Isolation and Amino Acid Sequences of Two Trypsin Inhibitors from the Seeds of Bitter Gourd (<i>Momordica charantia</i>)

Miura, Susumu; Funatsu, Gunki

doi:10.1271/bbb.59.469

Cited by 14 publications

(10 citation statements)

References 5 publications

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“…Previous studies have established the presence of low molecular weight protease inhibitors in BG seeds. Two novel trypsin inhibitors, MCTI-II’ and BGIT, have been purified from BG and their amino acid sequence have been elucidated 21 . MCTI-II’ consists of 27 amino acid residues while the BGIT is made up of 68 amino acid residues and is capable of inhibiting not only trypsin but also subtilisin Carlsberg.…”

Section: Resultsmentioning

confidence: 99%

BG-4, a novel anticancer peptide from bitter gourd (Momordica charantia), promotes apoptosis in human colon cancer cells

Dia

Krishnan

2016

Sci Rep

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Momordica charantia is a perennial plant with reported health benefits. BG-4, a novel peptide from Momordica charantia, was isolated, purified and characterized. The trypsin inhibitory activity of BG-4 is 8.6 times higher than purified soybean trypsin inhibitor. The high trypsin inhibitory activity of BG-4 may be responsible for its capability to cause cytotoxicity to HCT-116 and HT-29 human colon cancer cells with ED50 values of 134.4 and 217.0 μg/mL after 48 h of treatment, respectively. The mechanism involved in the cytotoxic effect may be associated with induction of apoptosis as evidenced by increased percentage of HCT-116 and HT-29 colon cancer cells undergoing apoptosis from 5.4% (untreated) to 24.8% (BG-4 treated, 125 μg/mL for 16 h) and 8.5% (untreated) to 31.9% (BG-4 treated, 125 μg/mL for 16 h), respectively. The molecular mechanistic explanation in the apoptosis inducing property of BG-4 is due to reduced expression of Bcl-2 and increased expression of Bax leading to increased expression of caspase-3 and affecting the expression of cell cycle proteins p21 and CDK2. This is the first report on the anti-cancer potential of a novel bioactive peptide isolated from Momordica charantia in vitro supporting the potential therapeutic property of BG-4 against colon cancer that must be addressed using in vivo models of colon carcinogenesis.

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Section: Resultsmentioning

confidence: 99%

BG-4, a novel anticancer peptide from bitter gourd (Momordica charantia), promotes apoptosis in human colon cancer cells

Dia

Krishnan

2016

Sci Rep

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“…The presence of trypsin inhibitors (Miura and Funatsu, 1995;Hamato et al, 1995;Chakraborty et al, 2000), elastase inhibitors (Hamato et al, 1995), guanylate cyclase inhibitors (Vesely et al, 1977;Takemoto et al, 1980) and alpha-glucosidase inhibitor like D-(+)-trehalose are reported (Matsuur et al, 2002).…”

Section: Phytochemistrymentioning

confidence: 98%

Pharmacological actions and potential uses of Momordica charantia: a review

Grover

Yadav

2004

Journal of Ethnopharmacology

687

380

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“…13 Trypsin inhibitor, also named as bitter gourd trypsin inhibitor or MC trypsin inhibitor, has been isolated from MC, and its amino acid sequences have been identified. 14 Trypsin inhibitor consists of 68 amino acid residues and inhibits not only trypsin but also subtilisin Carlsberg. In this study, we renamed this protein as MC IR-binding protein (mcIRBP) because of its novel function on glucose homeostasis.…”

Section: ■ Introductionmentioning

confidence: 99%

“…By proteomic and docking analyses, we have found that trypsin inhibitor might interact with IR . Trypsin inhibitor, also named as bitter gourd trypsin inhibitor or MC trypsin inhibitor, has been isolated from MC, and its amino acid sequences have been identified . Trypsin inhibitor consists of 68 amino acid residues and inhibits not only trypsin but also subtilisin Carlsberg.…”

Section: Introductionmentioning

confidence: 99%

A Novel Insulin Receptor-Binding Protein from Momordica charantia Enhances Glucose Uptake and Glucose Clearance in Vitro and in Vivo through Triggering Insulin Receptor Signaling Pathway

et al. 2014

J. Agric. Food Chem.

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Diabetes, a common metabolic disorder, is characterized by hyperglycemia. Insulin is the principal mediator of glucose homeostasis. In a previous study, we identified a trypsin inhibitor, named Momordica charantia insulin receptor (IR)-binding protein (mcIRBP) in this study, that might interact with IR. The physical and functional interactions between mcIRBP and IR were clearly analyzed in the present study. Photo-cross-linking coupled with mass spectrometry showed that three regions (17-21, 34-40, and 59-66 residues) located on mcIRBP physically interacted with leucine-rich repeat domain and cysteine-rich region of IR. IR-binding assay showed that the binding behavior of mcIRBP and insulin displayed a cooperative manner. After binding to IR, mcIRBP activated the kinase activity of IR by (5.87 ± 0.45)-fold, increased the amount of phospho-IR protein by (1.31 ± 0.03)-fold, affected phosphoinositide-3-kinase/Akt pathways, and consequently stimulated the uptake of glucose in 3T3-L1 cells by (1.36 ± 0.12)-fold. Intraperitoneal injection of 2.5 nmol/kg mcIRBP significantly decreased the blood glucose levels by 20.9 ± 3.2% and 10.8 ± 3.6% in normal and diabetic mice, respectively. Microarray analysis showed that mcIRBP affected genes involved in insulin signaling transduction pathway in mice. In conclusion, our findings suggest that mcIRBP is a novel IRBP that binds to sites different from the insulin-binding sites on IR and stimulates both the glucose uptake in cells and the glucose clearance in mice.

show abstract

Isolation and Amino Acid Sequences of Two Trypsin Inhibitors from the Seeds of Bitter Gourd (Momordica charantia)

Cited by 14 publications

References 5 publications

BG-4, a novel anticancer peptide from bitter gourd (Momordica charantia), promotes apoptosis in human colon cancer cells

BG-4, a novel anticancer peptide from bitter gourd (Momordica charantia), promotes apoptosis in human colon cancer cells

Pharmacological actions and potential uses of Momordica charantia: a review

A Novel Insulin Receptor-Binding Protein from Momordica charantia Enhances Glucose Uptake and Glucose Clearance in Vitro and in Vivo through Triggering Insulin Receptor Signaling Pathway

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