Please wait a minute...
Frontiers of Chemical Science and Engineering

ISSN 2095-0179

ISSN 2095-0187(Online)

CN 11-5981/TQ

邮发代号 80-969

2019 Impact Factor: 3.552

Frontiers of Chemical Science and Engineering  2014, Vol. 8 Issue (3): 362-368   https://doi.org/10.1007/s11705-014-1439-5
  本期目录
Development of a multi-component drug from turmeric using central composite design
Xiaohang ZHANG,Shengnan HAN,Yan LI,Jianlan JIANG()
Key Laboratory of Systems Bioengineering, Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China
 全文: PDF(865 KB)   HTML
Abstract

A methodology to develop multi-component drugs based on traditional Chinese medicines has been developed using central composite design. Several active components from the traditional Chinese medicine turmeric were chosen for use in a multi-component antitumor drug. Response surface methodology based on a central composite design was applied to determine the quantitative composition-activity relationships in order to optimize the amount of each component in the drug. An MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay was used to measure the pharmacological activity as the response value. The experimental antitumor activity of the optimum combination was 92.85% in the MTT assay and superior to the activities of each single component. These results demonstrate that response surface methodology based on a central composite design is suitable for the design of multi-component drugs.

Key wordsmulti-component drug development    central composite design    turmeric    curcuminoids
收稿日期: 2013-12-22      出版日期: 2014-10-11
Corresponding Author(s): Jianlan JIANG   
 引用本文:   
. [J]. Frontiers of Chemical Science and Engineering, 2014, 8(3): 362-368.
Xiaohang ZHANG,Shengnan HAN,Yan LI,Jianlan JIANG. Development of a multi-component drug from turmeric using central composite design. Front. Chem. Sci. Eng., 2014, 8(3): 362-368.
 链接本文:  
https://academic.hep.com.cn/fcse/CN/10.1007/s11705-014-1439-5
https://academic.hep.com.cn/fcse/CN/Y2014/V8/I3/362
Variable parametersVariable levels
-10+1
A Curcumin05.714.022.328.0
B Demethoxycurcumin02.56.310.012.5
C Bisdemethoxycurcumin02.86.810.813.6
Tab.1  
No.ABCInhibition ratio /%
122.352.5410.8385.29?±?4.81
25.689.972.7591.27?±?8.84
314.016.256.7987.15?±?8.28
414.016.2513.5879.43?±?5.56
55.689.9710.8378.95?±?13.04
614.016.256.7989.93?±?7.54
722.359.9710.8389.21?±?7.98
814.010.006.7977.50?±?4.69
914.016.256.7990.69?±?7.16
1022.352.542.7581.76?±?4.58
1114.0112.516.7992.31?±?5.71
1222.359.972.7592.77?±?6.50
130.006.256.7982.63?±?8.15
145.682.542.7587.61?±?4.41
1514.016.250.0079.76?±?6.98
1628.036.256.7992.23?±?6.32
1714.016.256.7990.45?±?0.61
185.682.5410.8382.43?±?3.07
1914.016.256.7988.83?±?8.02
2014.016.256.7987.12?±?5.20
Tab.2  
SourceSum of squaresDegree of freedomMean squareF-valueP-value
Model398.57944.295.660.0061
A14.79114.791.890.1992
B22.69122.692.900.1194
C35.36135.364.520.0594
AB27.13127.133.470.0922
AC38.16138.164.880.0517
BC25.29125.293.230.1024
A20.02310.0232.916E-0030.9580
B212.52112.521.600.2345
C2113.701113.7014.530.0034
Residual78.24107.82
Lack of Fit65.47513.095.130.0486
Pure Error12.7752.55
Total476.8119
Tab.3  
Fig.1  
Fig.2  
Fig.3  
Fig.4  
1 Wang Y, Fan X, Qu H, Gao X, Cheng Y Y. Strategies and techniques for multi-component drug design from medicinal herbs and traditional Chinese medicine. Current Topics in Medicinal Chemistry, 2012, 129(12): 1356–1362
2 Ruffolo R R. Why has R&D productivity declined in the pharmaceutical industry? Expert Opinion Drug Discovery, 2006, 1(2): 99–102
3 Hiroaki K. A robustness-based approach to systems-oriented drug design. Nature Reviews. Drug Discovery, 2007, 6(3): 202–210
