anupam Bishayee
Keyword(s):  
Systematic Review ◽  
Antitumor Activity ◽  
Cancer Treatment ◽  
Topoisomerase I ◽  
Antitumor Agents ◽  
Critical Evaluation ◽  
Antitumor Activities ◽  
Passive Targeting

Camptothecin (CPT), a natural plant alkaloid, has indicated potent antitumor activities via targeting intracellular topoisomerase I. The promise that CPT holds in therapies is restricted through factors that include lactone ring instability and water insolubility, which limits the drug oral solubility and bioavailability in blood plasma. Novel strategies involving CPT pharmacological and low doses combined with nanoparticles have indicated potent anticancer activity in vitro and in vivo. This systematic review aims to provide a comprehensive and critical evaluation of the anticancer ability of nano-CPT in various cancers as a novel and more efficient natural compound for drug development. Studies were identified through systematic searches of PubMed, Scopus, and ScienceDirect. Eligibility checks were performed based on predefined selection criteria. Eighty-two papers were included in this systematic review. There was strong evidence for the association between antitumor activity and CPT treatment. Furthermore, studies indicated that CPT nano-formulations have higher antitumor activity in comparison to free CPT, which results in enhanced efficacy for cancer treatment. The results of our study indicate that CPT nano-formulations are a potent candidate for cancer treatment and may provide further support for the clinical application of natural antitumor agents with passive targeting of tumors in the future.

scholarly journals Formulation And Characterization of Carageenan Gels Encapsulating Amphotericin B And Lactobacillus acidophilus Against Candidal Vaginitis

2017 ◽  
Vol 4 (1) ◽  
pp. 37-49
Author(s):  
R Kaur ◽  
M Khurana ◽  
M Bindal ◽  
A Sharma
Keyword(s):  
Candida Albicans ◽  
Drug Release ◽  
Sustained Release ◽  
Amphotericin B ◽  
Lactobacillus Acidophilus ◽  
Drug Carriers ◽  
In Vitro Drug Release ◽  
Antimicrobial Studies

The present study is concerned with the development and characterization of bioadhesive carageenan gel encapsulating Amphotericin B and Lactobacillus acidophillus, prepared by graft co-polymeriztion against Candidal vaginitis. Intravaginal gel systems based on bioadhesive polymer (carrageenan) were characterized with respect to swelling index, bioadhesive strength, percent encapsulation and in vitro drug release antimicrobial studies. A marked increase in swelling index of gel encapsulating Lactobacillus was found to be 1.9±0.35. The percent encapsulation of drug was found to be 98.63%±.0.2% and that of Lactobacillus was 91.81 ±0.01. The viability was observed for interval of 6 hrs on trypton soya agar and showed that viability was highly conserved till 4 hrs. The antimicrobial study of gels encapsulating Amphotericin B and Lactobacillus showed that carageenan gel can inhibit Candida albicans upto a maximum extent. Bioadhesivity study also conducted for gels that showed a bioadhesivity of 84.66% ±.0.5% with drug, 88.66% ±.02% with Lactobacillus. In-vitro drug release showed a sustained type release of drug from the polymer i.e. there was initial burst of Amphotericin B up to 5 hours, after which there was a sustained release upto 10 days. Thus it has been concluded from the present study that bioadhesive gels encapsulating Amphotericin B can act as promising drug carriers along with Lactobacillus against candidal vaginitis.

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