Protein tyrosine phosphatase 1B inhibitors from Morus root bark

Cui, Long; Na, MinKyun; Oh, Hyuncheol; Bae, Eun Young; Jeong, Dae Gwin; Ryu, Seong Eon; Kim, Sohee; Kim, Bo Yeon; Oh, Won Keun; Ahn, Jong Seog

doi:10.1016/j.bmcl.2005.11.071

Cited by 142 publications

(66 citation statements)

References 23 publications

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“…The PTP1B inhibitory activities of the plant extracts were evaluated by using pNPP. 43) To each of 96 wells (100 mL final volume), 40 mL of the PTP1B enzyme [0.5 unit diluted with a PTP1B reaction buffer containing 50 mM citrate (pH 6.0), 0.1 M NaCl, 1 mM EDTA, and 1 mM DTT] was added with or without a sample in a test concentration ranging from 0.05 to 50 mg/mL for the extract and fractions, and 0.10 to 100 mM for the phlorotannins dissolved in 10% DMSO. The plate was preincubated at 37 C for 10 min, and then 50 mL of 2 mM pNPP in the PTP1B reaction buffer was added.…”

Section: Methodsmentioning

confidence: 99%

Protein Tyrosine Phosphatase 1B and α-Glucosidase Inhibitory Phlorotannins from Edible Brown Algae,Ecklonia stoloniferaandEisenia bicyclis

Moon

Islam

Ahn

et al. 2011

Bioscience, Biotechnology, and Biochemistry

137

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Section: Methodsmentioning

confidence: 99%

Protein Tyrosine Phosphatase 1B and α-Glucosidase Inhibitory Phlorotannins from Edible Brown Algae,Ecklonia stoloniferaandEisenia bicyclis

Moon

Islam

Ahn

et al. 2011

Bioscience, Biotechnology, and Biochemistry

137

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“…It has also been proposed that Sanggenon C decreases ICAM-1 protein expression at a post-translational level (11). In addition, it was reported that Sanggenon C inhibited protein tyrosine phosphatase 1B (12) and possessed the function to decrease blood pressure. Since Sanggenon C possesses the most potent cell toxicity among the flavonoids from Sangbaipi (13), it could serve as a candidate anti-cancer agent.…”

Section: Introductionmentioning

confidence: 99%

Sanggenon C decreases tumor cell viability associated with proteasome inhibition

Huang¹

2009

Front Biosci

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Several flavonoids have been reported to be proteasome inhibitors, but whether prenylated flavonoids are able to inhibit proteasome function remains unknown. We report for the first time that Sanggenon C, a natural prenylated flavonoid, inhibits tumor cellular proteasomal activity and cell viability. We found that (1) Sanggenon C inhibited tumor cell viability and induced cell cycle arrest at G0/G1 phase; (2) Sanggenon C inhibited the chymotrypsin-like activity of purified human 20S proteasome and 26S proteasome in H22 cell lysate, and Sanggenon C was able to dosedependently accumulate ubiquitinated proteins and proteasome substrate protein p27; (3) Sanggenon C-induced proteasome inhibition occurred prior to cell death in murine H22 and P388 cell lines; (4) Sanggenon C induced death of human K562 cancer cells and primary cells isolated from leukemic patients. We conclude that Sanggenon C inhibits tumor cell viability via induction of cell cycle arrest and cell death, which is associated with its ability to inhibit the proteasome function and that proteasome inhibition by Sanggenon C at least partially contributes to the observed tumor cell growth-inhibitory activity. Proteasome inhibition has been demonstrated as a novel therapeutic strategy in multiple disease models, including fibrosis (4), inflammation (5), ischemia-reperefusion injury (6), myocardial hypertrophy (7) and cancer (8). Proteasome inhibitor bortezomib (Valcade or PS-341) has been approved by the United States FDA to treat multiple myeloma. Other proteasome inhibitors are now under clinical trials for cancer therapy (8). However, there were some associated toxicity observed in the clinical trials using bortezomib (8). Therefore, there is a need to search for novel proteasome inhibitors with decreased side effect. It is an attractive idea to identify and isolate novel natural proteasome inhibitors from medicinal plants. Many of the reported natural proteasome inhibitors belong to the flavonoid family (3). Among all these reported natural flavonoid proteasome inhibitors, an aromatic ketone structure plays a very important role for binding to the threonine residue at the N terminus (Thr 1) of the proteasome subunits and inhibiting the proteasomal activities (3, 9, 10). KeywordsSeveral flavonoids have been isolated from the stem bark of Morus cathayana (SANGPAIPI), including Sanggenon C. Sanggenon C is a flavanone Diel-Alder adduct compound. Up to now, there are only a few reports on the biological and pharmacological effects of Sanggenon C. It has been reported that Sanggenon C has anti-oxidant and antiinflammation activities (2) and could inhibit TNF-alpha-stimulated cell adhesion and expression of VCAM-1 by suppressing the activation of NF-kappa B. It has also been proposed that Sanggenon C decreases ICAM-1 protein expression at a post-translational level (11). In addition, it was reported that Sanggenon C inhibited protein tyrosine phosphatase 1B (12) and possessed the function to decrease blood pressure. Since Sanggenon C possesses the mo...

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“…The bioassay-guided fractionation of 'Sang-Bai-Pi' mentioned above also resulted in isolation of mulberrofuran C 156, which inhibited PTP1B with an IC 50 of 4.9±0.2 µmol/L in a mixed-type manner [66] . The bioassay for the inhibitory effects on other PPs showed that 156 had no inhibitory effects toward VHR and PP1 at levels up to 50 µmol/L.…”

Section: Phenolics Containing Furan or Pyran Ringsmentioning

confidence: 99%

“…From the extract of 'Sang-Bai-Pi', sanggenons C 116, G 117, and kuwanon L 118 were isolated [66] . Compounds 116-118 inhibited PTP1B (IC 50 values ranging from 1.6±0.3 to 16.9±1.1 μmol/L) with good selectivity over other PPs, expecially 116 and 118, which showed no inhibitory effects toward VHR and PP1 at levels up to 50 μmol/L.…”

Section: Flavonoidsmentioning

confidence: 99%

Natural products possessing protein tyrosine phosphatase 1B (PTP1B) inhibitory activity found in the last decades

2012

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This article provides an overview of approximately 300 secondary metabolites with inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), which were isolated from various natural sources or derived from synthetic process in the last decades. The structure-activity relationship and the selectivity of some compounds against other protein phosphatases were also discussed. Potential pharmaceutical applications of several PTP1B inhibitors were presented.

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Protein tyrosine phosphatase 1B inhibitors from Morus root bark

Cited by 142 publications

References 23 publications

Protein Tyrosine Phosphatase 1B and α-Glucosidase Inhibitory Phlorotannins from Edible Brown Algae,Ecklonia stoloniferaandEisenia bicyclis

Protein Tyrosine Phosphatase 1B and α-Glucosidase Inhibitory Phlorotannins from Edible Brown Algae,Ecklonia stoloniferaandEisenia bicyclis

Sanggenon C decreases tumor cell viability associated with proteasome inhibition

Natural products possessing protein tyrosine phosphatase 1B (PTP1B) inhibitory activity found in the last decades

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