scholarly journals Tris-(2-pyridyl)-pyrazolyl Borate Zinc(II) Complexes: Synthesis, DNA/Protein Binding and In Vitro Cytotoxicity Studies

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7341
Author(s):  
Manmath Narwane ◽  
Dorothy Priyanka Dorairaj ◽  
Yu-Lun Chang ◽  
Ramasamy Karvembu ◽  
Yu-Han Huang ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Binding Mode ◽  
In Vitro Cytotoxicity ◽  
Visible Absorption ◽  
Cytotoxicity Studies ◽  
Ic50 Values ◽  
State Behaviour ◽  
Analytical Tools ◽  
Ct Dna

Zn(II) complexes bearing tris[3-(2-pyridyl)-pyrazolyl] borate (Tppy) ligand (1–3) was synthesized and examined by spectroscopic and analytical tools. Mononuclear [TppyZnCl] (1) has a Zn(II) centre with one arm (pyrazolyl-pyridyl) dangling outside the coordination sphere which is a novel finding in TppyZn(II) chemistry. In complex [TppyZn(H2O)][BF4] (2) hydrogen bonding interaction of aqua moiety stabilizes the dangling arm. In addition, solution state behaviour of complex 1 confirms the tridentate binding mode and reactivity studies show the exogenous axial substituents used to form the [TppyZnN3] (3). The complexes (1–3) were tested for their ability to bind with Calf thymus (CT) DNA and Bovine serum albumin (BSA) wherein they revealed to exhibit good binding constant values with both the biomolecules in the order of 104–105 M−1. The intercalative binding mode with CT DNA was confirmed from the UV-Visible absorption, viscosity, and ethidium bromide (EB) DNA displacement studies. Further, the complexes were tested for in vitro cytotoxic ability on four triple-negative breast cancer (TNBC) cell lines (MDA-MB-231, MDA-MB-468, HCC1937, and Hs 578T). All three complexes (1–3) exhibited good IC50 values (6.81 to 16.87 μM for 24 h as seen from the MTS assay) results which indicated that these complexes were found to be potential anticancer agents against the TNBC cells.

Recent Advances in Curcumin Nanocarriers for the Treatment of Different Types of Cancer with Special Emphasis on In Vitro Cytotoxicity and Cellular Uptake Studies

2020 ◽  
Vol 10 (5) ◽  
pp. 577-590
Author(s):  
Jai B. Sharma ◽  
Shailendra Bhatt ◽  
Asmita Sharma ◽  
Manish Kumar
Keyword(s):  
Cancer Cells ◽  
Cellular Uptake ◽  
Anticancer Agents ◽  
Targeted Delivery ◽  
In Vitro Cytotoxicity ◽  
Curcumin Nanoparticles ◽  
Cytotoxicity Studies ◽  
Delivery Technique ◽  
Different Types

Background: The potential use of nanocarriers is being explored rapidly for the targeted delivery of anticancer agents. Curcumin is a natural polyphenolic compound obtained from rhizomes of turmeric, belongs to family Zingiberaceae. It possesses chemopreventive and chemotherapeutic activity with low toxicity in almost all types of cancer. The low solubility and bioavailability of curcumin make it unable to use for the clinical purpose. The necessity of an effective strategy to overcome the limitations of curcumin is responsible for the development of its nanocarriers. Objective: This study is aimed to review the role of curcumin nanocarriers for the treatment of cancer with special emphasis on cellular uptake and in vitro cytotoxicity studies. In addition to this, the effect of various ligand conjugated curcumin nanoparticles on different types of cancer was also studied. Methods: A systematic review was conducted by extensively surfing the PubMed, science direct and other portals to get the latest update on recent development in nanocarriers of curcumin. Results: The current data from recent studies showed that nanocarriers of curcumin resulted in the targeted delivery, higher efficacy, enhanced bioavailability and lower toxicity. The curcumin nanoparticles showed significant inhibitory effects on cancer cells as compared to free curcumin. Conclusion: It can be concluded that bioavailability of curcumin and its cytotoxic effect to cancer cells can be enhanced by the development of curcumin based nanocarriers and it was found to be a potential drug delivery technique for the treatment of cancer.

scholarly journals In vitro anti-inflammatory and cytotoxicity studies of two mangrove associated lichens, Dirinaria consimilis and Ramalina leiodea extracts

