1.Synthesis of some derivatives with biological properties of 2-amino-4,6-dimethyl-pirimidine
Pharmaceutical Journal 2003;327(7):15-16
The 2- hydroxy-4,6-dimethyl pyrimidine (8),2-amino-4,6 –dimethyl pyrimidine (10) and sulfamet-hazine(1)were prepared by condensation of urea (4), guanidine (5) or sulfaguanidine (6) with acetylacetone(7) and then the 2-chloro-4,6-dimethyl pyrimidine (9) was obtained by treating the compound (8) with phosphorylchoride (POCl3)
Biological Products
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chemistry
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pharmacy
2.Combining microbial and chemical syntheses for the production of complex natural products.
Chinese Journal of Natural Medicines (English Ed.) 2022;20(10):729-736
Nature, a rich source of bioactive natural products, serves as a massive pool of drug candidates for the pharmaceutical industry. However, the supply of these structurally complex chemicals is costly as most of the natural products are scarce in nature, thus requiring de novo synthesis. The supply chain issue hinders the development of novel therapeutic agents from natural products. Microbial synthesis, based on the expression of biosynthetic genes in a suitable microbial host to produce certain chemicals, is a sustainable strategy to produce complex natural products. However, this strategy requires gaining insights into the biosynthesis of target molecules. Most natural products are biosynthetically unknown or not fully elucidated; thus, the sole application of microbial synthesis strategy to produce a given molecule is challenging. In this review, we highlight a strategy that combines microbial and chemical syntheses to tackle the supply chain issue in developing drugs from natural products. We believe this strategy can revive the drug development pipeline for natural products.
Biological Products/chemistry*
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Aminoglycosides
3.Chemical composition of oral cholera vaccine 2001-2002
Journal of Practical Medicine 2003;450(4):55-57
19 lots of oral vaccine producted in the years 2001-2002 at the Company No1 of Vaccines and Biological Preparations were studied. pH=6.9 in the lot 110102, the highest was 7.3 in the lots 050901, 060901 and 091201 (permissible pH=6.8-7.4); thimerosant content from 0.005 g% in the lot 020801 to 0.015 g% in the lots 110102, 120302 and 150502 (permissible content ≤ 0.02 g%); formaldehyde content from 0.005 g% in the lot 060901 to 0.017 g% in the lot 110102 (permissible content ≤ 0.02 g%); total protein content 0.77 g% in the lot 091201 and 1.63 g% in the lot 181002 (permissible content ≤ 2 g%)
Cholera Vaccines
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chemistry
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Biological Products
4.Chemical composition of oral cholera vaccine 2001-2002
Journal of Practical Medicine 2003;450(4):57-59
At Cho Ray Hospital – Ho Chi Minh city from Dec 2001 to Dec 2002, 228 heart failure cases (96 males, 130 females, aged 58.4317.45) were studied. Their associated conditions were: 14 with diabetes, 5 brain blood infactus, 5 hyperthyroidies, 19 kidney failures. Among 162 patients with electrolyte disorders, 25 were died, the rate of hyponatremia and hyperkalemia was significantly higher in fatal group than in survival group. Hyponatremia was fatal risk factor and it should pay great attention to treat this condition with hypertonic natrium solution
Cholera Vaccines
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chemistry
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Biological Products
5.The efficiency of oral cholera vaccine produced industrial scale
Journal of Practical Medicine 2003;450(4):59-60
Oral cholera vaccine efficiency was studied with the strains of V. cholerae 01, Cairo 50, V. cholerae 01.569B, V. cholerae 01 Phil 6973, El Tor, as antigene. According to the standards issued by the National Centre of Control of Medical Biopreparation, the samples of vaccine producted at industrial scale in the Company No1 of Vaccines and Biological Preparation belong the National Institute of Hygiene and Epidemiology was satisfied
Cholera Vaccines
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chemistry
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Biological Products
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6.Chemical and pharmacological progress on usnic acid and its derivatives.
Sha-Na WUKEN ; Shun-Gang JIAO ; Xin-Yao YANG ; Xiao-Li GAO ; Chang-Hai QU ; Qian ZHANG ; Chun-Sheng LIU ; Peng-Fei TU ; Xing-Yun CHAI
China Journal of Chinese Materia Medica 2018;43(19):3811-3821
Usnic acid and its derivatives, a group of organic molecules with great importance, are characteristic to lichens, possessing pharmacological activities such as anti-virus, anti-bacteria, anti-humor, anti-inflammatory, analgesic, and anaesthetic effects. Many of them have been widely used as medicine, but also bring side effects such as dermatitis and liver damages. In the past decades, great efforts by isolation, organic synthesis, and structure modification methods were put on discovery of UA derivatives with higher biological activities or less side effects. This paper describes herein the most progress on natural sources, isolation and structure elucidation, structural characteristics, synthesis and modification results, pharmacological activities and toxicities of UA and its derivatives, hopefully to provide valuable reference for further research.
