scholarly journals Parvaxanthines D–F and Asponguanosines C and D, Racemic Natural Hybrids from the Insect Cyclopelta parva

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3531
Author(s):  
Heng Chen ◽  
Yong-Ming Yan ◽  
Dai-Wei Wang ◽  
Yong-Xian Cheng
Keyword(s):  
Natural Product ◽  
Computational Methods ◽  
Chiral Hplc ◽  
Natural Hybrids ◽  
Anti Inflammatory ◽  
New Compounds ◽  
Adenine Derivatives

Five new compounds including three pairs of enantiomeric xanthine analogues, parvaxanthines D–F (1–3), two new guanosine derivatives, asponguanosines C and D (6 and 7), along with two known adenine derivatives were isolated from the insect Cyclopelta parva. Racemic 1–3 were further separated by chiral HPLC. Their absolute configurations were assigned by spectroscopic and computational methods. It is interesting that all of these isolates are natural product hybrids. Antiviral, immunosuppressive, antitumor and anti-inflammatory properties of all the isolates were evaluated.

scholarly journals An Anti-Inflammatory 2,4-Cyclized-3,4-Secospongian Diterpenoid and Furanoterpene-Related Metabolites of a Marine Sponge Spongia sp. from the Red Sea

Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 38
Author(s):  
Chi-Jen Tai ◽  
Chiung-Yao Huang ◽  
Atallah F. Ahmed ◽  
Raha S. Orfali ◽  
Walied M. Alarif ◽  
...  
Keyword(s):  
Red Sea ◽  
Superoxide Anion ◽  
Dermal Fibroblast ◽  
Fibroblast Cell ◽  
Inhibitory Effect ◽  
Human Dermal Fibroblast ◽  
Superoxide Anion Generation ◽  
Potent Inhibitory Effect ◽  
Anti Inflammatory ◽  
New Compounds

Chemical investigation of a Red Sea Spongia sp. led to the isolation of four new compounds, i.e., 17-dehydroxysponalactone (1), a carboxylic acid, spongiafuranic acid A (2), one hydroxamic acid, spongiafuranohydroxamic acid A (3), and a furanyl trinorsesterpenoid 16-epi-irciformonin G (4), along with three known metabolites (−)-sponalisolide B (5), 18-nor- 3,17-dihydroxy-spongia-3,13(16),14-trien-2-one (6), and cholesta-7-ene-3β,5α-diol-6-one (7). The biosynthetic pathway for the molecular skeleton of 1 and related compounds was postulated for the first time. Anti-inflammatory activity of these metabolites to inhibit superoxide anion generation and elastase release in N-formyl-methionyl-leucyl phenylalanine/cytochalasin B (fMLF/CB)-induced human neutrophil cells and cytotoxicity of these compounds toward three cancer cell lines and one human dermal fibroblast cell line were assayed. Compound 1 was found to significantly reduce the superoxide anion generation and elastase release at a concentration of 10 μM, and compound 5 was also found to display strong inhibitory activity against superoxide anion generation at the same concentration. Due to the noncytotoxic activity and the potent inhibitory effect toward the superoxide anion generation and elastase release, 1 and 5 can be considered to be promising anti-inflammatory agents.

In cell scalaradial interactome profiling using a bio-orthogonal clickable probe

2014 ◽  
Vol 50 (45) ◽  
pp. 6043-6045 ◽  
Author(s):  
C. Cassiano ◽  
L. Margarucci ◽  
R. Esposito ◽  
R. Riccio ◽  
A. Tosco ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Natural Product ◽  
Marine Natural Product ◽  
Anti Inflammatory

A bio-orthogonal click-chemistry procedure was developed to allow thein cellinteractome profiling of scalaradial, an anti-inflammatory marine natural product.

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.

