Pharmaceutical composition comprising THA as active ingredient for treating breast cancer
Inventors
Kang, Keon Wook • Oh, Kwang-Seok • KIM, YoungChul • JEONG, Sung Baek
Assignees
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Publication Number
US-11793772-B2
Publication Date
2023-10-24
Expiration Date
Abstract
Provided is a composition comprising 2,4,6-trihydroxyacetophenone (THA) as an active ingredient, and a method for preventing, alleviating or treating breast cancer using the composition by inhibiting the activity of polo-like kinase 1 (PlK1).
Core Innovation
The document describes a breast-cancer treatment or alleviation composition containing 2,4,6-trihydroxyacetophenone (THA) as an active ingredient. The target disease scope is tamoxifen-resistant breast cancer, and THA is presented with therapeutic rationale related to inhibition of polo-like kinase 1 (Plk1). The content includes chemical structure context for THA, including Formula 1, in connection with its use in the breast-cancer compositions.
The described mechanism links THA to Plk1 activity inhibition and downstream effects including cdc25c and cyclin B1. The document reports that THA reduces Plk1 downstream cdc25c and increases cyclin B1, and that these effects are associated with inhibition of proliferation and induction of S-phase arrest and increased apoptosis in tamoxifen-resistant breast cancer cells.
The document further reports antitumor activity in a xenograft mouse model (TAMR-MCF-7) in which THA reduces tumor size/weight, with decreased PCNA and increased TUNEL, and with inhibited cdc25c. The document also states efficacy after oral dosing, and it links THA sensitivity to Plk1 expression in human breast cancer tissues using a cell-line panel showing higher Plk1 expression correlates with THA sensitivity (IC50).
Additionally, the document indicates that Plk1 expression and distribution are examined in human breast cancer tissues, and that THA shows selective activity toward breast cancer cells characterized by higher Plk1 expression. The content includes comparative context involving tamoxifen and BI-2536, positioned around the tamoxifen-resistant and Plk1-related therapeutic framework.
Claims Coverage
The partial content provides two independent claims, each centered on administering a THA-containing composition to an individual with tamoxifen-resistant breast cancer. Across the independent claims, the inventive focus is THA as the active ingredient for treating or alleviating tamoxifen-resistant breast cancer, with an added Plk1 activity-inhibition requirement appearing in the dependent claim members.
THA pharmaceutical treatment of tamoxifen-resistant breast cancer
Administering a pharmaceutical composition comprising 2,4,6-trihydroxyacetophenone (THA) as an active ingredient to an individual in need thereof, wherein the breast cancer is tamoxifen-resistant breast cancer.
THA health functional food alleviation of tamoxifen-resistant breast cancer
Administering a health functional food composition comprising 2,4,6-trihydroxyacetophenone (THA) as an active ingredient to an individual in need thereof, wherein the breast cancer is tamoxifen-resistant breast cancer.
In the provided independent claims, THA is administered either via a pharmaceutical composition or a health functional food composition to treat or alleviate tamoxifen-resistant breast cancer. Dependent claim members further specify that the administered THA-containing composition inhibits polo-like kinase 1 (Plk1) activity.
Stated Advantages
THA reduces Plk1 downstream cdc25c and increases cyclin B1.
THA inhibits proliferation and induces S-phase arrest in tamoxifen-resistant breast cancer cells.
THA increases apoptosis in tamoxifen-resistant breast cancer cells.
In a xenograft mouse model, THA reduces tumor size/weight.
In the xenograft model, THA decreases PCNA and increases TUNEL.
THA inhibits cdc25c in the xenograft model.
THA is reported to have efficacy after oral dosing.
Higher Plk1 expression is reported to correlate with THA sensitivity (IC50), and THA shows selective activity toward high-Plk1-expressing breast cancer cells.
Documented Applications
Treating breast cancer by administering a pharmaceutical composition comprising THA when the breast cancer is tamoxifen-resistant breast cancer.
Alleviating breast cancer by administering a health functional food composition comprising THA when the breast cancer is tamoxifen-resistant breast cancer.
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