2018 ◽  
Vol 10 (1) ◽  
pp. 16-26 ◽  
Author(s):  
Vinay Bharadwaj Tatipamula ◽  
Girija Sastry Vedula
Keyword(s):  
Ethyl Acetate ◽  
Anticancer Agents ◽  
Protein Denaturation ◽  
Cytotoxicity Activity ◽  
Low Degree ◽  
Cytotoxicity Studies ◽  
Ic50 Values ◽  
Anti Inflammatory ◽  
Cancer Outcome

Plan: To evaluate the anti-inflammatory and cytotoxicity activity of different extracts from two different manglicolous lichens (Dirinaria consimilis and Ramalina leiodea). Preface: Inflammation is the origin of several deadly diseases like cancer, atherosclerosis, Alzheimer’s and rheumatoid arthritis. From decades, lichen extracts and its metabolites are well known in treating inflammation and cancer. Outcome: The outcome of protein denaturation method confirmed that the ethyl acetate and acetone extract of R. leiodea depicted better inhibitory profile against protein denaturation with IC50 values of 268 and 330 µg/mL Furthermore, the results of SRB assay showed that ethyl acetate and acetone extracts of both the lichens acts potently against MCF-7, DLD-1, HeLa and A549. Simultaneously, all the tested extracts depicted the low degree of specificity towards NHME, they are less toxic. Hence, further screening of these extracts may lead to the exploration of safe and potent anti-inflammatory and anticancer agents.

scholarly journals Synthesis of Novel Benzamide- piperazine-sulfonamide Hybrids as Potential Anticancer Agents

2019 ◽  
Vol 92 (3) ◽  
pp. 393-402
Author(s):  
B. Ramalingeswara Rao ◽  
Mohana Rao Katiki ◽  
Dileep Kommula ◽  
SaiShyam Narayanan ◽  
Ruby John Anto ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
In Vitro Cytotoxicity ◽  
Sensitive Cell Line ◽  
Human Cancer Cell Lines ◽  
Ic50 Values ◽  
Different Origins ◽  
New Compounds ◽  
A549 Lung

The synthesis of a series of substituted hippuric acid (2-benzamidoacetic acid) derivatives containing arylsulfonylpiperazine nucleus (3a–j, 4a–j) is described. The compounds were synthesized by coupling hippuric/4-fluorohippuric acid with various arylsulfonylpiperazines using N-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI). The structures of all the new compounds were confirmed by IR, NMR and MS spectral data. All the synthesized compounds have been evaluated for their in vitro cytotoxicity towards five human cancer cell lines of different origins viz. HeLa (Cervical), A549 (Lung), A375 (Skin), MD-AMB-231(Breast) and T98G (brain) and their IC50 values were determined. Among the compounds tested, 3b, 3d, 3g, 4c and 4e displayed significant cytotoxic activity (IC50 = 24.2–38.2 µM). T98G was the most sensitive cell line towards the compounds studied followed by HeLa, A375, A549 and MD-AMB-231.

Design of Oleanolic Acid-Based Hybrid Compounds as Potential Pharmaceutical Scaffolds

2021 ◽  
Vol 18 ◽  
Author(s):  
Vuyolwethu Khwaza ◽  
Opeoluwa Oyehan Oyedeji ◽  
Blessing Atim Aderibigbe ◽  
Eric Morifi ◽  
Youmbi Thierry Fonkui ◽  
...  
Keyword(s):  
Oleanolic Acid ◽  
Klebsiella Oxytoca ◽  
In Vitro Cytotoxicity ◽  
Hybrid Compounds ◽  
Sulforhodamine B ◽  
Cytotoxicity Studies ◽  
Sulforhodamine B Assay ◽  
Ic50 Values ◽  
Further Development

Background: Infectious diseases as well as cancer are the leading causes of death worldwide. Drug resistance usually results in their treatment requiring a combination of two or more drugs. Objective: Oleanolic-based hybrid compounds were prepared via esterification and characterized using FTIR, NMR, and LC-MS. In vitro antibacterial and in vitro cytotoxicity studies were performed. Method: Oleanolic acid was hybridized with selected known pharmaceutical scaffolds via the carboxylic acid functionality to develop therapeutics with increased biological activity. Antibacterial activity was determined using the micro-dilution assay against selected Gram-positive and Gram-negative bacteria and cytotoxicity using the sulforhodamine B assay. Results: Compound 8 displayed potent antibacterial effect against five strains of bacteria such as Bacillus subtilis, Staphylococcus aureus, Proteus vulgaris, Klebsiella oxytoca, and Escherichia coli with MIC values of 1.25, 0.078, 0.078, 1.25, 1.25 mg/mL when compared to the control, oleanolic acid (MIC = 2.5 mg/mL). Furthermore, in vitro cytotoxicity, as determined using the SRB assay, against selected cancer cells revealed that compound 7 was the most cytotoxic to MDA, DU145, and MCF-7 cell lines with IC50 values of 69.87±1.04, 73.2±1.08, and 85.27±1.02 µg/mL, respectively, than oleanolic acid with an IC50 ˃200 µg/mL. Conclusion: Hybridization of oleanolic acids was successful, and further development of these potential antibacterial compounds with reduced cytotoxicity is warranted.

