Structure-activity relationship of citrus segment membrane RG-I pectin against galectin-3: The galactan is not the only important factor

Wu, Dongmei
Zheng, Jiaqi
Hu, Weiwei
Zheng, Xiaoliang
He, Qiaojun
Linhardt, Robert J.
Ye, Xingqian
Chen, Shiguo
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Biology , Chemistry and chemical biology , Chemical and biological engineering , Biomedical engineering
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Structure-activity relationship of citrus segment membrane RG-I pectin against galectin-3: The galactan is not the only important factor, D. Wu, J. Zheng, W. Hu, X. Zheng, Q. He, R. J. Linhardt, X. Ye, S. Chen, Carbohydrate Polymers, 245, 116526, 2020.
Rhamnogalacturonan I (RG-I) pectin are regarded as strong galectin-3 (Gal-3) antagonist because of galactan sidechains. The present study focused on discussing the effects of more structural regions in pectin on the anti-Gal-3 activity. The water-soluble pectin (WSP) recovered from citrus canning processing water was categorized as RG-I pectin. The controlled enzymatic hydrolysis was employed to sequentially remove the α-1,5-arabinan, homogalaturonan and β-1,4-galactan in WSP. The Gal-3-binding affinity KD (kd/ka) of WSP and debranched pectins were calculated to be 0.32 μM, 0.48 μM, 0.56 μM and 1.93 μM. Moreover, based on the more sensitive cell line (MCF-7) model, the IC30 value of WSP was lower than these of modified pectins, indicating decreased anti-Gal-3 activity. Our results suggested that the total amount of neutral sugar sidechains, the length of arabinan and cooperation between HG and RG-I played important roles in the anti-Gal-3 activity of WSP, not the Gal/Ara ratio or RG-I/HG ratio. These results provided a new insight into structure-activity relationship of citrus segment membrane RG-I as a galectin-3 antagonist and a new functional food.
Carbohydrate Polymers, 245, 116526
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The Linhardt Research Labs.
The Shirley Ann Jackson, Ph.D. Center for Biotechnology and Interdisciplinary Studies (CBIS)
The Linhardt Research Labs Online Collection
Rensselaer Polytechnic Institute, Troy, NY
Carbohydrate Polymers