cytotoxicities

Epoxomicin (BU-4061T,Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.

Shishijimicin C, a novel antitumor agent isolated from the ascidian Didemnum proliferum, exhibits highly potent cytotoxicities and anti-tumor activities. This compound also serves as a click chemistry reagent, featuring an alkyne group that can partake in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

Shishijimicin A, a novel antitumor agent isolated from the ascidian Didemnum proliferum, exhibits highly potent cytotoxicities and demonstrates considerable anti-tumor activity [1] [2]. This compound also serves as a click chemistry reagent due to its alkyne group, enabling it to partake in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules.

1-Hydroxyrutaecarpine exhibits cytotoxicities (ED50 values < 4 microg mL) against P-388 or HT-29 cell lines in vitro.

1,3-Diacetylvilasinin shows marginal cytotoxicities against certain human tumor cell lines. It also shows antifeeding activity towards insects.

1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone exhibits moderate cytotoxicity against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, but lacks antifungal activity against [Candida albicans].

1,4,5,6-Tetrahydroxy-7-prenylxanthone exhibits anti-cancer activity, demonstrating moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines, and shows moderate activity with GI50 values of 2.8 μM against the human leukaemic HL-60 cell line measured in vitro.

2,3-Dihydroamentoflavone 7,4'-dimethyl ether exhibits cytotoxicity (ED50 values < 4 microg mL) against P-388 and HT-29 cell lines in vitro.

2-Desoxy-4-epi-pulchellin has potent in vitro cytotoxicities against the K562, MCF-7, Hela, DU145, U937, H1975, SGC-7901, A549, MOLT-4, and HL60 cell lines with IC50 values ranging from 0.10 to 46.7uM, while it shows significant antiviral (H1N1 and H3N2) activities, it also displays significant antimycobacterial activity (IC50=7.6 uM).

'3'-Deoxy-4-O-methylsappanol exhibits moderate cytotoxicity against cultured human melanoma HMV-II cells, with an IC50 value of 872.0 µM ± [2.4].

6-Prenylapigenin(4',5,7-Trihydroxy-6-prenylflavone) shows potent inhibitory activity on melanin formation, it may be potential sources for skin whitening agents. It also shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarci

Guajadial B acts as a Top1 catalytic inhibitor and delays Top1 poison-mediated DNA damage. Guajadial B shows cytotoxicities against five human cancer cell lines, it is the most effective having an IC50 value of 150 nM toward A549 cells.

Hispidanin B shows significant cytotoxicities against tumor cell lines SGC7901, SMMC7721, and K562, with IC50 values of 10.7, 9.8, and 13.7 uM, respectively.

Nemoralisin exhibits weak cytotoxicities (IC50>10 uM) against HepG2, AGS, MCF-7, and A-549 cancer cell lines.

Pungiolide A exhibits moderate cytotoxicities with IC50 values in the range of 0.90-6.84 uM.

Shizukaol B exerts anti-inflammatory effects in LPS-activated microglia partly by modulating JNK-AP-1 signaling pathway; it also shows significant anti-neuroinflammatory effects by inhibiting nitric-oxide (NO) production in lipopolysaccharide (LPS)-stimul

1. Shizukaol C shows anti-HIV-1 replication activities in both wild-type HIV-1 and two NNRTIs-resistant strains.
2. Shizukaol C has significant cytotoxicities against C8166 cells.

Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 + - 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 + - 24.62 microM) but is weaker than finasteride (IC50 = 0.38 + - 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-κB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7 ADR cells.