T83899
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N-didesmethyl Loperamide是loperamide的一个活性代谢产物,属于周围μ1-阿片受体激动剂。它能抑制孤立的豚鼠肠膜丛中由电刺激引起的收缩(IC50 = 370 nM)。N-didesmethyl Loperamide还能增强对氯喹产生抗药性的P. falciparum菌株对氯喹的敏感性(EC50 = 482 nM),同时在A-10血管平滑肌细胞中未引起毒性(IC50 = >10,000 nM)。 |
T35732
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Diacetylcercosporin is a perylenequinone produced by Cercospora and Septoria that has diverse biological activities. It inhibits the growth of P. falciparum strains that are sensitive and resistant to chloroquine and L. donovani parasites (IC50 = 3.1 μM) in vitro. Diacetylcercosporin exhibits cytotoxicity against SK-MEL, KB, BT549, and SK-OV-3 human cancer cell lines (IC50s = 4.8-8.7 μM). It is also a phytotoxin that inhibits the growth of lettuce and bentgrass at a concentration of 1.62 mM |
T35483
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19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng/ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 µM, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 µM. |
TN4449
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Antifection
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Longistylin A and longistylin C show some cytotoxic effects, with IC(50) values of 0.7-14.7 microM against the range of cancer cell lines. Longistylin A and longistylin C, and betulinic acid show a moderately high in vitro activity against the chloroquine |
TN4113
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Antifection
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Garcinone E is active constituents in the anticomplement assay used. Garcinone E exhibits potent activity in vitro against Plasmodium falciparum chloroquine-resistant strain W2, with IC50 values below 3 µM. It has potent cytotoxic effect on all hepatocellular carcinomas cell lines as well as on the other gastric and lung cancer cell lines included in the screen, may be potentially useful for the treatment of certain types of cancer. |
T35909
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Penicinoline is an alkaloid that has been found in Penicillium and has antimalarial, insecticidal, and anticancer activities.1,2 It is active against chloroquine-sensitive and -resistant strains of P. falciparum (IC50 = 25 μM for both).1 Penicinoline (1,000 ppm) is also active against the aphid A. gossypii.2 It inhibits proliferation of 95-D and HepG2 cancer cells (IC50s = 0.57 and 6.5 μg/ml, respectively) but not HeLa, KB, KBv200, or Hep-2 cells (IC50s = >100 μg/ml).
|1. Naveen, B., Ommi, N.B., Mudiraj, A., et al. Total synthesis of penicinoline E, marinamide, methyl marinamide and their antimalarial activity. ChemistrySelect 2(11), 3256-3261 (2017).|2. Shao, C.-L., Wang, C.-Y., Gu, Y.-C., et al. Penicinoline, a new pyrrolyl 4-quinolinone alkaloid with an unprecedented ring system from an endophytic fungus Penicillium sp. Bioorg. Med. Chem. Lett. 20(11), 3284-3286 (2010). |
T35751
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Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1] |
T38297
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Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers.
1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980) |