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studyforhope 在Medhelp上 回答 Squalamine问题:
[stephenw]:
What is your view on Squalamine , the molecule that interferes with the surface membrane of many types of cells, including the hepatocytes?
[studyforhope]:
Thanks for the PNAS paper re squalamine. I had it, but did not pay detailed attention yet to the in vitro testing on HBV. The testing was done in a somewhat strange format, normally you expect IC 50 and IC90 in micromols.
It appears that the anti HBV activity is not very strong. This compound will have limiting toxicity, since it alters the electrical charge on the cells membrane by incorporating a cholesterol like molecule with a plus charge due to the amine group, that will tend to neutralize the normal negative charge due to the phospholipid head groups. This will lead to profound changes in the functionality of the mem brane and the proteins associated with it, which can, hopefully disturb viral mechanisms before fundamental cell mechanisms are dangerously influenced.
At 20microgram/ml they found already cytotoxic changes in the test system.
It would be good to see a duck or woodchuck study with this compound. |
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