4 Keith C T, Borisy A A, Stockwell B R. Multicomponent therapeutics for networked systems. Nature Reviews. Drug Discovery, 2005, 4(1): 71–78
5 Ke L, Wei J. An integrated metabolomics and pharmacokinetics strategy for multi-component drugs evaluation. Current Drug Metabolism, 2010, 11(1): 105–114
6 Tian X Y, Liu L. Drug discovery enters a new era with multi-target intervention strategy. Chinese Journal of Integrative Medicine, 2012, 18(7): 539–542
7 Li J, Lu C, Jiang M, Niu X Y, Guo H T, Li L, Bian Z X, Lin N, Lu A P. Traditional Chinese medicine-based network pharmacology could lead to new multicompound drug discovery. Evidence-Based Complementary and Alternative Medicine, 2012, 149762:1–149762:11
8 Borisy A A, Elliott P J, Hurst N W, Lee M S, Lehar J, Price E R, Serbedzija G, Zimmermann G R, Foley M A, Stockwell B R, Keith C T. Systematic discovery of multicomponent therapeutics. Proceedings of the National Academy of Sciences of the United States of America, 2003, 100(13): 7977–7982
9 Kvalheim O M, Chan H, Benzie I F F, Szeto Y T, Tzang A H C, Mok D K W, Chau F T. Chromatographic profiling and multivariate analysis for screening and quantifying the contributions from individual components to the bioactive signature in natural products. Chemometrics and Intelligent Laboratory Systems, 2011, 107(1): 98–105
10 Roldan C, Torre A, Mota S, Morales S A, Menendez J, Segura Carretero A. Identification of active compounds in vegetal extracts based on correlation between activity and HPLC-MS data. Food Chemistry, 2013, 136(2): 392–399
11 Süntar I, Küpeli Akkol E, Keles H, Yesilada E, Sarker S D, Arroo R, Baykal T. Efficacy of Daphne oleoides subsp. kurdica used for wound healing: Identification of active compounds through bioassay guided isolation techniqueSarker S D. Journal of Ethnopharmacology, 2012, 141(3): 1058–1070
12 Jiang J L, Jin X L, Zhang H, Su X, Qiao B, Yuan Y J. Identification of antitumor constituents in curcuminoids from Curcuma longa L. based on the composition-activity relationship. Journal of Pharmaceutical and Biomedical Analysis, 2012, 70: 664–670
13 Jiang J L, Su X, Zhang H, Zhang X H, Yuan Y J. A novel approach to active compounds identification based on support vector regression model and mean impact value. Chemical Biology & Drug Design, 2013, 81(5): 650–657
14 Jiang J L, Zhang H, Zhou P P, Han S N, Han Y D, Yuan Y J. Composition-activity relationship modeling to predict the antitumor activity for quality control of curcuminoids from Curcuma longa L. (turmeric). Analytical Methods, 2013, 5(3): 641–647
15 Goel A, Aggarwal B B. Curcumin, the golden spice from Indian saffron, is a chemosensitizer and radiosensitizer for tumors and chemoprotector and radioprotector for normal organs. Nutrition and Cancer, 2010, 62(7): 919–930
16 Shehzad A, Wahid F, Lee Y S. Curcumin in cancer chemoprevention: Molecular targets, pharmacokinetics, bioavailability, and clinical trials. Archivder Pharmazie Chemistry in Life Sciences, 2010, 343(9): 489–499
17 Zhang L J, Wu C F, Meng X L, Yuan D, Cai X D, Wang Q L, Yang J Y. Comparison of inhibitory potency of three different curcuminoid pigments on nitric oxide and tumor necrosis factor production of rat primary microglia induced by lipopolysaccharide. Neuroscience Letters, 2008, 447(1): 48–53
18 Luthra P M, Kumar R, Prakash A. Demethoxycurcumin induces Bcl-2 mediated G2/M arrest and apoptosis in human glioma U87 cells. Biochemical and Biophysical Research Communications, 2009, 384(4): 420–425
19 Yodkeeree S, Chaiwangyen W, Garbisa S, Limtrakul P. Curcumin, demethoxycurcumin and bisdemethoxycurcumin differentially inhibit cancer cell invasion through the down-regulation of MMPs and uPA. Journal of Nutritional Biochemistry, 2009, 20(2): 87–95
Viewed
Full text


Abstract

Cited

  Shared   
  Discussed