scholarly journals Biological Activities of NHC–Pd(II) Complexes Based on Benzimidazolylidene N-heterocyclic Carbene (NHC) Ligands Bearing Aryl Substituents

Catalysts ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1190
Author(s):  
Ibrahim Al Nasr ◽  
Nedra Touj ◽  
Waleed Koko ◽  
Tariq Khan ◽  
Ismail Özdemir ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Leishmania Major ◽  
Biological Activities ◽  
Vero Cells ◽  
Spectroscopic Techniques ◽  
Biological Assays ◽  
Drug Candidates ◽  
Highly Active ◽  
Antileishmanial Activities

N-heterocyclic carbene (NHC) precursors (2a–i), their pyridine-enhanced precatalyst preparation stabilization and initiation (PEPPSI)-themed palladium N-heterocyclic carbene complexes (3a–i) and palladium N-heterocyclic triphenylphosphines complexes (4a–i) were synthesized and characterized by elemental analysis and 1H NMR, 13C NMR, IR, and LC–MS spectroscopic techniques. The (NHC)Pd(II) complexes 3–4 were tested against MCF7 and MDA-MB-231 cancer cells, Escherichia coli, methicillin-resistant Staphylococcus aureus (MRSA), Candida albicans microorganisms, Leishmania major promastigotes and amastigotes, Toxoplasma gondii parasites, and Vero cells in vitro. The biological assays indicated that all compounds are highly active against cancer cells, with an IC50 < 1.5 µg mL−1. Eight compounds proved antibacterial and antileishmanial activities, while only three compounds had strong antifungal activities against C. albicans. In our conclusion, compounds 3 (b, f, g, and h) and 4b are the most suitable drug candidates for anticancer, antimicrobial, and antiparasitical.

scholarly journals Synthesis of 4-substituted ethers of benzophenone and their antileishmanial activities

2018 ◽  
Vol 5 (5) ◽  
pp. 171771 ◽  
Author(s):  
◽  
Faiza Ahad ◽  
Nida Ghouri ◽  
Khalid Mohammed Khan ◽  
Shahnaz Perveen ◽  
...  
Keyword(s):  
Electron Impact ◽  
Leishmania Major ◽  
Spectroscopic Techniques ◽  
Resolution Electron ◽  
Electron Impact Mass ◽  
Promastigote Form ◽  
Vector Borne ◽  
Antileishmanial Activities ◽  
Synthetic Derivatives

Leishmaniasis is a vector-borne protozoan disease; it mainly originates from the bite of sandfly and initiated when parasite is transmitted to human at metacyclic flagellated promastigote form. In the current study, a synthesis of a series of 4-substituted benzophenone ethers 1–20 was carried out in good yields and their in vitro antileishmanial activities were also screened. Among synthetic derivatives, 15 compounds 1 , 3 , 5–12 , 15 and 17 – 20 showed antileishmanial activities against promastigotes of Leishmania major with IC 50 values in the range of 1.19–82.30 µg ml −1 , and the values were compared with those of the standard pentamidine (IC 50  = 5.09 ± 0.09 µg ml −1 ). Our study identified a series of new antileishmanial molecules as potential leads. Structures of these synthetic compounds were deduced by different spectroscopic techniques, such as 1 H and 13 C nuclear magnetic resonance, electron impact and high-resolution electron impact mass spectrometry and IR.

scholarly journals In vitro study of the efficacy of Solanum nigrum against Leishmania major

F1000Research ◽  
2018 ◽  
Vol 7 ◽  
pp. 1329 ◽  
Author(s):  
Christine N. Mutoro ◽  
Johnson K. Kinyua ◽  
Joseph K. Ng'ang'a ◽  
Daniel W. Kariuki ◽  
Johnstone M. Ingonga ◽  
...  
Keyword(s):  
Leishmania Major ◽  
In Vitro Study ◽  
Vero Cells ◽  
Solanum Nigrum ◽  
Therapeutic Interventions ◽  
Phlebotomine Sandflies ◽  
High Concentrations ◽  
Antileishmanial Activities