Binuclear ruthenium(II) complexes of 4,4′-azopyridine bridging ligand as anticancer agents: synthesis, characterization, and in vitro cytotoxicity studies

2019 ◽  
Vol 72 (16) ◽  
pp. 2617-2635 ◽  
Author(s):  
Priyanka Khanvilkar ◽  
Ramadevi Pulipaka ◽  
Kavita Shirsath ◽  
Ranjitsinh Devkar ◽  
Debjani Chakraborty
Keyword(s):  
Anticancer Agents ◽  
In Vitro Cytotoxicity ◽  
Bridging Ligand ◽  
Cytotoxicity Studies

The Effect of Phase Transition Temperature on Therapeutic Efficacy of Liposomal Bortezomib

2020 ◽  
Vol 20 (6) ◽  
pp. 700-708
Author(s):  
Mitra Korani ◽  
Sara Nikoofal-Sahlabadi ◽  
Amin R. Nikpoor ◽  
Solmaz Ghaffari ◽  
Hossein Attar ◽  
...  
Keyword(s):  
Side Effects ◽  
Cell Line ◽  
Therapeutic Efficacy ◽  
Drug Loading ◽  
Particle Diameter ◽  
In Vitro Cytotoxicity ◽  
Liposomal Formulations ◽  
Cytotoxicity Studies ◽  
Anti Tumor Activity

Aims: Here, three liposomal formulations of DPPC/DPPG/Chol/DSPE-mPEG2000 (F1), DPPC/DPPG/Chol (F2) and HSPC/DPPG/Chol/DSPE-mPEG2000 (F3) encapsulating BTZ were prepared and characterized in terms of their size, surface charge, drug loading, and release profile. Mannitol was used as a trapping agent to entrap the BTZ inside the liposomal core. The cytotoxicity and anti-tumor activity of formulations were investigated in vitro and in vivo in mice bearing tumor. Background: Bortezomib (BTZ) is an FDA approved proteasome inhibitor for the treatment of mantle cell lymphoma and multiple myeloma. The low solubility of BTZ has been responsible for the several side effects and low therapeutic efficacy of the drug. Encapsulating BTZ in a nano drug delivery system; helps overcome such issues. Among NDDSs, liposomes are promising diagnostic and therapeutic delivery vehicles in cancer treatment. Objective: Evaluating anti-tumor activity of bortezomib liposomal formulations. Methods: Data prompted us to design and develop three different liposomal formulations of BTZ based on Tm parameter, which determines liposomal stiffness. DPPC (Tm 41°C) and HSPC (Tm 55°C) lipids were chosen as variables associated with liposome rigidity. In vitro cytotoxicity assay was then carried out for the three designed liposomal formulations on C26 and B16F0, which are the colon and melanoma cancer mouse-cell lines, respectively. NIH 3T3 mouse embryonic fibroblast cell line was also used as a normal cell line. The therapeutic efficacy of these formulations was further assessed in mice tumor models. Result: MBTZ were successfully encapsulated into all the three liposomal formulations with a high entrapment efficacy of 60, 64, and 84% for F1, F2, and F3, respectively. The findings showed that liposomes mean particle diameter ranged from 103.4 to 146.8nm. In vitro cytotoxicity studies showed that liposomal-BTZ formulations had higher IC50 value in comparison to free BTZ. F2-liposomes with DPPC, having lower Tm of 41°C, showed much higher anti-tumor efficacy in mice models of C26 and B16F0 tumors compared to F3-HSPC liposomes with a Tm of 55°C. F2 formulation also enhanced mice survival compared with untreated groups, either in BALB/c or in C57BL/6 mice. Conclusion: Our findings indicated that F2-DPPC-liposomal formulations prepared with Tm close to body temperature seem to be effective in reducing the side effects and increasing the therapeutic efficacy of BTZ and merits further investigation.

Sign in / Sign up

Export Citation Format

Share Document