Retracted Article: A self-assembled supramolecular natural product gel from liquidambaric acid in traditional Chinese medicine with inherent anti-inflammatory activity for drug delivery

2020 ◽  
Vol 8 (4) ◽  
pp. 715-726 ◽  
Author(s):  
Kangkang Zhi ◽  
Jiacheng Wang
Keyword(s):  
Drug Delivery ◽  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Natural Product ◽  
Inflammatory Activity ◽  
Retracted Article ◽  
Anti Inflammatory ◽  
Self Assembled

A supramolecular self-assembled natural product gel from liquidambaric acid in traditional Chinese medicine with inherent anti-inflammatory activity for drug delivery was constructed.

scholarly journals A Systematic Review of Recently Reported Marine Derived Natural Product Kinase Inhibitors

Marine Drugs ◽  
2019 ◽  
Vol 17 (9) ◽  
pp. 493 ◽  
Author(s):  
Li ◽  
Wang ◽  
Zhang ◽  
Zhang ◽  
Sajeevan ◽  
...  
Keyword(s):  
Small Molecules ◽  
Natural Product ◽  
Drug Targets ◽  
Kinase Inhibitors ◽  
Protein Kinase Inhibitors ◽  
Disease States ◽  
Clinical Drugs ◽  
Kinase Inhibitory Activity ◽  
New Compounds ◽  
Further Development

Protein kinases are validated drug targets for a number of therapeutic areas, as kinase deregulation is known to play an essential role in many disease states. Many investigated protein kinase inhibitors are natural product small molecules or their derivatives. Many marine-derived natural products from various marine sources, such as bacteria and cyanobacteria, fungi, animals, algae, soft corals, sponges, etc. have been found to have potent kinase inhibitory activity, or desirable pharmacophores for further development. This review covers the new compounds reported from the beginning of 2014 through the middle of 2019 as having been isolated from marine organisms and having potential therapeutic applications due to kinase inhibitory and associated bioactivities. Moreover, some existing clinical drugs based on marine-derived natural product scaffolds are also discussed.

scholarly journals Pyrrolizine-5-carboxamides: Exploring the impact of various substituents on anti-inflammatory and anticancer activities

2018 ◽  
Vol 68 (3) ◽  
pp. 251-273 ◽  
Author(s):  
Ahmed M. Gouda ◽  
Ahmed H. Abdelazeem ◽  
Ashraf N. Abdalla ◽  
Muhammad Ahmed
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Inflammatory Activity ◽  
Electronic Effects ◽  
Anticancer Activities ◽  
Phenyl Rings ◽  
Anti Inflammatory ◽  
New Compounds ◽  
The Impact ◽  
Mcf 7

Abstract Towards optimization of the pyrrolizine-5-carboxamide scaffold, a novel series of six derivatives (4a-c and 5a-c) was prepared and evaluated for their anti-inflammatory, analgesic and anticancer activities. The (EZ)-7-cyano-6-((4-hydroxybenzylidene)amino)-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine-5-carboxamide (4b) and (EZ)-6-((4-chlorobenzylidene)-amino)-7-cyano-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine-5-carboxamide (5b) bearing the electron donating methyl group showed the highest anti-inflammatory activity while (EZ)-6-((4-chlorobenzylidene)amino)-7-cyano-N-phenyl-2,3-dihydro-1H-pyrrolizine-5-carboxamide (5a) was the most active analgesic agent. Cytotoxicity of the new compounds was evaluated against the MCF-7, A2780 and HT29 cancer cell lines using the MTT assay. Compounds 4b and 5b displayed high anticancer activity with IC50 in the range of 0.30–0.92 μmol L−1 against the three cell lines, while compound (EZ)-N-(4-chlorophenyl)-7-cyano-6-((4-hydroxybenzylidene)-amino)-2,3-dihydro-1H-pyrrolizine-5-carboxamide (4c) was the most active against MCF-7 cells (IC50 = 0.08 μmol L−1). Both the anti-inflammatory and anticancer activities of the new compounds were dependent on the type of substituent on the phenyl rings. Substituents with opposite electronic effects on the two phenyl rings are preferable for high cytotoxicity against the MCF-7 and A2780 cells. COX inhibition was suggested as the molecular mechanism of the anti-inflammatory activity of the new compounds while no clear relationship could be observed between COX inhibition and anticancer activity. Compound 5b, the most active against the three cell lines, induced dose-dependent early apoptosis with 0.1–0.2 % necrosis in MCF-7 cells. New compounds showed promising drug-likeness scores while the docking study revealed high binding affinity to COX-2. Taken together, this study highlighted the significant impact of the substituents on the anti-inflammatory and anticancer activity of pyrrolizine-5-carboxamides, which could help in further optimization to discover good leads for the treatment of cancer and inflammation.

