Table 1.
Marine Pharmacology in 2005–6: Marine Compounds with Anthelmintic, Antibacterial, Anticoagulant, Antifungal, Antimalarial, Antiprotozoal, Antituberculosis, and Antiviral Activities
Drug Class | Compound/Organisma | Chemistry | Pharmacologic Activity | IC50b | MMOAb | Countryc | References |
---|---|---|---|---|---|---|---|
Anthelmintic | (−)-echinobetaine A & (+)-B (1,2)/sponge | Alkaloidf | Activity against nematode Haemonchus contortus | 8.3–83 μg/mL++ | Undetermined | AUS | [27,28] |
Anthelmintic | Laurencia scoparia terpene (3)/alga | Sesquiterpenee | Activity against nematode Nippostrongylus brasiliensis | 0.11 mM | Undetermined | URY, BRA | [29] |
Antibacterial | caminosides B & D (4,5)/sponge | Polysaccharideg | Methicillin-resistant S. aureus & vancomicin- resistant Enterococcus inhibition | 3.1–6.3 μg/disk+ | E. coli Type III secretion inhibition | CAN, NLD, USA | [30] |
Antibacterial | Spongosorites sp. alkaloids (6,7)/sponge | Alkaloidf | S. aureus inhibition | 3.12–6.25 | Sortase A inhibition | S.KOR | [31] |
Antibacterial | aurelin (8)/jellyfish | Peptidef | E. Coli inhibition | 7.7 μg/mL+ | Undetermined | RUS | [32] |
Antibacterial | batzellaside A (9)/sponge | Alkaloidf | S. epidermidis inhibition | ≤ 6.3 μg/mL+ | Undetermined | USA | [33] |
Antibacterial | dendridine A (10)/sponge | Alkaloidf | B. subtilis & M. luteus inhibition | 4.2–8.3 μg/mL+ | Undetermined | AUS, JPN | [34] |
Antibacterial | 6-oxo-de-O-methyllasiodiplodi n (11)/fungus | Polyketided | B. subtilis, S. aureus & S. enteritidis inhibition | 6.25–12.5 μg/mL+ | Undetermined | CHN | [35] |
Antibacterial | grammistins (12)/fish | Peptidef | B. subtilis, S. aureus & E. coli inhibition | 3.13–12.5 μg/mL+ | Undetermined | JPN | [36] |
Antibacterial | halichonadin C (13)/sponge | Sesquiterpenee | M. luteus inhibition | 0.52 μg/mL+ | Undetermined | JPN | [37] |
Antibacterial | lajollamycin (14)/bacterium | Polyketided | S. aureus & S. pneumoniae inhibition | 1.5–4 μg/mL+ | Undetermined | USA | [38] |
Antibacterial | marinomycins A–D (15–18)/bacterium | Polyketided | S. aureus & E. faceium inhibition | 0.1–0.6 μM | Undetermined | USA | [39] |
Antibacterial | resistoflavin methyl ether(19)/bacteria | Polyketided | B. subtilis inhibition | 3.1 μg/mL+ | Undetermined | DEU | [40] |
Antibacterial | Streptomyces anthraquinones (20,21)/bacterium | Polyketided | Methicillin-resistant S. aureus inhibition | 0.15–0.36 | Undetermined | USA | [41] |
Antibacterial | Streptomycetaceae quinone (22)/bacterium | Polyketided | Methicillin-resistant S. aureus & vancomicin-resistant Enterococcus inhibition | 1.95–3.90 μg/mL+ | Undetermined | USA | [42] |
Antibacterial | xeniolide I (23)/soft coral | Terpenee | E. coli & B. subtilis inhibition | 1.2 μg/mL+ | Undetermined | ISR | [43] |
Anticoagulant | Limandra aspera protein/fish | Peptidef | Factor XIIa and platelet integrins inhibition | < 1 μM | Formation of inactive complex with XIIa | KOR | [57] |
Anticoagulant | fucoidans (24)/alga | Polysaccharideg | Thrombin and factor Xa inhibition in vitro and in vivo | ND | RUS | [58] | |
Anticoagulant | heparin (25)/clam | Polysaccharideg | Activated partial thromboplastin time & Xa inhibition in vitro | 52–97 IU/mg | Lower activity than bovine mucosal heparin | ITA | [59] |
Anticoagulant | sulfated galactans (26,27)/alga | Polysaccharideg | Thrombin and factor Xa inhibition in vitro | ND | 2,3-disulfated a- galactose units critical motif | BRA | [60] |
Anticoagulant | sulfated galactofucan (28)/alga | Polysaccharideg | Endothelial cell heparan sulfate synthesis stimulation | ND | Factor Xa inhibition in vitro | BRA | [61] |
Antifungal | capisterones A & B (29,30)/alga | Steroide | Enhancement of fluconazole activity | ND | CDR1 & MDR1 efflux pump reversal activity | USA | [62] |
Antifungal | Dysidea herbacea phenol (31)/sponge | Polyketided | C. albicans & A. niger inhibition | 1.95–7.8 μg/mL+ | Leakage of K+ from fungal cells | ISR | [63] |
Antifungal | spongistatin (32)/sponge | Polyketided | Broad panel of yeasts and filamentous fungi | 1–32 μg/mL+ | Disruption of microtubule network | USA | [64] |
Antifungal | halocidin (33)/ascidian | Peptidef | C. albicans inhibition | 1–4 μg/mL+ | Membrane pore formation | KOR | [66] |
Antifungal | hassallidin A (34)/bacterium | Lipopeptidef | C. albicans & A. fumigatus inhibition | 4.8 μM+ | Undetermined | DEU | [67] |
