Antileukemic Scalarane Sesterterpenoids and Meroditerpenoid from Carteriospongia (Phyllospongia) sp., Induce Apoptosis via Dual Inhibitory Effects on Topoisomerase II and Hsp90

  title={Antileukemic Scalarane Sesterterpenoids and Meroditerpenoid from Carteriospongia (Phyllospongia) sp., Induce Apoptosis via Dual Inhibitory Effects on Topoisomerase II and Hsp90},
  author={Kuei-Hung Lai and Yi-Chang Liu and Jui Hsin Su and Mohamed El‐Shazly and Chih-Fung Wu and Ying-Chi Du and Y M Hsu and Juan-Cheng Yang and Ming-kai Weng and Chia-Hua Chou and Guan-Yu Chen and Yu-Cheng Chen and Mei-Chin Lu},
  journal={Scientific Reports},
Two new scalarane sesterterpenoids, 12β-(3′β-hydroxybutanoyloxy)-20,24-dimethyl-24-oxo-scalara-16-en-25-al (1) and 12β-(3′β-hydroxypentanoyloxy)-20,24-dimethyl-24-oxo-scalara-16-en-25-al (2), along with one known tetraprenyltoluquinol-related metabolite (3), were isolated from the sponge Carteriospongia sp. In leukemia Molt 4 cells, 1 at 0.0625 μg/mL (125 nM) triggered mitochondrial membrane potential (MMP) disruption and apoptosis showing more potent effect than 2 and 3. The isolates inhibited… 
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Six new asperane-type sesterterpenoids, asperunguisins A-F (1-6), were isolated from the endolichenic fungus Aspergillus unguis and showed cytotoxicity against the human cancer cell line A549, revealing that the observed cell death was a result of G0/G1 cell cycle arrest via DNA damage followed by cellular apoptosis.
Deacetylphylloketal, a New Phylloketal Derivative from a Marine Sponge, Genus Phyllospongia, with Potent Anti-Inflammatory Activity in In Vitro Co-Culture Model of Intestine
The potential use of sponge genus Phyllospongia and its metabolites as a pharmaceutical aid in the treatment of inflammation-related diseases including IBD is suggested.
Cytotoxic Furan- and Pyrrole-Containing Scalarane Sesterterpenoids Isolated from the Sponge Scalarispongia sp.
Three furan-containing scalarane sesterterpenoids (1–3) and a novel pyrrole-containing analog (4) were isolated from the sponge Scalarispongia species. Compound 3, reported in the literature as a
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Most of the meroterpenoids possess antimicrobial, cytotoxic, antioxidant, anti-inflammatory, antiviral, enzyme inhibitory, and immunosupressive effects.


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The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(+)-turmerone, which showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II.
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The results suggested that the antileukemic effect of HQ is ROS-mediated mitochondrial apoptosis combined with the inhibitory effect on HDAC and topoisomerase activities.
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10AB-induced apoptosis is mediated through the overproduction of ROS and the disruption of mitochondrial metabolism, suggesting that ROS overproduction plays a crucial rule in the cytotoxic activity of 10AB.
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Results suggesting that PG-containing drugs may selectively kill tumour cells by generating hydrogen peroxide are reported.
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Topoisomerase II and leukemia
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Molecular mechanisms mediating antimyeloma activity of proteasome inhibitor PS-341.
Molecular mechanisms whereby PS-341 mediates anti-MM activity are demonstrated by inducing p53 and MDM2 protein expression; inducing the phosphorylation (Ser15) of p53 protein; activating c-Jun NH(2)-terminal kinase (JNK), caspase-8, and caspases-3; and cleaving the DNA protein kinase catalytic subunit, ATM, andMDM2.
Scalarane-based sesterterpenoid RCE-protease inhibitors isolated from the Indonesian marine sponge Carteriospongia foliascens.
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