Chinese Journal of Integrative Medicine

, Volume 24, Issue 3, pp 237–240 | Cite as

Chinese Medicine Amygdalin and β-Glucosidase Combined with Antibody Enzymatic Prodrug System As A Feasible Antitumor Therapy

  • Yun-long Li
  • Qiao-xing Li
  • Rui-jiang Liu
  • Xiang-qian Shen
Academic Exploration


Amarogentin is an efficacious Chinese herbal medicine and a component of the bitter apricot kernel. It is commonly used as an expectorant and supplementary anti-cancer drug. β-Glucosidase is an enzyme that hydrolyzes the glycosidic bond between aryl and saccharide groups to release glucose. Upon their interaction, β-glucosidase catalyzes amarogentin to produce considerable amounts of hydrocyanic acid, which inhibits cytochrome C oxidase, the terminal enzyme in the mitochondrial respiration chain, and suspends adenosine triphosphate synthesis, resulting in cell death. Hydrocyanic acid is a cell-cycle-stage-nonspecific agent that kills cancer cells. Thus, β-glucosidase can be coupled with a tumor-specific monoclonal antibody. β-Glucosidase can combine with cancer-cell-surface antigens and specifically convert amarogentin to an active drug that acts on cancer cells and the surrounding antibodies to achieve a killing effect. β-Glucosidase is injected intravenously and recognizes cancer-cell-surface antigens with the help of an antibody. The prodrug amarogentin is infused after β-glucosidase has reached the target position. Coupling of cell membrane peptides with β-glucosidase allows the enzyme to penetrate capillary endothelial cells and clear extracellular deep solid tumors to kill the cells therein. The Chinese medicine amarogentin and β-glucosidase will become an important treatment for various tumors when an appropriate monoclonal antibody is developed.


amarogentin β-glucosidase antibody enzymatic prodrug targeting therapy Chinese medicine 


