Abstract
Five new norditerpene endoperoxides, named diacarperoxides H–L (1–5), and a new norditerpene diol, called diacardiol B (6), were isolated from the South China Sea sponge, Diacarnus megaspinorhabdosa. Their structures, including conformations and absolute configurations, were determined by using spectroscopic analyses, computational approaches and chemical degradation. Diacarperoxides H–J (1–3) showed some interesting stereochemical issues, as well as antimalarial activity.
Highlights
Malaria kills a child every minute, 154–289 million people are infected each year [1]
Antimalarial activities were determined against chloroquine sensitive (D6, Sierra Leone) and resistant (W2, Indo China) strains of Plasmodium falciparum in vitro by measuring plasmodial LDH
The NMR calculations were performed by using the Gauge-invariant atomic orbital (GIAO) method at the B3LYP/6-31G(d,p) and MPW1PW91/6-31G(d,p) levels, and the calculated chemical shifts for TMS at the corresponding levels were used as references
Summary
Malaria kills a child every minute, 154–289 million people are infected each year [1]. The plant-derived quinine family of antimalarials has provided centuries of relief for this disease. The long history of usage had, produced drug resistance, which was relieved by incorporating the artemisinin class isolated from the plant Artemisia annua [2,3]. Exploring bioactive secondary metabolites from marine invertebrates has provided us potent leads fighting against this disease [4], the marine-derived endoperoxide family has been known for decades and has generated interest for drug discovery [5,6]. Computation is seeing greater utility in the natural product field, including quantitative modeling on the molecular scale to disclose structural information, as well as in complex molecular systems to rationalize bioactivities targeting fatal diseases [7,8,9]. We report the details of the isolation and structural elucidation of these compounds
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