scholarly journals Therapeutic Potential of Hispidin—Fungal and Plant Polyketide

2021 ◽  
Vol 7 (5) ◽  
pp. 323
Author(s):  
Kseniia A. Palkina ◽  
Daria A. Ipatova ◽  
Ekaterina S. Shakhova ◽  
Anastasia V. Balakireva ◽  
Nadezhda M. Markina
Keyword(s):  
Metabolic Syndrome ◽  
Cancer Cell ◽  
Therapeutic Potential ◽  
Cell Activity ◽  
Viral Diseases ◽  
Fungal Metabolite ◽  
Cholesterol Lowering ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Secondary Plant

There is a large number of bioactive polyketides well-known for their anticancer, antibiotic, cholesterol-lowering, and other therapeutic functions, and hispidin is among them. It is a highly abundant secondary plant and fungal metabolite, which is investigated in research devoted to cancer, metabolic syndrome, cardiovascular, neurodegenerative, and viral diseases. This review summarizes over 20 years of hispidin studies of its antioxidant, anti-inflammatory, anti-apoptotic, antiviral, and anti-cancer cell activity.

C5-curcuminoid-dithiocarbamate based molecular hybrids: synthesis and anti-inflammatory and anti-cancer activity evaluation

RSC Advances ◽  
2014 ◽  
Vol 4 (54) ◽  
pp. 28756-28764 ◽  
Author(s):  
Amit Anthwal ◽  
Kundan Singh ◽  
M. S. M. Rawat ◽  
Amit K. Tyagi ◽  
Bharat B. Aggarwal ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Activity Evaluation ◽  
Anti Cancer ◽  
Molecular Hybrids ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Cancer Activity ◽  
Proliferation Potential

The C5-curcumin-dithiocarbamate analogues were synthesized in search of new molecules with anti-proliferation potential against cancer cells. These new compounds demonstrated higher anti-proliferation and anti-inflammatory activity against cancer cell lines in comparison to curcumin.

scholarly journals Pro- and Anti-Inflammatory Cytokine Expression Levels in Macrophages; An Approach to Develop Indazolpyridin-methanones as Novel Inflammation Medication

2020 ◽  
Vol 19 (4) ◽  
pp. 425-435 ◽  
Author(s):  
Manikandan Alagumuthu ◽  
Vanshika Srivastava ◽  
Manisha Shah ◽  
Sivakumar Arumugam ◽  
Mohandoss Sonaimuthu ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Lines ◽  
Cancer Cell ◽  
Inflammatory Cytokine ◽  
Cancer Cell Lines ◽  
Tnf Α ◽  
Anti Cancer ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Anti Inflammatory Cytokine

Background: Macrophages play a serious part in the instigation, upkeep, and resolution of inflammation. They are activated or deactivated during inflammation progression. Activation signals include cytokines (IF-γ, granulocyte-monocyte colonystimulating factor (GM-CSF), and TNF-α), extracellular matrix proteins, and other chemical mediators. Activated macrophages are deactivated by anti-inflammatory cytokines (IL- 10 and TGF-β (transforming growth factor-beta) and cytokine antagonists that are mainly produced by macrophages. Based on this, the present study aimed to develop novel (E)- Benzylidene-indazolpyridin methanones (Cpd-1-10) as effective anti-inflammatory agents by analyzing pro- and anti-inflammatory cytokine levels in macrophages. Objectives: To determine the anti-inflammatory effect of indazolpyridin-methanones by examining pro- and anti-inflammatory interleukin levels in J77A.1 macrophages. Methods: Expression of cytokines such as TNF-α, IL-1β, IL-6 and IL-10 serum levels measured by ELISA method. Anti-cancer and cytotoxicity studies were carried out by MTT assay. COX-2 seems to be associated with cancers and atypical developments in the duodenal tract. So, a competitive ELISA based COX-2 inhibition assay was done. To validate the inhibitory potentials and to get more insight into the interaction of COX-2 with Cpd1-10, molecular docking was performed. Results: Briefly, the COX-2 inhibitory relative activity was found to be in between the range of 80-92% (Diclofenac showed 84%, IC50 0.95 μM). Conclusion: Cytotoxicity effect of the compounds against breast cancer cell lines found excellent and an extended anticancer study ensured that these compounds are also alternative therapeutic agents against breast cancer. Among all the tested cancer cell lines, the anti- cancer effect on breast cancer was exceptional for the most active compounds Cpd5 and Cpd9.