Leishmania parasites (Kinetoplastida: Trypanosomatidae) are obligate intracellular parasites of macrophages that causes visceral and cutaneous leishmaniases. Currently, there is inadequate therapeutic interventions to manage this endemic tropical disease, transmitted mainly by phlebotomine sandflies hence there is need to develop affordable and effective therapeutic measures. This study determined the in vitro efficacy of Solanum nigrum methanolic and aqueous plant extracts on Leishmania major parasites.  Cytotoxic effects of the extracts were determined using vero cells and reported as percentage viability of the cells. The promastigote parasites of Leishmania major were cultured and grown for 3 days in different concentrations of extracts to determine the MIC and IC50 values. The in vitro antileishmanial efficacy was done on macrophages infected with L. major amastigote parasites and then treated with extracts in varying concentrations. The study revealed that all the test extracts had lower toxicity than control drugs, pentostam (IC50= 0.0 92 mg/ml) and amphotericin B (IC50=0.049 mg/ml).  The extracts tended to show a dose dependent cytotoxic effect which corresponded to high vero cells viability as their concentration increased.  Methanolic extract of S. nigrum from Kisii seemed to be more efficacious in vitro since it knocked out the promastigotes at a lower MIC level (0.5 mg/ml) when compared to all other extracts whose effective MIC level was ≥ 1 mg/ml. High concentrations of the test extracts and control drugs resulted to low infectivity and multiplication of L. major amastigotes. Findings from this study demonstrate that S. nigrum extracts have potential antileishmanial activities however; further investigation needs to be done on pure compound isolation, in vivo assays and clinical trials so as to use the promising compounds as effective antileishmanial agents.

scholarly journals Microwave Assisted Synthesis, Spectral and Antifungal Studies of 2-Phenyl-N,N′-bis(pyridin-4-ylcarbonyl)butanediamide Ligand and Its Metal Complexes

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Rayees Ahmad Shiekh ◽  
Maqsood Ahmad Malik ◽  
Shaeel Ahmed Al-Thabaiti ◽  
Mohmmad Younus Wani ◽  
Arshid Nabi
Keyword(s):  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Structural Features ◽  
Conventional Heating ◽  
Microwave Assisted Synthesis ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Drug Candidates ◽  
Highly Active

2-Phenyl-N,N′-bis(pyridin-4-ylcarbonyl)butanediamide ligand with a series of transition metal complexes has been synthesizedviatwo routes: microwave irradiation and conventional heating method. Microwave irritation method happened to be the efficient and versatile route for the synthesis of these metal complexes. These complexes were found to have the general composition M(L)Cl2/M(L)(CH3COO)2(where M = Cu(II), Co(II), Ni(II), and L = ligand). Different physical and spectroscopic techniques were used to investigate the structural features of the synthesized compounds, which supported an octahedral geometry for these complexes.In vitroantifungal activity of the ligand and its metal complexes revealed that the metal complexes are highly active compared to the standard drug. Metal complexes showed enhanced activity compared to the ligand, which is an important step towards the designing of antifungal drug candidates.

Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies

2020 ◽  
Vol 16 ◽  
Author(s):  
Mahboob Ali ◽  
Momin Khan ◽  
Khair Zaman ◽  
Abdul Wadood ◽  
Maryam Iqbal ◽  
...  
Keyword(s):  
In Silico ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Type Ii Diabetes Mellitus ◽  
Spectroscopic Techniques ◽  
Chalcone Derivatives ◽  
In Silico Studies ◽  
Wide Range

: Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biological activities. Objective: In the current study chalcone derivatives (1-17) were synthesized and evaluated their inhibitory potential against α-amylase enzyme. Method: For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by ClaisenSchmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via different spectroscopic techniques such as EI-MS, HREI-MS, 1H-, and 13C-NMR. Results: Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard commercial drug acarbose (IC50 = 1.34 ± 0.3 μM). Conclusion: Chalcone derivatives (1-17) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed that electron donating groups in the phenyl ring have more influence on enzyme inhibition. However, to insight the participation of different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) molecular modeling analyses were carried out.

Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines In Vitro

2020 ◽  
Vol 19 (16) ◽  
pp. 1949-1965 ◽  
Author(s):  
Natalia Szkaradek ◽  
Daniel Sypniewski ◽  
Dorota Żelaszczyk ◽  
Sabina Gałka ◽  
Paulina Borzdziłowska ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Higher Plants ◽  
Biological Activities ◽  
Human Tumor ◽  
Plant Metabolites ◽  
Xtt Assay ◽  
Treatment Protocols

Background: Natural plant metabolites and their semisynthetic derivatives have been used for years in cancer therapy. Xanthones are oxygenated heterocyclic compounds produced as secondary metabolites by higher plants, fungi or lichens. Xanthone core may serve as a template in the synthesis of many derivatives that have broad biological activities. Objective: This study synthesized a series of 17 new xanthones, and their anticancer potential was also evaluated. Methods: The anticancer potential was evaluated in vitro using a highly invasive T24 cancer cell line. Direct cytotoxic effects of the xanthones were established by IC50 estimation based on XTT assay. Results: 5 compounds of the total 17 showed significant cytotoxicity toward the studied cancer cultures and were submitted to further detailed analysis, including studies examining their influence on gelatinase A and B expression, as well as on the cancer cells migration and adhesion to an extracellular matrix. These analyses were carried out on five human tumor cell lines: A2780 (ovarian cancer), A549 (lung cancer), HeLa (cervical cancer), Hep G2 (liver cancer), and T24 (urinary bladder cancer). All the compounds, especially 4, showed promising anticancer activity: they exhibited significant cytotoxicity towards all the evaluated cell lines, including MCF-7 breast cancer, and hindered migration-motility activity of cancer cells demonstrating more potent activity than α-mangostin which served as a reference xanthone. Conclusion: These results suggest that our xanthone derivatives may be further analyzed in order to include them in cancer treatment protocols.

scholarly journals In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Sospeter N. Njeru ◽  
Jackson M. Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extract ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

Phytochemical concentrations and biological activities of Sorghum bicolor alcoholic extracts

2016 ◽  
Vol 7 (8) ◽  
pp. 3410-3420 ◽  
Author(s):  
Vermont P. Dia ◽  
Philipus Pangloli ◽  
Lynsey Jones ◽  
Angela McClure ◽  
Anjali Patel
Keyword(s):  
Ovarian Cancer ◽  
Antioxidant Activity ◽  
Sorghum Bicolor ◽  
Cancer Cells ◽  
Biological Activities ◽  
Ovarian Cancer Cells

Sorghum alcoholic extracts exhibited antioxidant activity and capability to inhibit and chemosensitize ovarian cancer cells in vitro.

scholarly journals Caspofungin and LTX-315 inhibit SARS-CoV-2 replication by targeting the nsp12 polymerase

2020 ◽  
Author(s):  
Min Wang ◽  
Fei Ye ◽  
Jiaqi Su ◽  
Jingru Zhao ◽  
Bin Yuan ◽  
...  
Keyword(s):  
Severe Acute Respiratory Syndrome ◽  
Vero Cells ◽  
Polymerase Activity ◽  
Structural Protein ◽  
Live Virus ◽  
Drug Candidates ◽  
Virtual Screen ◽  
Virus Assay ◽  
Promising Target

Abstract The ongoing severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2, previously designated as 2019-nCoV) outbreak has caused global concern1. Currently, there are no clinically approved specific drugs or vaccines available for this virus. The viral polymerase is a promising target for developing broad- spectrum antiviral drugs. Here, based on the highly similar structure of SARS- CoV non-structural protein 12 (nsp12) polymerase subunit2, we applied virtual screen for the available compounds, including both the FDA-approved and under- clinic drugs, to identify potential antiviral molecules against SARS-CoV-2. We found two drugs, the clinically approved anti-fungi drug Caspofungin Acetate (Cancidas) and the oncolytic peptide LTX-315, can bind SARS-CoV-2 nsp12 protein to block the polymerase activity in vitro. Further live virus assay revealed that both Caspofungin Acetate and LTX-315 can effectively inhibit SARS-CoV-2 replication in vero cells. These findings present promising drug candidates for treatment of related diseases and would also stimulate the development of pan- coronavirus antiviral agents.Authors Min Wang, Fei Ye, Jiaqi Su, Jingru Zhao, and Bin Yuan contributed equally to this work.

scholarly journals Salvia ceratophylla L. from South of Jordan: new insights on chemical composition and biological activities