scholarly journals Antitussive and Anti-inflammatory Dual-active Agents Developed from Natural Product Lead Compound 1-Methylhydantoin

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2355 ◽  
Author(s):  
Yang Xu ◽  
Fang Wang ◽  
Hongye Guo ◽  
Shihan Wang ◽  
Shuling Ni ◽  
...  
Keyword(s):  
Natural Product ◽  
Binding Pocket ◽  
In Vivo Model ◽  
Lead Compound ◽  
Pm 2.5 ◽  
In Silico Study ◽  
Acute Pneumonia ◽  
Long Time ◽  
Anti Inflammatory

Natural products play an important role in drug discovery. This work employed a natural product 1-methylhydantoin as the lead compound to develop novel dual-active drugs. 1-Methylhydantoin was isolated from Oviductus Ranae, which is a traditional Chinese medicine that has been used for tussive and inflammation treatment for a long time. An in silico study screened the more active 1-methylhydantoin derivatives. Antitussive assessment indicated that the newly synthesized agent had similar bioactivity with the natural product. An anti-inflammatory model used xylene induced ear edema model. At the same dosage (100 mg/Kg), the newly prepared agent had an inhibition rate 53.18% which was much higher than that of the lead compound (22.69%). The results might be ascribed to the cyclooxygenases-1 (COX-1) and cyclooxygenases-2 (COX-2) selectivity, and the fitness of the compound, and the binding pocket. The anti-particulate matter (PM 2.5) acute pneumonia was evaluated through an in vivo model constructed by nasal instillation with PM 2.5 suspension. The results of the above models suggested that this novel agent had remarkable antitussive, anti-inflammatory, and anti-PM 2.5 acute pneumonia activities.

scholarly journals Synthesis of 1-(4-phenoxyphenyl)-3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]propan-1-ones as safer anti-inflammatory and analgesic agents

2008 ◽  
Vol 73 (8-9) ◽  
pp. 781-791 ◽  
Author(s):  
Asif Husain ◽  
F.J. Ahmad ◽  
Mohd Ajmal ◽  
Priyanka Ahuja
Keyword(s):  
Lipid Peroxidation ◽  
Phosphorus Oxychloride ◽  
1H And 13C Nmr ◽  
Writhing Test ◽  
Rat Paw Edema ◽  
Malondialdehyde Content ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
New Compounds

A novel series of 1-(4-phenoxyphenyl)-3-[5-(substituted aryl)-1,3,4-oxa- diazol-2-yl]propan-1-one was synthesized by reaction of 3-(4-phenoxybenzoyl)propionic acid with several aryl acid hydrazides in phosphorus oxychloride. The structures of the compounds were supported by IR, 1H- and 13C-NMR, MS data and elemental analysis results. These compounds were tested for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation actions. A few compounds were found to have very good anti-inflammatory activity in the carrageenan-induced rat paw edema test, while a fair number of the compounds showed significant analgesic activity in the acetic acid-induced writhing test. These new compounds showed very low ulcerogenic action with reduced malondialdehyde content (MDA), which is one of the by-products of lipid peroxidation.

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