Hubei University of Technology

Hongmei Li

Yajie Tang

Wei Zhao

Yong Yang

Quan Zhang

Kaizhi Jia

Yanghua Xu

Jianlong Li

Embodiment of the present invention discloses a kind of methionine lyase and its encoding gene and biosynthetic method. According to the present invention, the gene encoding methionine lyase as shown in SEQ ID No. 1 is separated from the genome of. Embodiment of the present invention further provides an efficient biosynthetic method of methionine lyase, comprising: (1) cloning gene (shown in SEQ ID No.1) encoding methionine degradation enzyme into a yeast expression vector to construct recombinant yeast expression vector; (2) transforming the recombinant yeast expression vector intoto obtain expression strain; (3) inducing the expression strain to express the methionine lyase, collecting induced strains, purifying expressed recombinant methionine lyase. Purity of recombinant methionine lyase prepared according to the present invention is above 90%, and its efficiency of degradating methionine can reach 0.53&#xb1;0.0030 &#x3bc;M MTL&#xb7;h&#xb7;mg protein.

Methionine lyase, encoding gene and biosynthetic method thereof

The present invention discloses a sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof. The present invention introduces a rigid aromatic heterocyclic compound, as well as a further sulfonamidated product of 3-amino-5-mercapto-1,2,4-triazole, 2-amino-5-mercapto-1,3,4-thiadiazole, 4-methylbenzenesulfonyl chloride, or 4-methoxybenzenesulfonyl chloride as a substituent group, into position 4 of the C-ring of podophyllotoxin or 4'-demethylepipodophyllotoxin to obtain the podophyllotoxin derivative shown in formula (V), said derivative having significantly increased antitumor activity and reduced toxic side effects. Experiments on in vitro tumor cell inhibition indicate that the antitumor activity of the compound of formula (V) of the present invention is significantly higher than the antitumor activity of podophyllotoxin or 4&#x2032;-demethylepipodophyllotoxin.

Sulfur-substituted podophyllotoxin derivative, synthesis method thereof, and use thereof

The present invention discloses an anilino-substituted podophyllin derivative having antitumor activity, method for preparation thereof, and use thereof. By means of anilino reactions, the present invention introduces 4-chloro-3-methylaniline, 3-fluoro-4-methoxyaniline, 4,4'-diaminodiphenylmethane, o-anisidine, 4-chloro-2-aminoanisole, anthranilonitrile, 2,6-dichloro-4-aminophenol, N,N-dimethylamino meta-aniline, 2-ethyl-5-nitroaniline, 2 2&#x2032;-diaminodiphenylsulfide, or 2-aminobenzotrifluoride into position 4 of the active C-ring of podophyllotoxin or 4&#x2032;-demethylepipodophyllotoxin to obtain the aniline-substituted podophyllotoxin derivative shown in formula (V); by means of multi-pathway and multi-target effects on tumor cells, said derivative has significantly increased antitumor activity, and can be prepared as an antineoplastic drug and applied in clinical antitumor therapy.

Anilino podophyllin derivative having antitumor activity, method for preparation thereof, and use thereof

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Wuhan, China

Hongmei Li