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. 2019 Dec 19;18(1):5. doi: 10.3390/md18010005

Table 2.

Marine pharmacology in 2014–2015: marine compounds with antidiabetic and anti-inflammatory activity, and affecting the immune and nervous system.

Drug Class Compound/Organism a+ Chemistry Pharmacological Activity IC50 b MMOA c Country d References
Antidiabetic fucoxanthin and fucoxanthinol (134, 135)/alga Terpenoid f Improved glucose tolerance in vitro and in vivo 50 µM * Cytokine inhibition JPN, S. KOR [154,155]
Antidiabetic octaphlorethol A (136)/alga Shikimate h α-glucosidase inhibition 110 µM Molecular docking on active site CAN, S. KOR [156]
Antidiabetic phlorofucofuroeckol-A (10)/alga Polyketide d Decreased glucose levels in vivo 10 mg/kg ** α-glucosidase inhibition S. KOR [157]
Antidiabetic Con-Ins G1 (137)/cone snail Peptide g Hypoglycemia induction 65 ng/g * Undetermined AUS, DNK, USA [158]
Antidiabetic dehydroeuryspongin A (138)/sponge Terpenoid f PTP1B inhibition 3.58 μM Undetermined IDN, JPN [159]
Antidiabetic Epicoccum sp. diterpene (139)/fungus Terpenoid f α-glucosidase inhibition 4.6 μM Undetermined CHN [160]
Antidiabetic suncheonoside A (140)/bacterium Terpenoid f Adiponectin production 10 μM * Undetermined S. KOR [161]
Antidiabetic terrelumamide A (141)/fungus Peptide g Adiponectin production 37 μM * Undetermined S. KOR [162]
Antidiabetic X. testudinaria lipid (142)/sponge Polyketide d PTP1B inhibition 5.3 μM Undetermined CHN [163]
Anti-inflammatory alcyonolide congeners (143, 144)/soft coral Terpenoid f Macrophage NO inhibition 2 μM * iNOS expression inhibition JPN [164]
Anti-inflammatory astaxanthin (145)/alga Terpenoid f Oxidative stress inhibition in vivo 10 mg/kg ** CAT and SOD enhancement CHN [165]
Anti-inflammatory 8,8′-bieckol (146)/alga Polyketide e Macrophage NO and PGE2 release inhibition 50 μM * Inhibition of NFκB S. KOR [166]
Anti-inflammatory convolutamydine A (147)/ bryozoa Alkaloid g Formalin-induced licking behavior inhibition 0.01 mg/kg * TNF-α, IL-6 release inhibition BRA [167]
Anti-inflammatory capgermacrene A (148)/ soft coral Terpenoid f Macrophage NO and IL-1β inhibition <10 μg/mL * iNOS expression inhibition MYS, S. KOR [168]
Anti-inflammatory cathelicidin (4)/sea snake Peptide g Binding of LPS to TLR4 inhibition 4 μg/mL * Inflammatory cytokine inhibition CHN [26]
Anti-inflammatory dactyloditerpenol acetate (149)/ sea hare Terpenoid f LPS- activated microglia in vitro inhibition 0.4–1 μM O2- and TXB2 inhibition USA [169]
Anti-inflammatory dieckol (150)/alga Shikimate h Macrophage iNOS transcription inhibition 30 μM * Inhibition of NFκB and p38MAPK S. KOR [170]
Anti-inflammatory dieckol (150)/alga Shikimate h Human keratinocyte MDC/CCL22 inhibition 12.5 μM * STAT1 phosphorylation inhibition S. KOR [171]
Anti-inflammatory excavatolide B (151)/gorgonian Terpenoid f Macrophage iNOS and COX-2 transcription inhibition 25 μM * In vivo iNOS protein expression reduction TWN [172]
Anti-inflammatory flexibilide (152)/soft coral Terpenoid f Neuropathic pain inhibition 10 µg * Upregulation of TGF-β1 TWN [173]
Anti-inflammatory fucoxanthinol (135)/alga Terpenoid f Macrophage TNF-α and MCP-1 release inhibition 10 μM COX-2 expression inhibition JPN [155]
Anti-inflammatory H. fusiforme flavone (153)/ alga Shikimate h/Polyketide d Macrophage NO and PGE2 release inhibition 10 μg/mL * iNOS, COX-2 expression inhibition S. KOR [174]
