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

Lai, Kuei-Hung (author)
Uppsala universitet,Avdelningen för farmakognosi,Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 944, Taiwan.;Natl Museum Marine Biol Aquarium, Pingtung 944, Taiwan.;Kaohsiung Med Univ, Coll Pharm, Grad Inst Nat Prod, Kaohsiung 807, Taiwan.
Liu, Yi-Chang (author)
Kaohsiung Med Univ Hosp, Dept Internal Med, Div Hematol Oncol, Kaohsiung 807, Taiwan.;Kaohsiung Med Univ, Coll Med, Fac Med, Dept Internal Med, Kaohsiung 807, Taiwan.
Su, Jui-Hsin (author)
Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 944, Taiwan.;Natl Museum Marine Biol Aquarium, Pingtung 944, Taiwan.
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El-Shazly, Mohamed (author)
Ain Shams Univ, Dept Pharmacognosy & Nat Prod Chem, Fac Pharm, Org African Unity St, Cairo 11566, Egypt.
Wu, Chih-Fung (author)
Kaohsiung Med Univ Hosp, Dept Surg, Div Surg Oncol, Kaohsiung 807, Taiwan.
Du, Ying-Chi (author)
Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 944, Taiwan.;Natl Museum Marine Biol Aquarium, Pingtung 944, Taiwan.;Kaohsiung Med Univ, Coll Pharm, Grad Inst Nat Prod, Kaohsiung 807, Taiwan.
Hsu, Yu-Ming (author)
Kaohsiung Med Univ, Coll Pharm, Grad Inst Nat Prod, Kaohsiung 807, Taiwan.
Yang, Juan-Cheng (author)
China Med Univ, Sch Pharm, Coll Pharm, Taichung, Taiwan.;China Med Univ Hosp, Chinese Med Res & Dev Ctr, Taichung, Taiwan.
Weng, Ming-Kai (author)
Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 944, Taiwan.
Chou, Chia-Hua (author)
Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 944, Taiwan.;Natl Museum Marine Biol Aquarium, Pingtung 944, Taiwan.
Chen, Guan-Yu (author)
China Med Univ, Sch Pharm, Coll Pharm, Taichung, Taiwan.;China Med Univ Hosp, Chinese Med Res & Dev Ctr, Taichung, Taiwan.
Chen, Yu-Cheng (author)
China Med Univ, PhD Program Canc Biol & Drug Discovery, Taichung, Taiwan.;Acad Sinica, Taichung, Taiwan.
Lu, Mei-Chin (author)
Natl Dong Hwa Univ, Grad Inst Marine Biol, Pingtung 944, Taiwan.;Natl Museum Marine Biol Aquarium, Pingtung 944, Taiwan.
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 (creator_code:org_t)
2016-10-31
2016
English.
In: Scientific Reports. - : Springer Science and Business Media LLC. - 2045-2322. ; 6
  • Journal article (peer-reviewed)
Abstract Subject headings
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  • Two new scalarane sesterterpenoids, 12 beta-(3'beta-hydroxybutanoyloxy)-20,24-dimethyl-24-oxo-scalara-16-en-25-al (1) and 12 beta-(3'beta-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 mu g/mL (125 nM) triggered mitochondrial membrane potential (MMP) disruption and apoptosis showing more potent effect than 2 and 3. The isolates inhibited topoisomerase II alpha expression. The apoptotic-inducing effect of 3 was supported by the in vivo experiment through suppressing the volume of xenograft tumor growth (47.58%) compared with the control. Compound 1 apoptotic mechanism of action in Molt 4 cells was further elucidated through inducing ROS generation, calcium release and ER stress. Using the molecular docking analysis, 1 exhibited more binding affinity to N-terminal ATP-binding pocket of Hsp90 protein than 17-AAG, a standard Hsp90 inhibitor. The expression of Hsp90 client proteins, Akt, p70(S6k), NF kappa B, Raf-1, p-GSK3 beta, and XIAP, MDM 2 and Rb2, and CDK4 and Cyclin D3, HIF1 and HSF1 were suppressed by the use of 1. However, the expression of Hsp70, acetylated tubulin, and activated caspase 3 were induced after 1 treatment. Our results suggested that the proapoptotic effect of the isolates is mediated through the inhibition of Hsp90 and topoisomerase activities.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)

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