Pharmaceutical composition comprising THA as effective ingredient for treatment of prostate cancer
Inventors
Kang, Keon Wook • JEONG, Sung Baek
Assignees
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Publication Number
US-11484511-B2
Publication Date
2022-11-01
Expiration Date
Abstract
The present invention relates to a composition comprising 2,4,6-trihydroxyacetophenone (THA) as an effective ingredient for prevention or treatment of prostate cancer. THA in the present invention is a main ingredient of Curcuma comosa. The composition of the present invention effectively inhibits the growth of prostate cancer by regulating in particular the activity of polo-like kinase 1 (PLK1) and thus is expected to find useful applications in use in the prevention, alleviation, and treatment of prostate cancer in future.
Core Innovation
The invention discloses a pharmaceutical composition containing 2,4,6-trihydroxyacetophenone (THA) as an effective ingredient. The described approach is directed to treating prostate cancer by administering the pharmaceutical composition to a subject in need, wherein the prostate cancer is prostate cancer with overexpressed polo-like kinase-1 (PLK1). THA is described as a main constituent of Curcuma comosa.
The disclosed composition is stated to inhibit PLK1 activity and related signaling, including cdc25c and cyclin B1 signaling, in prostate cancer contexts. The disclosure further states that the composition increases caspase-3/7 activity and apoptotic index. In addition, it is stated that the composition blocks cell-cycle progression at G2/M and is associated with apoptosis-related markers.
The disclosure includes exemplary findings in prostate cancer cell lines and models, including LnCaP, PC3, C4-2, and castration-resistant models. It states that PLK1 overexpression is shown in castration-resistant/AR-negative cells. It further states that THA-matched proliferation inhibition is shown to correspond to the PLK1 inhibitor BI2536 in high-PLK1 cells, together with apoptosis and cell-cycle effects.
Claims Coverage
The partial content provides one independent claim focusing on a method of treating prostate cancer with overexpressed PLK1 using a THA-containing pharmaceutical composition. The claim includes a single core inventive concept centered on the PLK1-overexpression-defined disease context and the use of THA as the effective ingredient.
Administering THA-containing pharmaceutical composition for PLK1-overexpressed prostate cancer treatment
A method for treating prostate cancer comprising administering a pharmaceutical composition comprising 2,4,6-trihydroxyacetophenone (THA) represented by Chemical Formula 1 or a pharmaceutically acceptable salt thereof as an effective ingredient to a subject in need of treatment, wherein the prostate cancer is prostate cancer with overexpressed polo-like kinase-1 (PLK1).
Across the provided independent claim, the inventive focus is administering a THA (Chemical Formula 1 or a pharmaceutically acceptable salt) pharmaceutical composition to treat prostate cancer specifically characterized by PLK1 overexpression.
Stated Advantages
Inhibits PLK1 activity and related cdc25c/cyclin B1 signaling.
Increases caspase-3/7 activity and apoptotic index.
Blocks cell-cycle progression at G2/M.
Documented Applications
Prevention or treatment of prostate cancer, particularly prostate cancer with PLK1 overexpression (including prostate cancer with PLK1 overexpression in castration-resistant/AR-negative contexts).
Use evaluated in prostate cancer cell lines and models including LnCaP, PC3, C4-2, and castration-resistant models, with comparisons to the PLK1 inhibitor BI2536 in high-PLK1 cells.
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