Anti-inflammatory 5β-hydroxypalisadin B (154)/alga Terpenoid f Macrophage NO release inhibition 17 μM Partial iNOS expression inhibition LKA, MYS, S. KOR [175]
Anti-inflammatory glaucumolides A and B (155, 156)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition 2.8–4 µM * iNOS, COX-2 inhibition TWN [176]
Anti-inflammatory phlorofucofuroeckol-B (157)/alga Polyketide d Microglia activation inhibition 0.1 μg/mL * iNOS, COX-2 inhibition S. KOR [177]
Anti-inflammatory P. palmata lipid (158)/alga Polyketide d Macrophage NO release inhibition 16.7 μM iNOS expression inhibition CAN [178]
Anti-inflammatory reduced scytonemin (159)/alga Alkaloid g Macrophage NO release inhibition 1 µM * HO-1 expression induction JPN [179]
Anti-inflammatory sinuleptolide (160)/soft coral Terpenoid f LPS-activated rat microglia in vitro inhibition 0.5–2.9 μM Cytokine release inhibition ESP, FIN, IND, ITA, [180]
Anti-inflammatory sarcopanol A (161)/soft coral Terpenoid f iNOS, COX-2, and ICAM-1 transcription inhibition 8.3 µM NFκB inhibition S. KOR, VNM [181]
Anti-inflammatory sinumaximol H (162)/sponge Terpenoid f iNOS and ICAM-1 transcription inhibition 1 µM * NFκB inhibition S. KOR, VNM [182]
Anti-inflammatory tanzawaic acid A (163)/fungus Polyketide d NO inhibition 7.1 µM iNOS and PTP1B inhibition VNM, S. KOR [183]
Anti-inflammatory aspertetranone D (164)/fungus Terpenoid f IL-6 inhibition 40 µM * Undetermined CHN, USA [184]
Anti-inflammatory briarenolide J (165)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition 10–15 µM Undetermined TWN [185]
Anti-inflammatory briarenolides K and L (166, 167)/soft coral Terpenoid f Macrophage iNOS inhibition >10 μg/mL * Undetermined TWN [186]
Anti-inflammatory briarenolides U, V, W (168, 169)/soft coral Terpenoid f Macrophage COX-2 and iNOS expression inhibition >10 μg/mL * Undetermined TWN [187]
Anti-inflammatory briaviolides E and I (170, 171)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition >10 μg/mL * Undetermined TWN [188]
Anti-inflammatory dermacozine H (172)/bacterium Alkaloid g Radical scavenging activity 18.8 µM Undetermined DEU, EGY, UK [189]
Anti-inflammatory dysifragilone A (173)/sponge Terpenoid f Macrophage NO release inhibition 6.6 µM Undetermined CHN [190]
Anti-inflammatory D. plectens xenicane (174)/alga Terpenoid f Macrophage NO release inhibition 10 µM Undetermined CHN [191]
Anti-inflammatory comaparvin (175)/crinoid Polyketide d Carrageenan-induced hyperalgesia inhibition 30 mg/kg * iNOS expression inhibition TWN [192]
Anti-inflammatory hirsutalins N and S (176, 177)/ soft coral Terpenoid f Neutrophil elastase inhibition 10 μM * Undetermined TWN [193,194]
Anti-inflammatory hirsutocospiro A (178)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition 3.7–4.1 μM Undetermined TWN [195]
Anti-inflammatory isosinulaflexiolide K (179)/soft coral Terpenoid f Macrophage COX-2 and iNOS expression inhibition >10 μM * Undetermined TWN [196]
Anti-inflammatory klyflaccisteroid F (180)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition 0.34 μM Undetermined TWN [197]
Anti-inflammatory krempfielin N (181)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition >10 μM * Undetermined TWN [198]
Anti-inflammatory krempfielins Q and R (182, 183)/soft coral Terpenoid f Neutrophil SOX and elastase inhibition >10 μM * Undetermined TWN [199]
Anti-inflammatory methylfarnesylquinone (184)/alga Shikimate h/Terpenoid f Neutrophil SOX and elastase inhibition 0.2–0.48 µg/mL Undetermined TWN [200]
