Crotonkinins A and B and Related Diterpenoids fromCroton tonkinensisas Anti-inflammatory and Antitumor Agents

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.

Download Full-text

Antitumor agents. 271: Total synthesis and evaluation of brazilein and analogs as anti-inflammatory and cytotoxic agents

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2009.12.041 ◽

2010 ◽

Vol 20 (3) ◽

pp. 1037-1039 ◽

Cited By ~ 39

Author(s):

Chiao-Ting Yen ◽

Kyoko Nakagawa-Goto ◽

Tsong-Long Hwang ◽

Pei-Chi Wu ◽

Susan L. Morris-Natschke ◽

...

Keyword(s):

Total Synthesis ◽

Antitumor Agents ◽

Cytotoxic Agents ◽

Anti Inflammatory

Download Full-text

Design, Synthesis and Evaluation of some Novel Pyrazoline Derivatives as Potential Anti-inflammatory and Antitumor Agents

Drug Research ◽

10.1055/s-0032-1333293 ◽

2013 ◽

Vol 63 (06) ◽

pp. 271-281

Author(s):

R. Elbayaa ◽

M. Badr ◽

A. Khalil ◽

M. Abdelhadi

Keyword(s):

Antitumor Agents ◽

Design Synthesis ◽

Anti Inflammatory

Download Full-text

Schiff Bases: Interesting Scaffolds with Promising Antitumoral Properties

Applied Sciences ◽

10.3390/app11041877 ◽

2021 ◽

Vol 11 (4) ◽

pp. 1877

Author(s):

Domenico Iacopetta ◽

Jessica Ceramella ◽

Alessia Catalano ◽

Carmela Saturnino ◽

Maria Grazia Bonomo ◽

...

Keyword(s):

Antitumor Activity ◽

Organic Compounds ◽

Organic Synthesis ◽

Schiff Bases ◽

Antitumor Agents ◽

Biological Activities ◽

Anti Inflammatory ◽

Polymer Stabilizers

Schiff bases, named after Hugo Schiff, are highly reactive organic compounds broadly used as pigments and dyes, catalysts, intermediates in organic synthesis, and polymer stabilizers. Lots of Schiff bases are described in the literature for various biological activities, including antimalarial, antibacterial, antifungal, anti-inflammatory, and antiviral. Schiff bases are also known for their ability to form complexes with several metals. Very often, complexes of Schiff bases with metals and Schiff bases alone have demonstrated interesting antitumor activity. Given the innumerable vastness of data regarding antitumor activity of all these compounds, we focused our attention on mono- and bis-Schiff bases alone as antitumor agents. We will highlight the most significant examples of compounds belonging to this class reported in the literature.

Download Full-text

Gloeothece sp.—Exploiting a New Source of Antioxidant, Anti-Inflammatory, and Antitumor Agents

Marine Drugs ◽

10.3390/md19110623 ◽

2021 ◽

Vol 19 (11) ◽

pp. 623

Author(s):

Helena M. Amaro ◽

Rita Barros ◽

Tânia Tavares ◽

Raquel Almeida ◽

Isabel Sousa Pinto ◽

...

Keyword(s):

