scholarly journals Synthesis and Biological Evaluation of Thiazolyl-Ethylidene Hydrazino-Thiazole Derivatives: A Novel Heterocyclic System

2021 ◽  
Vol 11 (19) ◽  
pp. 8908
Author(s):  
Laila A. Al-Mutabagani ◽  
Fathy M. Abdelrazek ◽  
Sobhi M. Gomha ◽  
Ali S. Hebishy ◽  
Mohamed S. Abdelfattah ◽  
...  
Keyword(s):  
Cell Lines ◽  
Biological Evaluation ◽  
Liver Carcinoma ◽  
Cytotoxic Activities ◽  
Thiazole Derivatives ◽  
Reference Drug ◽  
Anticancer Properties ◽  
Breast Carcinoma Cell Lines

The reaction of 2-(1-(2-(2-(4-methoxybenzylidene)hydrazinyl)-4-methylthiazol-5-yl)ethylidene)hydrazinecarbothioamide with a range of hydrazonoyl chlorides and α-halo-compounds yielded three new series of thiazole derivatives. Chemical and physical techniques were used to analyze all newly prepared derivatives (1H-NMR, 13C-NMR, FT-IR and mass spectrometry). The potential antimicrobial and anticancer properties of the synthesized derivatives were investigated using various in vitro biological experiments. Most of the thiazole compounds tested were effective against Gram-positive and Gram-negative bacteria. In addition, a minimum inhibition concentration was determined for the antibiotic properties of the most active produced substances. The cytotoxic activities were tested on HepG-2 (liver carcinoma), HCT-116 (colorectal carcinoma) and MDA-MB-231 (breast carcinoma) cell lines in comparison with cisplatin reference drug and using colorimetric MTT assay. The results detected that compound 10c was the most potent against the three tested cell lines. Interestingly, when the tested compounds were evaluated for their toxicity against normal (MRC-5) cells, they exhibited low toxic effects indicating the safe use of most of them that may require further in vivo and pharmacological studies.

Ellagic Acid Cytotoxic and Metalloproteinases Inhibitory Effects Against Oral Squamous Cell Carcinoma: An in Vitro Study

2021 ◽  
Author(s):  
Patricia Maria Wiziack Zago ◽  
Luiza Rodrigues Hellmeister ◽  
Lucas Novaes Teixeira ◽  
Rui Barbosa de Brito Junior ◽  
Elizabeth Ferreira Martinez
Keyword(s):  
Oral Cancer ◽  
Cell Lines ◽  
Ellagic Acid ◽  
Normal Cell ◽  
In Vitro Study ◽  
Significance Level ◽  
Viability Analysis ◽  
Anticancer Properties

Abstract ObjectivesThis study aimed to evaluate the in vitro antitumoral potential of different concentrations of EA against two OSCC cell lines with distinct tissue invasiveness profiles. Material and methodsNormal keratinocytes (NOK) and OSCC´s cells CAL-27 and SCC-9 were treated with concentrations of EA varying from 5 to 662 µM during 24, 48 or 72h. After each time of treatment, cells were submitted to viability analysis using MTT and the secretion of metalloproteinases (MMP-2 and MMP-9) and tissue metalloproteinases inhibitors (TIMP-1 and TIMP-2) were performed by Enzyme-Linked Immunoassay (ELISA). Data were submitted to ANOVA, followed by Bonferroni´s test, considering 5% as significance level. ResultsEA was cytotoxic to OSCC cells in all exposure times, rarely affecting normal cell viability, except for concentrations higher than 82 µM and after 72h treatment. For OSCC cells, EA decreased MMPs and increased TIMPs´s expression without effect on those enzymes for normal cell lines during all times of exposure. ConclusionEA is a promising therapeutic adjuvant to treat oral cancer, however, further in vivo studies are required to clinically validate its potential. Clinical RelevanceThe in vitro anticancer properties showed by Ellagic acid, a phenolic compound that could easily be accessed by oral cancer patients, provides data to base future clinical studies intended to develop a safe topical oral anticancer product.

scholarly journals Design, synthesis and biological evaluation of a series of CNS penetrant HDAC inhibitors structurally derived from amyloid-β probes

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Myeong A Choi ◽  
Sun You Park ◽  
Hye Yun Chae ◽  
Yoojin Song ◽  
Chiranjeev Sharma ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Hdac Inhibitors ◽  
Amyloid Β ◽  
Biological Evaluation ◽  
Pharmacokinetic Studies ◽  
Dependent Manner ◽  
Reference Drug ◽  
Novel Scaffold