Synthesis and Evaluation of 198Au/PAMAM-MPEG-FA against Cancer Cells

2020 ◽  
Vol 20 (10) ◽  
pp. 1250-1265
Author(s):  
Reza Rezaei ◽  
Simin Janitabar Darzi ◽  
Mahnaz Yazdani
Keyword(s):  
Breast Cancer ◽  
Cancer Cell ◽  
Therapeutic Potential ◽  
Analytical Techniques ◽  
Cell Uptake ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Clinical Investigations ◽  
Anti Cancer

Background: There is a significant dearth of clinical biochemistry researches to evaluate the facility of exploitation of folate targeted radioactive gold-labeled anti-cancer drugs against various cancer cell lines. Objective: The aim of this paper was to develop a gold-based compound with an efficient therapeutic potential against breast cancer. To this end, the synthesis of the 198Au/PAMAM-MPEG-FA composite was considered here. Methods: The radioactive gold (198Au) nanoparticles were encapsulated into Folic acid (FA)-targeted Polyamidoamine dendrimer (PAMAM) modified with Maleimide-Polyethylene glycol Succinimidyl Carboxymethyl ester (MPEG). After that, anticancer assessments of the prepared 198Au/PAMAM-MPEG-FA hybrid mater against breast cancer were investigated. : Further studies were also devised to compare the anticancer capabilities of the 198Au/PAMAM-MPEG-FA composite with the synthesized P-MPEG, 197Au/P-MPEG, 197Au/P-MPEG-FA, 197Au/P-FA and 198Au/P-MPEG-FA conjugates. The prepared drugs were characterized by means of various analytical techniques. The radionuclidic purity of the 198Au/P-MPEG-FA solution was determined using High Purity Germanium (HPGe) spectroscopy and its stability in the presence of human serum was studied. The cell uptake and toxicity of the prepared drugs were evaluated in vitro, and some comparative studies of the toxicity of the drugs were conducted towards the MCF7 (Human breast cancer cell), 4T1 (Mice breast adenocarcinoma cell) and C2C12 (Mice muscle normal cell). Results: The results showed that cell uptake of 198Au/P-MPEG-FA nanoparticles is high in the 4T1 cell line and the order of uptake is as 4T1> MCF7> C2C12. Moreover, of the tested compounds, 198Au/P-MPEG-FA had the highest toxicity towards the cancerous 4T1 and MCF7 in all concentrations after 24, 48 and 72h (P < 0.001). Furthermore, the cytotoxicity of the drugs was concentration-dependent. Conclusion: On the basis of the present research, 198Au/P-MPEG-FA has been proposed as a good candidate for the induction of cell death in breast cancer, although further experimental and clinical investigations are required.

Synthesis and anti-cancer cell activity of pseudo-ginsenoside Rh2

Steroids ◽  
2014 ◽  
Vol 92 ◽  
pp. 1-6 ◽  
Author(s):  
Guangtao Qian ◽  
Zhicai Wang ◽  
Jinyu Zhao ◽  
Dandan Li ◽  
Wei Gao ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Cell Activity ◽  
Ginsenoside Rh2 ◽  
Anti Cancer

scholarly journals LHH1, a novel antimicrobial peptide with anti-cancer cell activity identified from Lactobacillus casei HZ1

AMB Express ◽  
2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Jun-Fang He ◽  
Du-Xin Jin ◽  
Xue-Gang Luo ◽  
Tong-Cun Zhang
Keyword(s):  
Staphylococcus Aureus ◽  
Cell Membrane ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Lactobacillus Casei ◽  
Laser Scanning ◽  
Cell Activity ◽  
Antimicrobial Activities ◽  
Confocal Laser ◽  
Anti Cancer