Fatty Acids ◽

Antitumor Agents ◽

Brdu Incorporation ◽

Membrane Stabilization ◽

Screening Assay ◽

Associated Conditions ◽

Cox 2 ◽

Anti Inflammatory ◽

Incorporation Assay ◽

Bioactive Potential

Bioactive lipidic compounds of microalgae, such as polyunsaturated fatty acids (PUFA) and carotenoids, can avoid or treat oxidation-associated conditions and diseases like inflammation or cancer. This study aimed to assess the bioactive potential of lipidic extracts obtained from Gloeothece sp.–using Generally Recognized as Safe (GRAS) solvents like ethanol, acetone, hexane:isopropanol (3:2) (HI) and ethyl lactate. The bioactive potential of extracts was assessed in terms of antioxidant (ABTS•+, DPPH•, •NO and O2•assays), anti-inflammatory (HRBC membrane stabilization and Cox-2 screening assay), and antitumor capacity (death by TUNEL, and anti-proliferative by BrdU incorporation assay in AGS cancer cells); while its composition was characterized in terms of carotenoids and fatty acids, by HPLC-DAD and GC-FID methods, respectively. Results revealed a chemopreventive potential of the HI extract owing to its ability to: (I) scavenge -NO• radical (IC50, 1258 ± 0.353 µg·mL−1); (II) inhibit 50% of COX-2 expression at 130.2 ± 7.4 µg·mL−1; (III) protect 61.6 ± 9.2% of lysosomes from heat damage, and (IV) induce AGS cell death by 4.2-fold and avoid its proliferation up to 40% in a concentration of 23.2 ± 1.9 µg·mL−1. Hence, Gloeothece sp. extracts, namely HI, were revealed to have the potential to be used for nutraceutical purposes.

Download Full-text

Medicinal Plants from Brazilian Cerrado Biome: Potential sources of new anti-inflammatory compounds and antitumor agents on Ehrlich carcinoma

Anais da Academia Brasileira de Ciências ◽

10.1590/0001-3765202120191101 ◽

2021 ◽

Vol 93 (suppl 3) ◽

Author(s):

FÁBIO A. MALARA ◽

DJAMILE C. MATOS ◽

LÍVIA C.A. RIBEIRO ◽

THAIS O.R. FALCOSKI ◽

TERESINHA J.A.S. ANDRADE ◽

...

Keyword(s):

Medicinal Plants ◽

Antitumor Agents ◽

Ehrlich Carcinoma ◽

Brazilian Cerrado ◽

Cerrado Biome ◽

Potential Sources ◽

Anti Inflammatory

Download Full-text

Exploring the Pivotal Immunomodulatory and Anti-Inflammatory Potentials of Glycyrrhizic and Glycyrrhetinic Acids

Mediators of Inflammation ◽

10.1155/2021/6699560 ◽

2021 ◽

Vol 2021 ◽

pp. 1-15

Author(s):

Seidu A. Richard

Keyword(s):

Nitric Oxide ◽

Influenza A ◽

Antitumor Agents ◽

Enterovirus 71 ◽

High Mobility ◽

Interferon Γ ◽

Human Enterovirus ◽

Human Enterovirus 71 ◽

Anti Inflammatory ◽

Syncytial Virus

Licorice extract is a Chinese herbal medication most often used as a demulcent or elixir. The extract usually consists of many components but the key ingredients are glycyrrhizic (GL) and glycyrrhetinic acid (GA). GL and GA function as potent antioxidants, anti-inflammatory, antiviral, antitumor agents, and immuneregulators. GL and GA have potent activities against hepatitis A, B, and C viruses, human immunodeficiency virus type 1, vesicular stomatitis virus, herpes simplex virus, influenza A, severe acute respiratory syndrome-related coronavirus, respiratory syncytial virus, vaccinia virus, and arboviruses. Also, GA was observed to be of therapeutic valve in human enterovirus 71, which was recognized as the utmost regular virus responsible for hand, foot, and mouth disease. The anti-inflammatory mechanism of GL and GA is realized via cytokines like interferon-γ, tumor necrotizing factor-α, interleukin- (IL-) 1β, IL-4, IL-5, IL-6, IL-8, IL-10, IL-12, and IL-17. They also modulate anti-inflammatory mechanisms like intercellular cell adhesion molecule 1 and P-selectin, enzymes like inducible nitric oxide synthase (iNOS), and transcription factors such as nuclear factor-kappa B, signal transducer and activator of transcription- (STAT-) 3, and STAT-6. Furthermore, DCs treated with GL were capable of influencing T-cell differentiation toward Th1 subset. Moreover, GA is capable of blocking prostaglandin-E2 synthesis via blockade of cyclooxygenase- (COX-) 2 resulting in concurrent augmentation nitric oxide production through the enhancement of iNOS2 mRNA secretion in Leishmania-infected macrophages. GA is capable of inhibiting toll-like receptors as well as high-mobility group box 1.

Download Full-text