Marine natural products

Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC₅₀s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine also inhibits TAOK2 with an IC₅₀ of 3 μM. Staurosporine is an apoptosis inducer.

Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC₅₀ of 16 nM. Cytarabine has antiviral effects against HSV. Cytarabine shows anti-orthopoxvirus activity.

Adenosine (Adenine riboside), a ubiquitous and BBB-permeable endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.

Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation.

Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP). Okadaic acid has a significantly higher affinity for PP2A (IC₅₀=0.1-0.3 nM), and inhibits PP1 (IC₅₀=15-50 nM), PP3 (IC₅₀=3.7-4 nM), PP4 (IC₅₀=0.1 nM), PP5 (IC₅₀=3.5 nM), but does not inhibit PP2C. Okadaic acid increases of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter. Okadaic acid induces tau phosphorylation.

Cristatumin E (Eurocristatine) is a natural alkaloid.

Alginate oligosaccharides (AOS) are orally effective linear oligosaccharides with anti-inflammatory, antioxidant and antimicrobial activities. Alginate oligosaccharides inhibit the activation of NLRP3 inflammasome and NF-κB, promote nuclear translocation of Nrf2 and phosphorylation of AMPK, and reduce the enhanced functional level of TRPV1. Alginate oligosaccharides improve oxidative stress, ROS production, mitochondrial bioenergetic dysfunction and gait impairment. Alginate oligosaccharides inhibit the release of neuropeptides; alter the structure and viscoelasticity of mucin matrix; disrupt bacterial and fungal biofilms; regulate gut microbiota; and exert anti-apoptotic effects.

(+)-Aureol is a tetracyclic benzopyran-fused decalin-type 9-norspongiane heteroterpenoid. (+)-Aureol exhibits antifungal activity, with an EC₅₀ value of 6.9 μM against Rhizoctonia solani and an EC₅₀ value of 19 μM against Sclerotinia sclerotiorum. (+)-Aureol shows selective inhibitory activity against human tumor cells. (+)-Aureol acts as an anti-influenza agent with activity against influenza A virus. (+)-Aureol can be used in research related to fungal infections, non-small cell lung cancer, colon adenocarcinoma and influenza A virus infections.

Pristane (Norphytane) is a naturally occurring hydrocarbon oil found in small quantities in many plants, in various marine organisms, and as the most active component of mineral oil. Pristane is a non-antigenic adjuvant, and induces MHC class II-restricted, arthritogenic T cells in the rat.

Fucoidan, a biologically active polysaccharide, is an efficient inhibitor of α-amylase and α-glucosidase. Anticoagulant, antitumor, antioxidant and antisteatotic activities.

Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with K_ds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research. Latrunculin A blocks cell migration.

Jasplakinolide is a potent actin polymerization inducer and stabilizes pre-existing actin filaments. Jasplakinolide binds to F-actin competitively with phalloidin with a K_d of 15 nM. Jasplakinolide, a naturally occurring cyclic peptide from the marine sponge, has both fungicidal and anti-cancer activity.

Fucoxanthin (all-trans-Fucoxanthin) is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.

Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively).

Latrunculin B, an antimicrobial marine alkaloid, is an actin polymerization inhibitor. Latrunculin B regulates pulmonary vein electrophysiological characteristics and attenuates stretch-induced arrhythmogenesis. Antifungal and antiprotozoal activity.

Phenazine-1-carboxylic acid is an antifungal agent. Additionally, Phenazine-1-carboxylic acid exhibits anticancer activity by inducing apoptosis in cancer cells through the regulation of ROS generation. Phenazine-1-carboxylic acid can upregulate the expression of IL-8 and ICAM-1 while inhibiting the release of RANTES and MCP-1, demonstrating its potential immunomodulatory effects. Phenazine-1-carboxylic acid holds significant research value in the areas of anti-infection, anticancer, and immune response modulation.

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a K_i of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with K_i values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.

Plitidepsin (Aplidine) is a potent anti-cancer agent by targeting eEF1A2 ( K_D=80 nM). Plitidepsin possesses antiviral activity and is against SARS-CoV-2 with an IC₉₀ of 0.88 nM. Plitidepsin is usually used for multiple myeloma and advanced cancer research, and has the potential for COVID-19 research.

Xanthosine is a nucleoside derived from xanthine and ribose. Xanthosine activates the AMPK/FoxO1/AKT/GSK3β signaling cascade. Xanthosine promotes cell proliferation and regulates blood glucose metabolism. Xanthosine increases milk production in cows and goats. Xanthosine is used in mammary stem cell and type 2 diabetes research.

Sodium alginate is the sodium salt of alginic acid. Sodium alginate can be extracted and purified from brown seaweed Laminaria japonica. Sodium alginate can be used in food additives and pharmaceuticals, adsorb heavy metal ions, and has mucosal-protective and hemostatic effects.