Anti-inflammatory monanchosterol B (185)/sponge Terpenoid f Macrophage IL-6 expression inhibition 5 µM Undetermined S. KOR [201]
Anti-inflammatory P. nodosus sterol (186)/starfish Terpenoid f IL-12 and IL-6 inhibition 1.3–3.1 µM Undetermined VNM, S. KOR [202]
Anti-inflammatory rhytidenone C (187)/fungus Polyketide d Macrophage NO inhibition 0.31 µM Undetermined THA [203]
Anti-inflammatory sarcocrassocolide E (188)/soft coral Terpenoid f Macrophage COX-2 and iNOS expression inhibition <10 μM * Undetermined TWN [204]
Anti-inflammatory sinulacembranolide A (189)/octocoral Terpenoid f Macrophage iNOS expression inhibition <10 μM Undetermined TWN [205]
Anti-inflammatory thomimarine B (190)/fungus Terpenoid f Macrophage NO inhibition >10 μM Undetermined RUS, VNM [206]
Anti-inflammatory tortuosene A (191)/soft coral Terpenoid f Neutrophil SOX inhibition 7.3 μM Undetermined TWN [207]
Immune system grassypeptolide A (192)/cyanobacterium Peptide g IL-2 and T-cell proliferation inhibition 1 μM * Dipeptidyl peptidase 8 inhibition CHN, JPN, USA [208]
Immune system F. reticulata alkaloids (193)/sponge Alkaloid g IL-2 inhibition 5–50 µM * Undetermined CHN, NLD [209]
Immune system luzonicoside A (194)/starfish Terpenoid f Macrophage NO and ROS stimulation 0.01–0.1 µM * Undetermined RUS, VNM [210]
Immune system typicoside C1(195)/sea cucumber Terpenoid f Macrophage ROS stimulation <1 ng/mL * Undetermined IND, RUS [211]
Nervous system aurone glycoside (196)/fungus Shikimate h/Polyketide d Oxidative stress neuroprotection 1 µM * Apoptosis inhibition CHN [212]
Nervous system azaspiracid-1 (197)/alga Polyketide d/
Alkaloid g 		Peripherin-labelled neurite process 15 nM * Peripherin isoform downregulation NOR [213]
Nervous system caulerpine (198)/alga Alkaloid g Antinociceptive activity 40 mg/kg * Involves α2 and 5-HT3 receptors BRA [214]
Nervous systema 6-bromohypaphorine (199)/sea slug Alkaloid g Human α7 nAChR agonist 23 µM Rise [Ca2+ ]i RUS [215]
Nervous system piscidin (200)/fish Peptide g Antinociceptive activity 20 µg/rat * Phosphor-mTOR inhibition TWN [216]
Nervous system C. marmoreus conotoxin Mr1.7 (201)/cone snail Peptide g Ach-evoked membrane current inhibition 53.1 nM A3β2 nAChR inhibition CHN [217]
Nervous system C. litteratus conotoxin lt16a (202)/cone snail Peptide g Neuronal Na+ current inhibition 1 µM * Undetermined CHN [218]
Nervous system C. vitulinus peptide (203)/ cone snail Peptide g Neuronal BK channel inhibition 8.5 µM Electrostatic interaction with β4 subunits CHN, USA [219]
Nervous system echinochrome A (204)/sea urchin Polyketide d Acetylcholinesterase inhibition and NO scavenging 16.4 µM Irreversible and uncompetitive inhibition S. KOR, RUS [220]
Nervous system ganglioside LLG-3 (205)/starfish Glycolipid Neuritogenesis stimulation in vitro 1 nM * MAPK signaling stimulation JPN [221]
Nervous system heteronemin (206)/sponge Terpenoid f TDP-43 binding to DNA inhibition 10.1 nM Promoted aggregation of insoluble TDP-43 ITA [222]
Nervous system pinnatoxin A (207)/mollusc Polyketide d/
Alkaloid g 		Muscle and neuronal nAChRs receptor inhibition 0.086–47.5 nM EF-ketal ring confers nAChR subtype specificity FRA, USA [223]
Nervous tissue PhcrTx1 (208)/sea anemone Peptide g ASIC inhibition 100 nM Lower potency on Kv channels BEL, BRA, CUB, DEU, ESP, MEX [224]
Nervous tissue phlorofucofuroeckol-A (10)/alga Polyketide d Butyrylcholinesterase inhibition 0.95 µM β-secretase inhibition S. KOR [225]
