Additional Bioactive Compounds and Trilobacin, a Novel Highly Cytotoxic Acetogenin, from the Bark of Asimina triloba

Abstract

Fractionation of the EtOH extract of the bark of Asimina triloba, monitoring by brine shrimp lethality, has led to the isolation and structural elucidation of a novel highly cytotoxic Annonaceous acetogenin, trilobacin [1], in addition to six known compounds: asimicin 2], bullatacin [3], bullatacinone [4], N-p-coumaroyltyramine [5], N-trans-feruloyltyramine [6], and (+)-syringaresinol [7]. Acetogenin 1 was identified as a diastereomer of asimicin [2] by spectral and chemical methods, and both 1 and 2 showed potent and selective cytotoxicities in the NCI human tumor cell line screen.

Secondary metabolites, antimicrobial, brine shrimp lethality & 4 th instar Culex quinquefasciatus mosquito larvicidal screening of organic & inorganic root extracts of Microcos paniculata.

“…This observation clearly indicates that the existence of non-polar residues in the extracts which have higher antimicrobial abilities. Brine shrimp lethality bioassay is widely used in the bioassay for the bioactive compounds [16,26]. In toxicity evaluation of plant extracts by Brine shrimp lethality bioassay LC 50 values lower than 1000 μg/ml are considered bioactive [16].The Brine Shrimp Lethality Bioassay also indicates antifungal effects, pesticidal effects, teratogenic effects, toxicity to environment and many more [27].…”

Dietary Administration ofAsimina triloba.(Paw Paw) Extract Increases Tumor Latency inN.-Methyl-N.-nitrosourea–Treated Rats

“…Annonaceous acetogenins may be among the most potent cytotoxic agents with ED 50 values of <10 −9 ng/mL reported for trilobacin (Zhao et al, 1994) and asiminocin (Zhao et al, 1992) in several human tumor cell lines. However, different tumor cell lines show notable differences in their susceptibility to the same acetogenin (Bermejo et al, 2005).…”

“…Bullatacin ( Fig. 1), asimicin, and trilobacin represent the most potent and major bioactive acetogenins that are found in this paw paw extract (Hui et al, 1989;Zhao et al, 1992).…”

In vitro antimicrobial and cytotoxicity screening of n-hexane, chloroform and ethyl acetate extracts of Lablab purpureus (L.) leaves

“…A postulation denoted that by 2010, at least two-thirds of Americans will opt for alternative therapies (Zhao et al, 1992). The non prescription use of medicinal plants is cited today as an important health problem, in particularly their toxicity to the kidney (Humber, 2002).…”