Abstract Antimicrobial peptides have been attracting increasing attention for their multiple beneficial effects. In present study, a novel AMP with a molecular weight of 1875.5 Da, was identified from the genome of Lactobacillus casei HZ1. The peptide, which was named as LHH1 was comprised of 16 amino acid residues, and its α-helix content was 95.34% when dissolved in 30 mM SDS. LHH1 exhibited a broad range of antimicrobial activities against Gram-positive bacteria and fungus. It could effectively inhibit Staphylococcus aureus with a minimum inhibitory concentration of 3.5 μM and showed a low hemolytic activity. The scanning electron microscope, confocal laser scanning microscope and flow cytometry results showed that LHH1 exerted its antibacterial activity by damaging the cell membrane of Staphylococcus aureus. Meanwhile, LHH1 also exhibited anti-cancer cell activities against several cancer cells via breaking the cell membrane of MGC803, HCT116 and C666-1 cancer cells.

scholarly journals Identification of a novel toxicophore in anti-cancer chemotherapeutics that targets mitochondrial respiratory complex I

eLife ◽  
2020 ◽  
Vol 9 ◽  
Author(s):  
Zoe A Stephenson ◽  
Robert F Harvey ◽  
Kenneth R Pryde ◽  
Sarah Mistry ◽  
Rachel E Hardy ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Complex I ◽  
Cell Activity ◽  
High Energy ◽  
Cardiac Cells ◽  
Respiratory Complex ◽  
Mitochondrial Respiratory Complex ◽  
Anti Cancer ◽  
Respiratory Complex I ◽  
Mitochondrial Respiratory

Disruption of mitochondrial function selectively targets tumour cells that are dependent on oxidative phosphorylation. However, due to their high energy demands, cardiac cells are disproportionately targeted by mitochondrial toxins resulting in a loss of cardiac function. An analysis of the effects of mubritinib on cardiac cells showed that this drug did not inhibit HER2 as reported, but directly inhibits mitochondrial respiratory complex I, reducing cardiac-cell beat rate, with prolonged exposure resulting in cell death. We used a library of chemical variants of mubritinib and showed that modifying the 1H-1,2,3-triazole altered complex I inhibition, identifying the heterocyclic 1,3-nitrogen motif as the toxicophore. The same toxicophore is present in a second anti-cancer therapeutic carboxyamidotriazole (CAI) and we demonstrate that CAI also functions through complex I inhibition, mediated by the toxicophore. Complex I inhibition is directly linked to anti-cancer cell activity, with toxicophore modification ablating the desired effects of these compounds on cancer cell proliferation and apoptosis.

scholarly journals Cannabidiol – characteristic and application in cosmetology and dermatology

2021 ◽  
Vol 10 (6) ◽  
pp. 299-303
Author(s):  
Mirosława Grymel ◽  
◽  
Patrycja Grabiec ◽  
Kamila Nurkowska ◽  
◽  
...  
Keyword(s):  
Mental Disorders ◽  
Therapeutic Potential ◽  
Biological Properties ◽  
Active Ingredients ◽  
Anti Cancer ◽  
Anti Inflammatory

Cannabidiol (CBD) is one of the main active ingredients in hemp. It shows a number of valuable biological properties, such as anti-cancer, anti-depressant or anti-inflammatory. The aim of the article was to present the most importantproperties of cannabidiol and its possible application in cosmetology and dermatology. The wide therapeutic potential of CBD makes it possible to use in the treatment of, not only cancer or mental disorders, but also many dermatoses.

Probing into Therapeutic Anti-cancer Potential of Apigenin: Recent Trends and Future Directions

2019 ◽  
Vol 13 (2) ◽  
pp. 124-133
Author(s):  
Ajay Sharma ◽  
Abdul Ghani ◽  
Katrin Sak ◽  
Hardeep S. Tuli ◽  
Anil K. Sharma ◽  
...  
Keyword(s):  
Natural Products ◽  
Therapeutic Potential ◽  
Therapeutic Option ◽  
Cancer Therapies ◽  
Future Directions ◽  
Anti Cancer ◽  
Recent Trends ◽  
Anti Inflammatory ◽  
Key Terms