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  1. 1.
    Schellmann N, Deckert P M, Bachran D, Fuchs H, Bachran C. Targeted enzyme prodrug therapies. Mini Rev Med Chem 2010;10:887–904.CrossRefPubMedGoogle Scholar
  2. 2.
    Shen YY, ed. Pharmacology of traditional Chinese medicine. Beijing: People’s Medical Publishing House; 2011:684–687.Google Scholar
  3. 3.
    Milazzo S, Ernst E, Lejeune S, Schmidt K. Laetrile treatment for cancer. Cochrane Database Syst Rev 2006:2:CD005476.Google Scholar
  4. 4.
    Cao ML. Research progress of cyanogentic glycosides in plant. Plant Physiol Commun 1992;29:68–72.Google Scholar
  5. 5.
    Wu XR, Liu JW. Cyanogenic compounds structure and distribution in plants. Plant Physiol Commun 1985;1:8–14.Google Scholar
  6. 6.
    Swain E, Poulton JE. Utilization of amygdalin during seedling development of prunus serotina. Plant Physiol 1994;106:437–445.CrossRefPubMedPubMedCentralGoogle Scholar
  7. 7.
    Chang HK, Shin MS, Yang HY, Lee JW, Kim YS, Lee MH, et al. Amygdalin induces apoptosis through regulation of Bax and Bcl-2 expressions in human DU145 and LNCaP prostate cancer cells. Biol Pharm Bull 2006;29:1597–1602.CrossRefPubMedGoogle Scholar
  8. 8.
    Shukla S, Bafna K, Sundar D, Thorat SS. The bitter barricading of prostaglandin biosynthesis pathway: understanding the molecular mechanism of selective cyclooxygenase-2 inhibition by amarogentin, a secoiridoid glycoside from Swertia chirayita. PLoS One 2014;9:90637.CrossRefGoogle Scholar
  9. 9.
    Xie Y, Shang XX, Cao LH. Studies on the liquid-state culture medium of ß-glucosidase from Aspergillus niger. J Nanchang Hangkong Univ (Social Sci, Chin) 2007;21:49–52.Google Scholar
  10. 10.
    Yang JH, Ren DM. Selection of high-yield ß-glucosidase strain and the optimized of solid state fermentation. J Anhui Agricult Sci (Chin) 2005;33:1566–1568.Google Scholar
  11. 11.
    Lian YJ, Chen DD, Huang T, Ke ML, Xu TW, Zheng YB, et al. In vitro cytotoxity on colorectal carcinoma LoVo cells of amygdalin following specific activation by ß-glucosidase and influence on expression of bcl-2, bax gene and caspase-3 activity. Chin J Cancer prev Treat 2005;12:413.Google Scholar
  12. 12.
    Xu NX. The research progress of amygdalin. Inner Mongolia Chin Med (Chin) 2012;31:66–67.Google Scholar
  13. 13.
    Xing GX, Li N, Yang JY, Cui LJ, Wang T. Research progress of natural amygdalin. Chin Tradit Patent Med (Chin) 2003;25:1007–1009.Google Scholar
  14. 14.
    Lian YJ, Chen DD, Huang T. Research progress of tumor antibody oriented enzyme prodrug. Med J Chin People Health (Chin) 2006;18:888.Google Scholar
  15. 15.
    Nie Z, Zhou J, Wang QH, Wang GW. Bladder cancer cells apoptosis induced by amygdalin following specific activation by ß-gIucosidase. J Mod Urol 2013;18:113–116.Google Scholar
  16. 16.
    Chen SM. New use of bitter almond. Chin J Modern Appl Pharm (Chin) 1991;8:44–45.Google Scholar
  17. 17.
    Mu J. Research development of Apricot seed sapomin. Inform Tradit Chin Med (Chin) 2002;19:19–21.Google Scholar
  18. 18.
    Wei JT, Liu WQ. Research on and application of amygdalin in prescription. J Hainan Med Coll (Chin) 2007;13:589–590.Google Scholar
  19. 19.
    Lian YJ, Xu TW, Zheng YB, Ke ML, Li Z, Huang T, et al. Therapeutic effect of anti-CEAMcAb-ß-glucosidase conjugate/amygdalin system on colorectal cancer xenografts in nude mice. Orthopaedics 2005;29:50.Google Scholar
  20. 20.
    Fonseca SB, Pemim MP, Kelley SD. Recent advances in the use of cell-penetrating pepties for medical and biological applications. Adv Drug Deliy Rev 2009;61:953–964.CrossRefGoogle Scholar
  21. 21.
    Zhang XJ, Liu YW, Wang J, Deng P, Jiang Y. Construction and inhibitory effect of TAT-p38(AF) on UV-induced activation of p38 MAPK pathway. Shangdong Med J (Chin) 2010;50:19–21.Google Scholar
  22. 22.
    Wang GW, Zhou J, Wang QH, Liu YL. Preparation and identification of CPPs-ß-glucosidase conjugates. Shandong Med J (Chin) 2013;53:1–4.Google Scholar
  23. 23.
    Syrigos KN, Rowlinson Busza G, Epenetos AA. In vitro cytotoxicity following specific activation of amygadalin by beta-glicosidase conjugated to a bladder cancer-associated monoclonalantibody. Int J Cancer 1998;78:721–719.CrossRefGoogle Scholar

Copyright information

© Chinese Association of the Integration of Traditional and Western Medicine 2015

Authors and Affiliations

  • Yun-long Li
    • 1
  • Qiao-xing Li
    • 1
  • Rui-jiang Liu
    • 2
  • Xiang-qian Shen
    • 2
  1. 1.Department of UrologyKunshan Hospital Affiliated to Jiangsu UniversityKunshan, Zhejiang ProvinceChina
  2. 2.School of Material Science and EngineeringJiangsu UniversityZhenjiang, Zhejiang ProvinceChina

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