| dc.description.abstract | Chapter I
Anaphylaxis is a rare but severe allergic reaction, which has rapid onset and may put patients’ life in danger. Most common causes of anaphylaxis are food, medicines and insects. Antibiotics, non-steroidal anti-inflammatory drugs (NSAIDs) and anesthetics are the three most common causes of anaphylaxis among other medicines. Compares with the other common causes of drug-induced anaphylaxis, the diagnosis of anesthetic-induced anaphylaxis is way difficult, because that the patients used multiple drugs not only anesthetics but also induction agents during the perioperative period, which does not make the diagnosis of anesthetics hypersensitivity reaction to be as obvious as the one of other drug-induced hypersensitivity reaction. Anaphylaxis is considered to be a type I hypersensitivity reaction mediated by IgE. Hypersensitivity reactions are classified into four types. However, the detailed mechanism of anaphylaxis is still unclear. The existing in vitro tests for type I hypersensitivity, their sensitivity and specificity are poor to make the misjudgment plausible. For reasons outlined above, we cooperated with Wen-Hung Chung, M.D., Ph.D. in the study; we synthesized the analogues of fentanyl.
We synthesized FA04, FC04, FA22 and FC22. The results of in vitro tests showed that they could lead the increasing IgE, activated basophils, b cells and plasma cells. The calculation for the ratio of activated B cells is in progress, the results will reveal whether the activated B cells were truly cause by fentanyl derivatives.
Chapter II
Cancer has been a refractory disease, scientists sill found some molecules that are highly relative to cancer, and one of them is sialic acid. They also found that metastatic cancer cells have the property of expressing plenty of glycoproteins with numerous sialic acids to the terminal position on the surface. Sialic acid participated in tumor progressions. Sialylation is the attachment process of sialic acid onto other molecules, and it is mediated by sialyltransferases (STs). Sialyltransferases inhibitors may be a therapeutic treatment for cancer.
Our lab has been developing sialyltransferases inhibitors, and we have found a good sialyltransferases inhibitors based on lithocholic acids which is Lith-O-Asp. Now, we put expect on the immunomodulatory effect of fentanyl to create a series fentanyl/lithocholic acid analogs: KL03, KL04, KL05, KL06 and KL08.
We found that KL05 and KL04 have cytotoxicity and inhibition in MDA-MB-231 cells, but the inhibition may be due to their cytotoxicity. Thus, we are going to test their cytotoxicity in the normal cells to compare the result in MDA-MB-231 cells. | en_US |