Chemical conjugation of muramyl dipeptide and paclitaxel to explore the combination of immunotherapy and chemotherapy for cancer.
Paclitaxel (Taxol) conjugated to muramyl dipeptide (MDP) is described. Biological testing showed that the conjugation of MDP at 2'-O-paclitaxel (2'- O -MTC-01) not only has antitumor activity, but also have immunoenhancement capacity. Compared with paclitaxel or MDP alone or with a mixture of paclitaxel + MDP, 2'- O -MTC-01 significantly increases the production and expression of TNF-alpha and IL-12 from mouse peritoneal macrophages, which demonstrates a synergism of MDP and paclitaxel in one conjugated molecule.
Li
Xuqin
X
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Yu
Junli
J
Xu
Song
S
Wang
Nan
N
Yang
Hongzhen
H
Yan
Zheng
Z
Cheng
Guifang
G
Liu
Gang
G
D000119:Acetylmuramyl-Alanyl-Isoglutamine / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004359:Drug Therapy, Combination; D005786:Gene Expression Regulation / Q000187:drug effects; D006801:Humans; D007167:Immunotherapy; D018664:Interleukin-12 / Q000235:genetics / Q000378:metabolism; D017737:Macrophages, Peritoneal / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D017239:Paclitaxel / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D014409:Tumor Necrosis Factor-alpha / Q000235:genetics / Q000378:metabolism
D014409:Tumor Necrosis Factor-alpha; D018664:Interleukin-12; D000119:Acetylmuramyl-Alanyl-Isoglutamine; D017239:Paclitaxel