ASU researchers began to investigate the blue sponge Cribrochalina sp. in 1986. From this species they successively isolated Cribrostatins 1 to 5 compounds. Cribrostatins 3 and 5 disclosed high potency against a minipanel of human cancer cell lines (Mean panel GI50 values of 4.27 x 10-6M and 5.01 x 10-6M respectively) and Cribrostatins 2 and 4 had broad antimicrobial spectra.

Eventually Cribrostatin 6 was isolated from the same sponge, and its structure elucidated. When tested against a panel of human cancer cell lines, Cribrostatin 6 exhibited significant cancer cell growth inhibition (GI50 of 0.21 µg/mL against BXPC-3 cell line (pancreas adenocarcinoma), GI50 of 0.24 µg/mL against MCF-7 cell line (breast adenocarcinoma), GI50 of 0.38 µg/mL against DU-145 cell line (prostate)).

But Cribrostatin 6 also exhibited antimicrobial activity against 15 antibiotic-resistant Gram-positive bacteria and pathogenic fungi (Inhibitory concentration from 0.5 µg/mL) and against the Gram-negative bacterium Neisseria gonorrhoeae (Inhibitory concentration of 0.0625 µg/mL).

Thus, Cribrostatin 6 is a small compound combining outstanding antineoplasic, antibiotic and antifungal activities

The new compound has applications as:

• Anti-neoplasic and anti-cancer therapeutic agents
• Antibacterial and antifungal agents

Benefits and Advantages

• Diversity – Cribrostatin 6 presents a broad range of potential applications
• Synthesis – Synthesis of Cribrostatin 6 has been performed, and is described in literature

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For more information about the inventor(s) and their research, please see
Dr. Pettit's departmental webpage