Paclitaxel-antibacterial peptide conjugate, synthesis method and applications for inhibiting activity of cancer

A synthesis method and antibacterial peptide technology, applied in the field of tumor suppressor drug synthesis, can solve the problems such as the research lag in the tumor suppressor activity of LL-37

Active Publication Date: 2021-02-05
HONGHE COLLEGE
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Problems solved by technology

[0004] Through the above analysis, the existing problems and defects of the prior art are as follows: enhancing the antibacterial activity of LL-37 through molecular modification has become a research hotspot at present, but the research on the antitumor activity of LL-37 is still quite lagging behind

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  • Paclitaxel-antibacterial peptide conjugate, synthesis method and applications for inhibiting activity of cancer
  • Paclitaxel-antibacterial peptide conjugate, synthesis method and applications for inhibiting activity of cancer
  • Paclitaxel-antibacterial peptide conjugate, synthesis method and applications for inhibiting activity of cancer

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Embodiment Construction

[0039] In order to make the object, technical solution and advantages of the present invention more clear, the present invention will be further described in detail below in conjunction with the examples. It should be understood that the specific embodiments described here are only used to explain the present invention, not to limit the present invention.

[0040] The invention innovatively connects PTX and LL-24 through Mal, and the tumor suppressor activity of the PTX-LL-24 conjugate formed is much stronger than that of PTX or LL-24 alone, and there is no report on the coupling of PTX and antimicrobial peptides . LL-37, LL-24, paclitaxel (Paclitaxel, PTX), PTX-Mal-C-LL-24 (PTX-LL-24), maleiminopropionic acid (Mal).

[0041] Aiming at the problems existing in the prior art, the present invention provides a paclitaxel-antimicrobial peptide conjugate, a synthesis method, and an application for inhibiting cancer activity. The present invention will be described in detail below ...

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Abstract

The invention belongs to the technical field of synthesis of anticancer drugs, and discloses paclitaxel-antibacterial peptide conjugate, a synthesis method and applications for inhibiting the activityof cancer. The conjugate is PTX-LL-24; the amino acids at an alpha-helix region, a beta-sheet region, a transmembrane structure, signal peptide, charges, a hydrophobic region and a hydrophilic regionof LL-37 are analyzed by using a bioinformatics technique; antibacterial peptide consisting of 24 amino acids is formed through modification and named as LL-24; and a PTX-LL-24 compound can be obtained by coupling PTX with the LL-24. The inhibiting rate of the PTX-LL-24 compound to SW1990 and ME-180 cancer cells can reach 89.62% and 88.25%. The inhibition of the PTX-LL-24 compound on the two kinds of cancer cells is very obvious, so that solid foundation can be provided for the compound as a candidate drug for treating cancer.

Description

technical field [0001] The invention belongs to the technical field of anticancer drug synthesis, and in particular relates to a paclitaxel-antibacterial peptide conjugate, a synthesis method, and an application for inhibiting cancer activity. Background technique [0002] At present, paclitaxel, a new type of anti-microtubule anti-tumor drug, has long been used in the first-line treatment and subsequent treatment of various cancers. At present, there are four main PTX preparations commonly used in clinical practice: paclitaxel injection, docetaxel, and paclitaxel liposome , Paclitaxel albumin-bound, but they have the disadvantages of low water solubility and large side effects. Therefore, the development of new anticancer drugs is of great significance for cancer treatment. Antimicrobial peptides, also known as antimicrobial peptides or host defense peptides, are formed by long-term evolution in nature and widely exist in organisms such as animals, plants, and microorganism...

Claims

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Application Information

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IPC IPC(8): C07K14/00C07K1/107C07K1/04C07K1/06A61K31/4025C07D405/12A61K47/55A61K38/16A61K31/337A61P35/00
CPCC07K14/00A61K31/4025C07D405/12A61P35/00A61K47/55A61K38/16A61K31/337A61K2300/00
Inventor 谢昆王传铭
Owner HONGHE COLLEGE
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