Background: Natural products represent a therapeutic option for the treatment of inflammation- associated diseases. Flavonoids which are one of the special categories of such natural products, have previously shown promising therapeutic potential. Objectives: The current review discusses the synthetic preview and anti-inflammatory potential of apigenin along with the underlying molecular mechanism in chronic human diseases especially cancer. In addition, the relevant patents on the therapeutic potential of apigenin have also been mentioned. Methods: A literature search was carried out using PubMed/Science, Google Scholar, etc. which was further expended by the different combination of keywords: apigenin, inflammation, mechanism, therapeutic potential, cancer, etc. Patent information was retrieved by searching the key terms: apigenin, inflammation, therapeutic potential from various databanks including Espacenet, Google Patents, Free Patents Online and Mendeley of WIPO, USPTO, SIPO, JPO, KIPO and EPO databases. Results: A total of 76 references have been found relevant with the theme of the manuscript. These citations have described recent ongoing advances in the area of inflammation and cancer with respect to apigenin. Conclusion: Studies related to the anti-inflammatory and anticancer potential of apigenin have been explored through this review article. Moreover, the patent analysis of apigenin has further strengthened its therapeutic role. Probing into the therapeutic properties of apigenin, further adds value to this molecule in terms of its downregulation of major inflammatory and cancer-associated signaling pathways. The article would simultaneously assist the scientific community to precisely understand the role of apigenin and design novel anti-cancer therapies.

scholarly journals PVA coating of ferrite nanoparticles triggers pH-responsive release of 5-fluorouracil in cancer cells

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Sanele Mngadi ◽  
Moganavelli Singh ◽  
Seipati Mokhosi
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Targeted Delivery ◽  
Colloidal Stability ◽  
Therapeutic Potential ◽  
Cancer Cell Lines ◽  
Ferrite Nanoparticles ◽  
Cancer Drug ◽  
Anti Cancer

Abstract The use of magnetic nanoparticles (MNPs) has transformed both diagnostics and therapeutic approaches in cancer treatment. Along with developing novel anti-cancer drugs with high therapeutic potential, researchers are exploring innovative strategies for more targeted delivery in order to alleviate the associated potent side effects. In this study, we describe the synthesis of Mg0.5Co0.5Fe2O4 ferrite nanoparticles, their functionalisation with polyvinyl alcohol (PVA), and encapsulation of the anti-cancer drug 5-fluorouracil (5-FU). Functionalised nanoparticles viz. PVA-Mg0.5Co0.5Fe2O4 -5-FU displayed desirable physiochemical properties with regards to the spherical shape, hydrodynamic sizes of <120 nm and relative colloidal stability of up to <−33 mV. The drug encapsulating efficiency was found to be 68%. In vitro cytotoxicity profiles were determined using the MTT and SRB assays, with >65% cell death recorded in MCF-7 and HeLa cancer cell lines. Overall, the nanocomposites exhibited excellent physiochemical elements, high specificity towards cancerous cells and displayed pH-sensitive drug release in a simulated acidic tumour micro-environment. The encapsulation of 5-FU improved bioavailability of the drug in cancer cell lines for a prolonged duration, with the promise to enhance its therapeutic effect, biocompatibility and safety. These MNPs present as promising in vitro delivery systems that can further developed for therapeutic applications.

scholarly journals LHH1, a Novel Antimicrobial Peptide with Anti-Cancer Cell Activity Identified from Lactobacillus casei HZ1

2020 ◽  
Author(s):  
Junfang He ◽  
Duxin Jin ◽  
Xuegang Luo ◽  
Tongcun Zhang
Keyword(s):  
Staphylococcus Aureus ◽  
Cell Membrane ◽  
Cancer Cells ◽  
Cancer Cell ◽  
Lactobacillus Casei ◽  
Laser Scanning ◽  
Cell Activity ◽  
Antimicrobial Activities ◽  
Confocal Laser ◽  
Anti Cancer

Abstract Antimicrobial peptides have been attracting increasing attention for their multiple beneficial effects. In present study, a novel AMP with a molecular weight of 1875.5 Da, was identified from the genome of Lactobacillus casei HZ1. The peptide, which was named as LHH1 was comprised of 16 amino acid residues, and its α-helix content was 95.34% when dissolved in 30 mM SDS. LHH1 exhibited a broad range of antimicrobial activities against Gram-positive bacteria and fungus. It could effectively inhibit Staphylococcus aureus with a minimum inhibitory concentration of 3.5 μM and showed a low hemolytic activity. The scanning electron microscope, confocal laser scanning microscope and flow cytometry results showed that LHH1 exerted its antibacterial activity by damaging the cell membrane of Staphylococcus aureus. Meanwhile, LHH1 also exhibited anti-cancer cell activities against several cancer cells via breaking the cell membrane of MGC803, HCT116 and C666-1 cancer cells.

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