Abstract To develop novel CNS penetrant HDAC inhibitors, a new series of HDAC inhibitors having benzoheterocycle were designed, synthesized, and biologically evaluated. Among the synthesized compounds, benzothiazole derivative 9b exhibited a remarkable anti-proliferative activity (GI50 = 2.01 μM) against SH-SY5Y cancer cell line in a dose and time-dependent manner, better than the reference drug SAHA (GI50 = 2.90 μM). Moreover, compound 9b effectively promoted the accumulation of acetylated Histone H3 and α-tubulin through inhibition of HDAC1 and HDAC6 enzymes, respectively. HDAC enzyme assay also confirmed that compound 9b efficiently inhibited HDAC1 and HDAC6 isoforms with IC50 values of 84.9 nM and 95.9 nM. Furthermore, compound 9b inhibited colony formation capacity of SH-SY5Y cells, which is considered a hallmark of cell carcinogenesis and metastatic potential. The theoretical prediction, in vitro PAMPA-BBB assay, and in vivo brain pharmacokinetic studies confirmed that compound 9b had much higher BBB permeability than SAHA. In silico docking study demonstrated that compound 9b fitted in the substrate binding pocket of HDAC1 and HDAC6. Taken together, compound 9b provided a novel scaffold for developing CNS penetrant HDAC inhibitors and therapeutic potential for CNS-related diseases.

scholarly journals In VitroandIn VivoAntimalarial Evaluations of Myrtle Extract, a Plant Traditionally Used for Treatment of Parasitic Disorders

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Farzaneh Naghibi ◽  
Somayeh Esmaeili ◽  
Noor Rain Abdullah ◽  
Mehdi Nateghpour ◽  
Mahdieh Taghvai ◽  
...  
Keyword(s):  
Cell Lines ◽  
Mammalian Cell ◽  
Methanolic Extract ◽  
Cytotoxic Activities ◽  
Traditional Use ◽  
Aerial Parts ◽  
Mammalian Cell Lines ◽  
Phytochemical Investigation

Based on the collected ethnobotanical data from the Traditional Medicine and Materia Medica Research Center (TMRC), Iran,Myrtus communisL. (myrtle) was selected for the assessment ofin vitroandin vivoantimalarial and cytotoxic activities. Methanolic extract of myrtle was prepared from the aerial parts and assessed for antiplasmodial activity, using the parasite lactate dehydrogenase (pLDH) assay against chloroquine-resistant (K1) and chloroquine-sensitive (3D7) strains ofPlasmodium falciparum. The 4-day suppressive test was employed to determine the parasitemia suppression of the myrtle extract againstP. berghei  in vivo. The IC50values of myrtle extract were 35.44 µg/ml against K1 and 0.87 µg/ml against 3D7. Myrtle extract showed a significant suppression of parasitaemia (84.8 ± 1.1% at 10 mg/kg/day) in mice infected withP. bergheiafter 4 days of treatment. Cytotoxic activity was carried out against mammalian cell lines using methyl thiazol tetrazolium (MTT) assay. No cytotoxic effect on mammalian cell lines up to 100 µg/mL was shown. The results support the traditional use of myrtle in malaria. Phytochemical investigation and understanding the mechanism of action would be in our upcoming project.

scholarly journals A newfangled coordinated ruthenium phloretin complex reprogramming breast cancer microenvironment interceded by modulation of PI3K/Akt/mTOR/VEGF pathway and modifying the antioxidant status correlated with intensified apoptotic events.

2020 ◽  
Author(s):  
Chenyang He ◽  
Guo Yu ◽  
Anil Kumar Mondru ◽  
Tania Chakraborty ◽  
Souvik Roy
Keyword(s):  
Breast Carcinoma ◽  
Cell Lines ◽  
Human Cancer ◽  
In Vivo Model ◽  
Human Cancer Cell Lines ◽  
Vegf Pathway ◽  
Breast Carcinoma Cell Lines ◽  
Mcf 7

Abstract Background: Our recent investigation directed to synthesize and characterize a novel ruthenium– phloretin complex accompanied by the study of antioxidant in addition to DNA binding capabilities, and to determine the chemotherapeutic activity against breast carcinoma in vitro and in vivo approach.Methods: Ruthenium–phloretin complex was synthesized and characterized using various spectroscopic methods. The complex was further investigated to determine its efficacy in both MCF-7 and MDA-MB-231 human cancer cell lines and finally in an in vivo model of DMBA induced mammary carcinogenesis in ratsResults: Our studies confirm that the chelation of the metal and ligand was materialize by the 3-OH and 9-OH functional groups of the ligand and the complex is found crystalline and was capable of intercalating with CT-DNA. The complex was capable of reducing cellular propagation and initiate apoptotic events in MCF-7 and MDA-MB-231 breast carcinoma cell lines. Additionally, ruthenium-phloretin complex could modulate p53 intervene apoptosis in the breast carcinoma, initiated by the intrinsic apoptotic trail facilitated by the Bcl2 and Bax and at the same time down regulating the PI3K/Akt/mTOR pathway coupled with MMP9 regulated tumor invasive pathways.Conclusions: Ruthenium-phloretin chemotherapy could interrupt, revoke or suspend the succession of breast carcinoma by altering intrinsic apoptosis along with the antiangiogenic pathway, hence fulfilling the role of a prospective candidate in cancer chemotherapeutics in the in the near future.

scholarly journals A Newfangled Coordinated Ruthenium Phloretin Complex Reprogramming Breast Cancer Microenvironment Interceded by Modulation of PI3K/Akt/Mtor/VEGF Pathway and Modifying The Antioxidant Status Correlated With Intensified Apoptotic Events.

