Abstract
Our continuous search for marine bioactive secondary metabolites led to the screening of crude extracts from a variety of aquaculture soft corals. The ethyl acetate (EtOAc) extract of Lobophytum crassum showed a distinctive chemical profile that was different from the wild type. It demonstrated significant anti-proliferative activity against Molt 4 leukemia cell with an IC50 value of 1 μg/mL after 24 h. Chemical investigation focusing on the unique peaks in L. crassum profile led to the discovery of a new α-tocopherol crassumtocopherol C (1), and two new cembrane-based diterpenoids culobophylins D (2) and E (3), along with ten known cembranoids (4–13). The structures of these isolates were elucidated using extensive spectroscopic techniques and a comparison with previously published data of related metabolites. Compound 2 was found to possess the first identified saturated internal C4-O-C14 linkage six-membered ring among all cembrane-type diterpenoids. The anti-proliferative activity of all the isolates (except 3) was evaluated against a limited panel of leukemia cell lines (Molt 4, K562, U937, and Sup-T1). The major compounds 8 and 10 exhibited the most anti-proliferative potent effect, with IC50 values ranging from 1.2 to 7.1 μM. The Structure Activity Relationship (SAR) of the isolates suggested that the presence of lactone moieties is crucial for the anti-proliferative activity against leukemia cells. Our work indicated that the development of an efficient aquaculture protocols for soft corals led to the discovery of new secondary metabolites with unique structural features. Such protocols can lead to a sustainable supply of biologically active compounds in enough quantities for the pharmaceutical industry.
Highlights
In recent years, aquaculture techniques of soft corals witnessed significant advancements in terms of conditions and productivity
The anti-proliferative activity of the ethyl acetate (EtOAc) extracts of six cultured soft corals maintained at the National Museum of Marine Biology & Aquarium, Pingtung, Taiwan was examined and the aquaculture soft corals (Figure 1A) was selected for further study since it exhibited the most potent effect against several leukemia cells (Figure 1B)
2015CSC-2) from aquaculture L. crassum effect ofofits acetate (EtOAc) extracts displayed a similar chemical profile, but they were different from the wild sample
Summary
Aquaculture techniques of soft corals witnessed significant advancements in terms of conditions and productivity. Researchers have been able to obtain larger amounts of soft corals, and larger amounts of bioactive metabolites enabling them to investigate their biological. Mar. Drugs 2018, 16, 15; doi:10.3390/md16010015 www.mdpi.com/journal/marinedrugs. Mar. Drugs 2018, 16, 15 activities in many pharmacological assays and even producing enough quantities for clinical trials [1]. In the past few decades, a variety of aquaculture protocols for soft corals were established and the produced soft corals were extensively studied in terms of their chemical profiles and pharmacological properties. The soft coral Sinularia flexibilis was cultured by our institute and the anti-neuroinflammatory and analgesic activities of its active constituent, flexibilide, were studied
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