Dr Edmond Ma says the new rhodium(III) complex has the potential to be used in the treatment of skin cancer.


馬迪龍博士指出新研發的複合物有望進一步研製成為有效的抗腫瘤藥物。

The rhodium(III) complex was able to bind to the SH2 domain of STAT3, thereby inhibiting its activity.


研究證實銠(III)複合物有抑制腫瘤生長的效果。

Treatment with rhodium(III) complex inhibited the growth of melanoma xenografts in a mouse model (below).


腫瘤切片經接受新複合物實驗後(下圖),與沒有接受複合物(上圖)比較,體積和重量明顯減少。

Date: 19 May 2014 (Monday)

Archive

HKBU scholar discovers compound for potential treatment of skin cancer

浸大學者成功研發化合物抑制腫瘤 有望用於治療皮膚癌

Dr Edmond Ma Dik-lung, Assistant Professor of the Department of Chemistry of HKBU, in collaboration with a research team led by Dr Duncan Leung Chung-hang, Associate Professor, Institute of Chinese Medical Sciences of the University of Macau, and experts from Kaohsiung Medical University in Taiwan, have become the first in the world to successfully develop a novel compound that could potentially be used to treat skin cancer. The study entitled “Antagonising STAT3 Dimerization by a Rhodium(III) Complex” was published in the prestigious chemistry journal Angewandte Chemie (International Edition), and was selected as a “Very Important Paper” by the editors of the journal.

Signal transducer and activator of transcription 3 (STAT3) is a signaling protein that is linked to the development of multiple types of cancer in humans, including skin cancer. Dr Ma and his collaborators hypothesised that by blocking the activity of STAT3, a new treatment for skin cancer could potentially be developed. In their study, a rhodium(III) metal complex was discovered from a series of complexes as a potent inhibitor of STAT3 activity. This compound blocked the effects of STAT3 in the living cells of mice bearing xenografts of melanoma, which is the most aggressive and dangerous form of skin cancer in humans. More importantly, the treatment of mice carrying melanoma xenografts with the rhodium(III) complex led to a reduction in tumour size and weight, and reduced the formation of new blood vessels around the tumour site. These results demonstrated that the rhodium(III) complex was able to effectively hinder the growth of melanoma in the mouse model.
 
Dr Ma said, “This study is important because it shows that by inhibiting the activity of STAT3 in cells, an effective treatment for melanoma could potentially be developed. In addition, our team is the first in the world to utilise a rhodium(III) complex to inhibit STAT3 directly. Our experiments demonstrating the efficacy of the rhodium(III) complex against melanoma in the animal model are a stepping stone towards developing this compound as an anti-cancer agent for potential human use.”

浸大化學系助理教授馬迪龍博士,聯同澳門大學中華醫藥研究院副教授梁重恆博士和台灣高雄醫科大學的專家,全球首次成功研發了一種新的金屬複合物「銠(III)」,有望用於治療皮膚癌。研究論文〈直接抑制STAT3二聚化的複合物銠〉已刊登於國際期刊《Angewandte Chemie》(國際版,2014年),並獲得編輯評選為「非常重要論文」。

「訊號傳導和轉錄激活因子3」(STAT3)訊號蛋白經過二聚化過程(dimerisation)後可以導致人體內各種癌症(包括皮膚癌)。馬迪龍博士與團隊提出抑制STAT3二聚化的活動,有機會抑制皮膚惡性腫瘤。這次研究中,團隊從一系列的金屬複合物中篩選出銠(III)作為主要的抑制劑。實驗顯示,該複合物能抑制患有黑色素瘤皮膚癌的老鼠體內惡性腫瘤的生長(黑色素瘤皮膚癌是最嚴重及死亡率最高的人類皮膚癌)。更重要是老鼠接受銠(III)複合物治療後,惡性腫瘤的大小和重量明顯減少,亦能抑制腫瘤附近血管增生的情況。因此,研究結果顯示銠(III)複合物有效抑制老鼠內黑色素瘤的生長。

馬博士說﹕「今次研究結果非常重要,因為抑制細胞內致癌的STAT3活動,便有機會有效抑制黑色素瘤的生長。此外,我們的團隊是全球首次發現銠(III)這種複合物可直接抑制STAT3蛋白的二聚化活動。我們的實驗顯示了銠(III)複合物可有效用於動物身上對抗黑色素瘤,為日後研發人類抗癌藥物奠下了重要的基礎。」