Nervous tissue S. auritum ceramide (209)/soft coral Polyketide d Anxiolytic and CNS depressing activity in vivo 1 mg/kg ** GABA(A) receptor modulation EGY, USA [226]
Nervous system spirolide C (210)/dinoflagellate Polyketide d/
Alkaloid g 		nAChR inhibition 1.5–3 nM * Muscle and neuronal -type nAChR inhibition FRA [227]
Nervous system zonarol (211)/alga Meroterpenoid f Glutamate toxicity inhibition in vitro 0.22 µM Nrf2/ARE pathway activation JPN, USA [228]
Nervous system aplysinellamide-1 (212)/sponge Alkaloid g ApoE secretion modulation 30 µM * Undetermined AUS, CAN [229]
Nervous system A. terreus lactones (120, 121)/fungus Polyketide d acetylcholinesterase inhibition 4.2 µM Undetermined CHN [115]
Nervous system C. araneosus ar3j conotoxin (213)/cone snail Peptide g Sleep induction 2 nM * Undetermined IND [230]
Nervous system D. cejpii steroid (214)/fungus Terpenoid f Amyloid β-42 production inhibition 10 µM * Undetermined DEU, FRA [231]
Nervous system genuanine (215)/cone snail Alkaloid g Paralysis in vivo 40 nM * Undetermined PRT, USA [232]
Nervous system homoaerothionin (216)/sponge Alkaloid g acetylcholinesterase inhibition 2.9–6.2 µM Undetermined THA [233]
Nervous system mooreamide A (217)/bacterium Polyketide d CB1 binding 0.47 µM ** Undetermined ITA, PNG, USA [234]
Nervous system S. spinosulus hydroquinone (218)/sponge Shikimate h/Polyketide d Enhance glutamate and ACh release 10 µM * Undetermined ITA [235]

aOrganism:Kingdom Animalia: fish (Phylum Chordata); bryozoan; coral and sea anemone (Phylum Cnidaria); crinoid, sea urchin, starfish (Phylum Echinodermata); cone snail, sea slug (Phylum Mollusca); sponge (Phylum Porifera); Kingdom Fungi: fungus; Kingdom Plantae: alga; Kingdom Monera: bacterium; Kingdom Protozoa: dinoflagellates; b IC50: concentration of a compound required for 50% inhibition, *: apparent IC50, **: in vivo study; **: Ki: concentration needed to reduce the activity of an enzyme by half; c MMOA: molecular mechanism of action; d Country: AUS: Australia; BEL: Belgium; BRA: Brazil; CAN: Canada; CHN: China; CUB: Cuba; DEU: Germany; DNK: Denmark; EGY: Egypt; ESP: Spain; FIN, Finland; FRA: France; IDN: Indonesia; IND, India; ITA: Italy; JPN: Japan; LKA: Sri Lanka; MEX: Mexico; MYS: Malaysia; NLD: Netherlands; NOR: Norway; PNG: Papua New Guinea; PRT: Portugal; RUS: Russian Federation; S. KOR: South Korea; THA: Thailand; TWN: Taiwan; VNM: Vietnam; Chemistry: e Polyketide; f Terpene; g Nitrogen-containing compound; h Shikimate. Abbreviations: Ach: acetylcholine; ApoE: apolipoprotein E; ASIC: acid-sensing sodium ion channel; CAT: catalase; CB1: cannabinoid receptor 1; CNS: central nervous system; COX: cyclooxygenase; HO-1: heme oxygenase-1; ICAM: intercellular adhesion molecule-1; IL: interleukin; iNOS: inducible nitric oxide synthase; Kv current: voltage-gated K+ current; MAPK: mitogen-activated protein kinase pathway; MDC/CCL22: macrophage-derived chemokine, C–C motif chemokine 22; nAChR: nicotinic acetylcholine receptor; NA: not available; NF-κB: nuclear factor kappa-light-chain-enhancer of activated B cells; NO: nitric oxide; nAChR: nicotinic acetylcholine receptor; Nrf2-ARE: nuclear transcription factor E2-related factor antioxidant response element; PTP1B: tyrosine protein; phosphatase 1B; ROS: reactive oxygen species; SOD: superoxide dismutase; SOX: superoxide; STAT1: signal transducer and activator of transcription1; TDP-43: trans-activation response DNA-binding protein of 43 kDa.