Alpha-momorcharin possessing high immunogenicity, immunotoxicity and hepatotoxicity in SD rats

Meng, Yao; Liu, Bin; Lei, Ning; Zheng, Jie; He, Qianchuan; Li, Dan; Zhao, Xiaobo; Shen, Fubing

doi:10.1016/j.jep.2011.11.057

Cited by 31 publications

(28 citation statements)

References 29 publications

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“…Momordin A was matched to the highest Mascot score and sequence coverage relative to the other proteins, which suggested that it is abundant in BMSPs. This conclusion is consistent with Meng's study [52]. Since the potent ACEI peptide VY-7 is derived from momordin A, this implies that the production of BMSP lysate with high concentration of VY-7 is promising.…”

Section: Protein Profiling By Sds-pagesupporting

confidence: 91%

Screening, discovery, and characterization of angiotensin-I converting enzyme inhibitory peptides derived from proteolytic hydrolysate of bitter melon seed proteins

Priyanto

Doerksen

Chang

et al. 2015

Journal of Proteomics

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Section: Protein Profiling By Sds-pagesupporting

confidence: 91%

Screening, discovery, and characterization of angiotensin-I converting enzyme inhibitory peptides derived from proteolytic hydrolysate of bitter melon seed proteins

Priyanto

Doerksen

Chang

et al. 2015

Journal of Proteomics

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“…In the animals treated with the low dose of a-MMC (0.03 mg/kg), only a mild toxic reaction was observed. These phenomena were consistent with our previous studies in rats (Meng et al, 2012;Zheng et al, 2012) and again verified that a-MMC has a strong toxic effect correlated with the dosage. However, following PEGylation, the toxicity of a-MMC was significantly reduced.…”

Section: Antitumor Efficacy Studies In Vivosupporting

confidence: 93%

“…However, as proteins originating from plants, RIPs have a wide range of toxic side effects in our inchoate studies (Meng et al, 2012). These side effects include severe systemic anaphylaxis, immunogenicity and toxicity such as hepatotoxicity and bone marrow inhibition.…”

Section: Introductionmentioning

confidence: 99%

PEGylation alleviates the non-specific toxicities of Alpha-Momorcharin and preserves its antitumor efficacy in vivo

Deng

Zheng

et al. 2014

Drug Delivery

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Alpha-Momorcharin (α-MMC) is a ribosome inactivating protein from Momordica charantia with anti-tumor activity. Previously, we had observed that modification of α-MMC with polyethylene glycol (PEG) could reduce toxicity, but it also reduces its anti-tumor activity in vitro. This study aims to investigate whether the metabolism-extended properties of α-MMC resulting from PEGylation could preserve its anti-tumor efficacy in vivo through pharmacokinetics and antitumor experiments. The pharmacokinetics experiments were conducted in rats using the TCA (Trichloroacetic Acid) method. Antitumor activity in vivo was investigated in murine mammary carcinoma (EMT-6) and human mammary carcinoma (MDA-MB-231) transplanted tumor mouse models. The results showed that PEGylation increased the plasma half-life of α-MMC in rats from 6.2-7.5 h to 52-87 h. When administered at 1 mg/kg, α-MMC-PEG and α-MMC showed similar anti-tumor activities in vivo, with a T/C% of 38.56% for α-MMC versus 35.43% for α-MMC-PEG in the EMT-6 tumor model and 36.30% for α-MMC versus 39.88% for α-MMC-PEG in the MDA-MB-231 tumor model (p > 0.05). Importantly, at the dose of 3 mg/kg, all the animals treated with α-MMC died while the animals treated with α-MMC-PEG exhibited only moderate toxic reactions, and α-MMC-PEG exhibited improved anti-tumor efficacy with a T/C% (relative tumor growth rate) of 25.18% and 21.07% in the EMT-6 and MDA-MB-231 tumor models, respectively. The present study demonstrates that PEGylation extends the half-life of α-MMC and alleviates non-specific toxicity, thereby preserving its antitumor efficacy in vivo, and a higher lever of dosage can be used to achieve better therapeutic efficacy.

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“…(117) Finally, Meng and co-workers reported that α-momorcharin, a bioactive compound isolated and purified from bitter melon seeds, exhibited immunomodulatory properties. (118) However, their results showed that high doses or long-term consumption of alpha-momorcharin could lead to toxicity.…”

Section: Wound-healing Antimicrobial and Immunomodulatory Effectsmentioning

confidence: 99%

Bitter melon (Momordica charantiaL.) bioactive composition and health benefits: A review

Tan

Kha

Parks

et al. 2015

Food Reviews International

115

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Running head: Bitter Melon: its composition and health benefitsBitter melon (Momordica charantia L.) has traditionally been used as medicinal foods in many developing countries. It is a tropical fruit claimed to have therapeutic effects due to its content of bioactive compounds. The present review is an attempt to highlight the bitter melon varieties, bioactive composition that linked to its therapeutic effects, especially anti-diabetics, in vitro and in vivo models and understanding the mechanisms of actions of bitter melon that associated with epidemiological evidences. This paper also outlines a proposed processing scheme aiming to fully utilise bitter melon and further add values to this fruit.

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Alpha-momorcharin possessing high immunogenicity, immunotoxicity and hepatotoxicity in SD rats

Cited by 31 publications

References 29 publications

Screening, discovery, and characterization of angiotensin-I converting enzyme inhibitory peptides derived from proteolytic hydrolysate of bitter melon seed proteins

Screening, discovery, and characterization of angiotensin-I converting enzyme inhibitory peptides derived from proteolytic hydrolysate of bitter melon seed proteins

PEGylation alleviates the non-specific toxicities of Alpha-Momorcharin and preserves its antitumor efficacy in vivo

Bitter melon (Momordica charantiaL.) bioactive composition and health benefits: A review

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