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Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
The isomer of fucosterol, isofucosterol, has been identified as a minor constituent of marine sponge, Gynostemma pentafillum, oat seeds and a few other plants. Isofucosterol of marine sponge is believed to be the biosynthetic precursors of the antiviral orthoesterols and weinbersterols found in the same sponge. Isofucosterol exhibits lipase inhibitory effect, suggesting that it has potential as anti-obesity agent.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
M-475271 (AZM475271) is an investigational drug targeting cancer invasion and metastasis. It is an aminoquinoline class inhibitor with high affinity and specificity for the nonreceptor tyrosine kinase (Src). In vitro AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-Src, lck, and c-yes was 0.01, 0.03, and 0.08 uM, respectively, in comparison with an IC50 of 0.7 uM AZM475271 to inhibit KDR. AZM475271 reduced tumor size, vascularity and metastasis, and increased apoptosis in human pancreatic cells grown orthotopically in nude mice. It also exhibited antiangiogenic activity in vitro and in vivo, and sensitized tumor cells to the cytotoxic effects of gemcitabine. The effect of daily oral treatment with M475271 on subcutaneous tumors and lung metastasis caused by human lung adenocarcinoma cells in NK-cell depleted SCID mice demonstrated inhibition of the growth of subcutaneous tumors via inhibition of tumor cells proliferation, VEGF production and/or vascularization in the mice in a dose-dependent manner. In the metastasis model with A549 cells, the lung weight in the M475271 (50 mg/kg)-treated group was less than that of the control group, despite no difference in the number of metastatic nodules. These findings suggest that M475271 may be efficacious in treating pancreatic adenocarcinomas and might be helpful for controlling the progression of human lung adenocarcinomas.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Tyrphostin A23 belongs to a novel class of low molecular weight proteins that inhibit protein tyrosine kinase and block the EGF-dependent autophosphorylation of the receptor. It has been considered as potential anti-cancer drug. It inhibits pancreatic cancer cell growth in vitro. Inhibition of EGF receptor by tyrphostin A23 was associated with a significantly increased proportion of apoptotic cells in human prostate cancer DU145 cell culture.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Beauvericin is a famous mycotoxin produced by many fungi, such as Beaveria bassiana and Fusarium spp. Beauvericin is a cyclic hexadepsipeptide (Figure 1) that belongs to the enniatin antibiotic family. It contains three D-hydroxyisovaleryl and three N-methylphenylalanyl residues in an alternating sequence. Beauvericin was first isolated from Beaveria bassiana, which is a common and commercial entomopathogenic mycoinsecticide. Beauvericin was one of the active constituents of B. bassiana and was confirmed to have antimicrobial and anti-tumor activities. Beauvericin has a strong antibacterial activity against human, animal and plant pathogenic bacteria with no selectively between Gram-positive and Gram-negative bacteria. The cytotoxicity of beauvericin to human tumor cells has been frequently reported.