Antifungal | latrunculins (35–42)/sponge | Polyketided | C. albicans inhibition comparable to clotrimazole | 2.5–19 μM+ | Undetermined | EGY, USA | [49] |
Antifungal | majusculoic acid (43)/bacterium | Polyketided | C. albicans inhibition, less potent than fluconazole | 8 μM+ | Undetermined | USA | [68] |
Antimalarial | pycnidione (44)/fungus | Polyketided | P. falciparum W2 & D6 strain inhibition | 0.2–0.4 ng/mL | Undetermined | AUS, USA | [77] |
Antimalarial | plakortide Q (45)/sponge | Polyketided | P. falciparum D10 & W2 strain inhibition | 0.5–1 μM | Undetermined | ITA | [78] |
Antimalarial | Xestospongia sp. xestoquinone (46)/sponge | Polyketided | FCB1 P. falciparum inhibition | 3 μM | Pfnek-1 kinase inhibition | FRA | [79] |
Antimalarial | manzamine Y (47)/sponge | Alkaloidf | P. falciparum D6 & W2 strain inhibition | 0.4–0.85 μg/mL | Undetermined | IDN, ESP, USA | [80] |
Antimalarial | caucanolides A & D (48,49)/soft coral | Diterpenee | P. falciparum W2 inhibition | 17 μg/mL | Undetermined | COL, PAN, USA | [81] |
Antimalarial | Eunicea sp. sesquiterpenoids (50–54)/coral | Sesquiterpenee | P. falciparum W2 strain inhibition | 10–18 μg/mL | Undetermined | COL, PAN, USA | [82] |
Antimalarial | kallolide D (55)/sea whip | Diterpenee | P. falciparum inhibition | 30.6 μM | Undetermined | PAN, USA | [83] |
Antimalarial | leptolide & deoxypseudopter olide (56,57)/coral | Diterpenee | P. falciparum W2 strain inhibition | 50 & 74 μM | Undetermined | ESP, PAN | [84] |
Antimalarial | Muricea austera tyramine (58)/coral | Tyramine | P. falciparum W2 strain inhibition | 36 μM | Undetermined | ESP, PAN | [85] |
Antiprotozoal | ent-plakortide P (59)/sponge | Polyketided | Leishmania mexicana inhibition | 1 μg/mL | Undetermined | KOR | [86] |
Antiprotozoal | karatungiol A (60)/alga | Polyketided | Trichomonas foetus inhibition | 1 μg/mL+ | Undetermined | JPN | [87] |
Antiprotozoal | isoakaterpin (61)/sponge | Meroterpenoide | Leishmania spp. adenosine phosphoribosyl transferase inhibition | 1.05 μM | Undetermined | CAN, BRA | [88] |
Antituberculosi s | fistularin-3 & 11- deoxyfistularin-3 (62,63)/sponge | Tyrosine | M. tuberculosis inhibition | 7.1–7.3 μM+ | Undetermined | BRA | [89] |
Antituberculosi s | ileabethoxazole (64)/soft coral | Diterpenee | M. tuberculosis inhibition | 61 μg/mL+ | Undetermined | USA | [91] |
Antituberculosi s | manzamine alkaloid (65- 73)/sponge | Alkaloidsf | M. tuberculosis inhibition | 0.4–5.2 μg/mL+ | Undetermined | IDN, ESP, USA | [80] |
Antiviral | Callophylis variegata galactans/alga | Polysaccharideg | Herpes simplex & dengue type 2 inhibition | 0.1–2.2 μg/mL | Undetermined | ARG | [92] |
Antiviral | naviculan/diatom | Polysaccharideg | Herpes simplex 1 & 2 inhibition | 7.4–14 μM | Undetermined | JPN | [93] |
Antiviral | Schizymenia binderi sulfated galactan/alga | Polysaccharideg | Herpes simplex 1 & 2 inhibition | 0.18–0.76 μg/mL | Interference with HSV-heparan sulfate cellular residues | ARG, CHL | [94] |
Antiviral | Sargassum plastoquinones (74–76)/alga | Terpenoide | Measles & cytomegalovirus inhibition | 0.49–3.1 μM | Lipid peroxidation observed | JPN | [95] |
Antiviral | Dictyota diterpenes (77,78)/alga | Diterpenee | Inhibition of HIV-1 reverse transcriptase | 10–35 μM** | RNA-dependent DNA-polymerase activity inhibition | BRA | [96] |
Antiviral | griffithsin/alga | Proteinf | T- & M-tropic HIV-1 inhibition | 0.043–0.63 nM | Inhibition of CD4- dependent gp120 binding | USA | [97] |
Organism, Kingdom Animalia: fish and ascidian (Phylum Chordata); sea star (Phylum Echinodermata), clam (Phylum Mollusca), sponges (Phylum Porifera); corals, sea whips and jellyfish (Phylum Cnidaria); Kingdom Monera: bacteria (Phylum Cyanobacteria); Kingdom Fungi: fungus; Kingdom Plantae: diatom, alga;
IC50: concentration of a compound required for 50% inhibition in vitro,
estimated IC50,
Ki: inhibition constant for a drug,
Kd: concentration at which 50% of ligand binding sites are occupied, ND: not determined;
MIC: minimum inhibitory concentration,
LD99: dose required to kill 99% of test population;
MMOA: molecular mechanism of action
Country: ARG: Argentina; AUS: Australia; BRA: Brazil; CAN: Canada; CHN: China; CHL: Chile; COL: Colombia; DEU: Germany; EGY: Egypt; ESP: Spain; FRA: France; IDN: Indonesia; IND: India; ISR: Israel; ITA: Italy; JPN: Japan; NLD: The Netherlands; NZL: New Zealand; PAN: Panama; PRT: Portugal; RUS: Russia; SVN: Slovenia; URY: Uruguay;
Polyketide;
Terpene;
Nitrogen-containing compound;
Polysaccharide.