| Objective: The production of L-dopa through chemical synthesis has been declining due to the cost, environmental pollution control and other reasons in foreign country. The supply of natural L-dopa in foreign country is mainly imported from China. We can see that the potential market of producing natural L-dopa from Maodou is very great. In order to set up supporting technologies for the development of industry of Maodou in Guangxi, we have done a series of investigation in Maodou.Methods:In order to set up supporting technologies for the development of industry of Maodou in Guangxi, we have done a series of investigation in Maodou. These investigations focused on application of Maodou, technology of Maodou planting, extraction of L-dopa from Maodou, mucunaguanide in Maodou, non-levodopa components in Maodou, L-dopa derivatives, recycle of extraction waste of Maodou and so on.Results: In this paper, we have developed a series of technology in high-yield planting of Maodou, efficient extraction of high purity of levodopa and wet-preservation of extraction waste of Maodou. We have synthesized, isolated and purified 17 new L-dopa derivatives. These are levodopa methyl ester hydrochloride,(3,4-dihydroxy-L-phenylalanine ethyl ester),((S)-propyl 2-amino-3-(3,4-dihydroxyphenyl) propanoate),((S)-isopropyl 2-amino-3-(3,4-dihydroxyphenyl)propanoate),((S)-butyl -2-amino-3-(3,4- dihydroxyphenyl)propanoate hydrochloride),((S)-iso -butyl 2-amino-3-(3,4-dihydroxyphenyl) propanoate hydrochloride),((S)- pentyl 2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride),((S) -isopentyl-2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride),((S)-hexyl 2-amino-3-(3,4-dihydroxyphenyl)propanoate hydrochloride),((S)-4-(2-acetamido-3-methoxy-3-oxopropyl)-1,2-phenylene diacetate), ((S)-4-(2-acetamido-3-ethoxy-3-oxopropyl)-1,2-phenylene diacetate),((S)-4-(2-acetamido-3-oxy-3-propoxypropyl)-1, 2-phenylene diacetate),((S)-4-(2-acetamido-3-isopropoxy-3-oxopropyl)-1,2-phenylene diaceta -te),((S)-4-(2-acetami-do-3-butoxy-3-oxopropyl)-1, 2-phenylene diaceta -te),((S)-4-(2-acetamido-3-isobutoxy-3-oxopropyl)-1, 2-phenylene diacet -ate),((S)-4-(2-acetamido-3-oxo-3-(pentyloxy) propyl)-1, 2-phenylene diacetate) and ((S)-2-((tert-butoxycarbonyl)amino)-3-(3,4-dihydroxyph -enyl) propanoic acid) Charaterization and functional detection of all derivatives have been done. We found one derivative, levodopa methyl ester hydrochloride was useful in treatment of amblyopia. Translational research of Levodopa methyl ester hydrochloride is under going. This expands the use of levodopa, and enhance the profitability of industrial chain of Maodou. These technologies have been used in Guangxi Napo Pharma Co., Ltd.. We have founded a new company, Guangxi Sedopa Co., Ltd. on the base of Guangxi Banger Pharma Co., Ltd. with the strategy investment of 50 million yuan. We are applying certificate of cGMP. Our goal is to become the largest manufacturer of levodopa in the world.Conclusions: The supporting technologies for the development of industry of Maodou in Guangxi expands the use of levodopa, and enhance the profitability of industrial chain of Maodou. |