2020 ◽  
Author(s):  
Chenyang He ◽  
Junli Wang ◽  
Tania Chakraborty ◽  
Souvik Roy
Keyword(s):  
Breast Carcinoma ◽  
Cell Lines ◽  
Human Cancer ◽  
In Vivo Model ◽  
Human Cancer Cell Lines ◽  
Vegf Pathway ◽  
Breast Carcinoma Cell Lines ◽  
Mcf 7

Abstract Background: Our recent investigation directed to synthesize and characterize a novel ruthenium– phloretin complex accompanied by the study of antioxidant in addition to DNA binding capabilities, and to determine the chemotherapeutic activity against breast carcinoma in vitro and in vivo approach.Methods: Ruthenium–phloretin complex was synthesized and characterized using various spectroscopic methods. The complex was further investigated to determine its efficacy in both MCF-7 and MDA-MB-231 human cancer cell lines and finally in an in vivo model of DMBA induced mammary carcinogenesis in ratsResults: Our studies confirm that the chelation of the metal and ligand was materialize by the 3-OH and 9-OH functional groups of the ligand and the complex is found crystalline and was capable of intercalating with CT-DNA. The complex was capable of reducing cellular propagation and initiate apoptotic events in MCF-7 and MDA-MB-231 breast carcinoma cell lines. Additionally, ruthenium-phloretin complex could modulate p53 intervene apoptosis in the breast carcinoma, initiated by the intrinsic apoptotic trail facilitated by the Bcl2 and Bax and at the same time down regulating the PI3K/Akt/mTOR pathway coupled with MMP9 regulated tumor invasive pathways.Conclusions: Ruthenium-phloretin chemotherapy could interrupt, revoke or suspend the succession of breast carcinoma by altering intrinsic apoptosis along with the antiangiogenic pathway, hence fulfilling the role of a prospective candidate in cancer chemotherapeutics in the in the near future.

scholarly journals In vitro Evaluation of Antibacterial, Cytotoxic and Adherence Studies of Selected Commercial Probiotics

2020 ◽  
Vol 14 (3) ◽  
pp. 2085-2091
Author(s):  
Kolli Guna Ranjan ◽  
Girija Sankar G. ◽  
D.V.V. Satyanarayana Raju
Keyword(s):  
Cell Lines ◽  
Scientific Evidence ◽  
In Vivo Studies ◽  
Cytotoxic Activities ◽  
Safety Aspects ◽  
A Value ◽  
And Performance ◽  
Commercial Probiotics

There is increasing scientific evidence and commercial interest for using probiotics for eliminating and handling of specific diseases. Probiotics can be evaluated for its role and performance against isolated pathogens from contaminating sources. The present work reports on invitro antimicrobial activity of commercial selected probiotics against pathogenic microbe Vibrio parahaemolyticus. The work also describes cytotoxic activities using MTT assay and adherence studies of selected probiotics. Results for the studies showed maximum zone of inhibition 13.66±0.46mm in probiotic enteroplus,12.33±0.93mm in lactobacillus (NCIM2056) and 10.66±0.93mm in Avant Bact. Cytotoxicity was expressed as IC50(µg/ml) values, observed on CaCO cell lines for different probiotics. Avant Bact showed a IC50 value of 104.7745, Lactobacillus (NCIM2056) a value of 58.13223 and Enteroplus a value of 50.09716. These values expressed different safety aspects of probiotics used for study. Finally the adherence study was done to check probiotic colonizing capacity. The probiotics showed varied adherence capacity against caco cell lines. Enteroplus has % adhesion of 10.25±0.74, Avant Bact. 7.25±0.82 and Lactobacillus (NCIM2056) 7.5±1.12. In conclusion antimicrobial results show importance of probiotics to be used against specific gastro intestinal diseases. Cytotoxicity determines safety aspects of probiotics and adherence study determines probiotic as a promising candidate for in vivo studies.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

scholarly journals Biological Evaluation ofPupalia lappaceafor Antidiabetic, Antiadipogenic, and Hypolipidemic Activity BothIn VitroandIn Vivo