2020 ◽  
Vol 10 (5) ◽  
pp. 307-316
Author(s):  
Mohammad Sanad Abu-Darwish ◽  
Célia Cabral ◽  
Zulfigar Ali ◽  
Mei Wang ◽  
Shabana I. Khan ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Gas Chromatography ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Vero Cells ◽  
Gas Chromatography Mass Spectrometry ◽  
No Production ◽  
Main Constituent ◽  
Microbial Infections

Abstract In Jordan, Salvia ceratophylla L. is traditionally used in the treatment of cancer, microbial infections, and urinary disorders. This study aimed: (1) to chemically characterize S. ceratophylla essential oil (EO) from South Jordan, by gas chromatography (GC) and gas chromatography-mass spectrometry (GC–MS); and (2) to evaluate in vitro the cytotoxic, anti-inflammatory, and antiprotozoal activities of the EO, it’s predominant components, and the hexane (A), ethyl acetate (B), methanol (C) and crude-methanol extracts (D). The analysis revealed that the EO has 71 compounds, with linalool (54.8%) as main constituent. Only the hexane extract (A) showed some cytotoxic activity against SK-MEL, KB, BT-549, SK-OV-3, LLC-PK1 and VERO cells lines with IC50 between 60 and > 100 µg/mL. The EO inhibited NO production (IC50 90 µg/mL) and NF-κB activity (IC50 38 µg/mL). The extracts A, B, and D inhibited NO production and NF- κB activity with IC50 between 32 and 150 µg/mL. Linalool considerably inhibited NO production (IC50 18 µg/mL). The extracts tested did not exhibit antileishmanial activity. Regarding antitrypanosomal activity, the EO exhibited significant results with IC50 2.65 µg/mL. In conclusion, Jordan S. ceratophylla EO represents a rich source of linalool and bears a promising therapeutic potential for further antitrypanosomal drug development.

Antileishmanial activities of leaf latex and compound isolated from Aloe ghibensis Sebsebe & Friis

2020 ◽  
Vol 35 (1) ◽  
pp. 51-58
Author(s):  
Tamirat Tekassa ◽  
Yitagesu Tewabe ◽  
Daniel Bisrat ◽  
Asrat Hailu ◽  
Kaleab Asres
Keyword(s):  
Leishmania Donovani ◽  
Leishmania Species ◽  
2D Nmr ◽  
Antileishmanial Activity ◽  
Spectroscopic Techniques ◽  
Monocytic Cell ◽  
Monocytic Cell Line ◽  
Phytochemical Constituents ◽  
Antileishmanial Activities

Aloe ghibensis Sebsebe & Friis is traditionally used in Ethiopia for the treatment of various ailments including skin problem, wounds and malaria. Phytochemical constituents and antileshimanial properties of the leaf latex of A. ghibensis have not been reported. The objective of this study was, therefore, to determine the phytochemical constituents and in vitro antileishmanial activities of the leaf latex of A. ghibensis and its major compounds against two Leishmania species. Preparative TLC was used to isolate compounds from the leaf latex of A. ghibensis and spectroscopic techniques including 1D- and 2D-NMR as well as ESI-MS were employed to elucidate structures of the isolated compounds. In vitro antileishmanial activity was performed against promastigotes and axenically cultured amastigotes of Leishmania aethiopica and Leishmania donovani clinical isolates using Alamar Blue assay. Phytochemical investigation led to the isolation of two major anthrones, identified as aloin A/B and 7-hydroxyaloin A/B. Both the leaf latex of A. ghibensis and isolated compounds showed antileishmanial activity with IC50 values ranging from 1.6 ± 0.43 to 3.64 ± 0.09 µg/ml and 1.87 ± 0.21 to 3.72 ± 0.12 against promastigotes and axenically cultured amastigotes of L. aethopica and L. donovani, respectively. Moreover, the test substances were found to be less toxic (LC50 = 145 ± 0.72 to 156 ± 0.08 µg/ml) than amphotericin B (LC50 = 12.11 ± 0.51 µg/ml) towards human monocytic cell line (THP-1). The present study revealed that the latex and pure compounds possess genuine antileishmanial activity with high selectivity indices (SIs). Therefore, the isolated compounds can be used as a scaffold for the development of effective drugs for leishmaniasis.  

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