Scientifica ◽  
2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Vivek Kumar ◽  
Parag Jain ◽  
Kalpana Rathore ◽  
Zabeer Ahmed
Keyword(s):  
Cell Line ◽  
Reference Group ◽  
Lipid Level ◽  
Biological Evaluation ◽  
Diabetic Rats ◽  
Hypolipidemic Activity ◽  
Albino Rats ◽  
Reference Drug

Objective. The present study assesses the effect ofPupalia lappacea(L.) Juss. (Amaranthaceae) (PL) leaves ethanolic extract on adipocytes, blood glucose level, and lipid level in streptozotocin (STZ) induced diabetic rats.Materials and Methods. Male Albino rats were rendered diabetic by a single moderately sized dose of STZ (45 mg/kg, intraperitoneally) at once before starting the treatment. Animals were divided into five groups: normoglycemic control, diabetic control, reference group (glibenclamide, 5.0 mg/kg), AS001 (250 mg/kg extract), and AS002 (500 mg/kg extract) each containing six animals forin vivostudy. Antidiabetic and hypolipidemic activity of extract were determined byin vivomethod on STZ induced diabetic rats. Antiadipogenic activity was determined byin vitromethod on 3T3-L1 cell line in comparison to simvastatin as reference drug.Result. The extract showed significant fall in fasting serum glucose (FSG), that is, 234.68 and 211.61 mg/dL, in STZ induced diabetic animals for dose groups AS001 and AS002, respectively. ThePLextract also exhibited noteworthy antiadipogenic activity on 3T3-L1 cell line. The value of inhibitory concentration (IC50) ofPLextract to reduce adipocyte cells was found to be 662.14 μg/mL.Conclusion. ThePLextract exhibited significant antiadipogenic, antidiabetic, and hypolipidemic activities.

Synthesis and biological evaluation of novel bivalent β-carbolines as potential antitumor agents

MedChemComm ◽  
2014 ◽  
Vol 5 (7) ◽  
pp. 953-957 ◽  
Author(s):  
Qifeng Wu ◽  
Zhushuang Bai ◽  
Qin Ma ◽  
Wenxi Fan ◽  
Liang Guo ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Lewis Lung ◽  
Lewis Lung Cancer ◽  
Synthesis And Biological Evaluation ◽  
Tumor Inhibition Rate ◽  
Potential Antitumor

A series of bivalent β-carbolines with a spacer between the 3-carboxyl oxygens was synthesized and their cytotoxic activities in vitro and antitumor efficacies in vivo were evaluated. Compound 22 exhibited potent antitumor activity against Lewis lung cancer in mice with a tumor inhibition rate of 64.2%.

scholarly journals Comparative Cytotoxic Activity of Wild Harvested Stems and In Vitro-Raised Protocorms of Dendrobium chryseum Rolfe in Human Cervical Carcinoma and Glioblastoma Cell Lines

2021 ◽  
Vol 2021 ◽  
pp. 1-8
Author(s):  
Bijaya Pant ◽  
Pusp Raj Joshi ◽  
Sabitri Maharjan ◽  
Laxmi Sen Thakuri ◽  
Shreeti Pradhan ◽  
...  
Keyword(s):  
Cell Lines ◽  
Cervical Carcinoma ◽  
Significant Inhibition ◽  
Cytotoxic Activities ◽  
Naphthaleneacetic Acid ◽  
U251 Cell ◽  
Human Cervical Carcinoma ◽  
Hela Cell Lines

From the medicinal orchid Dendrobium chryseum Rolfe, which is used in traditional and folk Chinese medicine, the protocorms were raised in Murashige and Skoog (MS) media in three strengths, full strength (FMS), half strength (1/2 MS), and quarter strength (1/4 MS), with or without the phytohormones 6-benzylaminopurine (BAP) and 1-naphthaleneacetic acid (NAA) and coconut water (CW). The comparative cytotoxic activities of the wild and in vitro-raised protocorms were evaluated in human cervical carcinoma (HeLa) and human glioblastoma (U251) cell lines by MTT assay. In in vivo and in vitro, the methanol extracts of D. chryseum showed significant cytotoxic activities. Significant growth inhibition (%) and potent IC50 values were demonstrated in HeLa cell lines (49.79% (210.5 μg/mL) for in vitro-raised Dendrobium chryseum (DCT) versus 46.97% (226.5 μg/mL) for wild Dendrobium chryseum (DCW)). Similarly, activities against U251 cell lines exhibited also significant inhibition (28.76% (612.54 μg/mL) for DCW and 17.15% (1059.92 μg/mL) for DCT). The cytotoxic activities of both, wild and tissue-cultured samples, were superior in HeLa cells. In U251 cells, the wild sample was more active than the tissue-cultured one with a moderate cytotoxic effect. Hence, protocorm culture may therefore be a promising future tool for producing pharmacologically bioactive compounds in medicinal orchids. Such sustainable technology approach will minimize the pressure on the natural population of threatened but commercially important medicinal orchids.

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