Benzofurans
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chemistry
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pharmacology
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Biological Products
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Lichens
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chemistry
7.Research progress on application of multi-enzyme-catalyzed cascade reactions in enzymatic synthesis of natural products.
Wen-Qian HUANG ; Ying-Xia WANG ; Wei-Sheng TIAN ; Juan WANG ; Peng-Fei TU ; Xiao-Hui WANG ; She-Po SHI ; Xiao LIU
China Journal of Chinese Materia Medica 2023;48(2):336-348
As a biocatalyst, enzyme has the advantages of high catalytic efficiency, strong reaction selectivity, specific target products, mild reaction conditions, and environmental friendliness, and serves as an important tool for the synthesis of complex organic molecules. With the continuous development of gene sequencing technology, molecular biology, genetic manipulation, and other technologies, the diversity of enzymes increases steadily and the reactions that can be catalyzed are also gradually diversified. In the process of enzyme-catalyzed synthesis, the majority of common enzymatic reactions can be achieved by single enzyme catalysis, while many complex reactions often require the participation of two or more enzymes. Therefore, the combination of multiple enzymes together to construct the multi-enzyme cascade reactions has become a research hotspot in the field of biochemistry. Nowadays, the biosynthetic pathways of more natural products with complex structures have been clarified, and secondary metabolic enzymes with novel catalytic activities have been identified, discovered, and combined in enzymatic synthesis of natural/unnatural molecules with diverse structures. This study summarized a series of examples of multi-enzyme-catalyzed cascades and highlighted the application of cascade catalysis methods in the synthesis of carbohydrates, nucleosides, flavonoids, terpenes, alkaloids, and chiral molecules. Furthermore, the existing problems and solutions of multi-enzyme-catalyzed cascade method were discussed, and the future development direction was prospected.
Biological Products/chemistry*
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Catalysis
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Alkaloids
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Biocatalysis
8.Advances in studies on chemical constituents, pharmacological effects and clinical application of Aspongopus chinensis.
Sha LI ; Lei LI ; Hong-Bing PENG ; Xiao-Jing MA ; Lu-Qi HUANG ; Juan LI
China Journal of Chinese Materia Medica 2020;45(2):303-311
The Aspongopus chinensis is an insect of the genus Hemiptera, which can be used both as a medicinal and as a gourmet in the folk. It has a long history as a drug, which has the effect of regulating Qi and relieving pain, and warming the Yang. It is mainly used to treat stomach cold and pain, liver and stomach pain, kidney deficiency and impotence, and waist and knee pain. Modern pharmacological studies have shown that A. chinensis has a variety of pharmacological activities. For example, it can be used to fight tumors, improve reproductive damage, and antibacterial, anti-oxidation, anti-coagulation, anti-ulcer, anti-fatigue and so on. The chemical constituents of A. chinensis currently reported mainly include odorous components, vitamins, fatty acids and proteins, amino acids, and other nutrients, as well as nucleosides and dopamines. This study summarizes and analyzes the related research literatures of A. chinensis in China and abroad, and provides a reference for its further development and research from the aspects of chemical composition, pharmacological action and clinical application.
Animals
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Biological Products/chemistry*
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China
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Heteroptera/chemistry*
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Medicine, Chinese Traditional
9.Trace phenolic compounds from Red Yeast Rice.
Yu-Bin JI ; Fei XU ; Bing-Yu LIU ; Qian WEI ; Yong-Zhi GUO ; Yu DONG ; Ying SUN ; You-Cai HU
China Journal of Chinese Materia Medica 2018;43(4):755-759
Trace chemical constituents from the ethyl acetate extract of Red Yeast Rice were investigated. Four phenolic compounds were isolated by various column chromatographies, and their structures were identified on the basis of spectroscopic analysis including UV, MS, IR and NMR. The four compounds were identified as 2-methyl-5-(2'R-methyl-4'-hydroxy-butyl)-cinnamic acid(1), 5-(2'-hydroxy-6'-methyl phenyl)-3-methylfuran-2-carboxylic acid(2), daidzein(3), and genistein(4). Compound 1 was new and 2 was firstly discovered from the genus Monascus, while 3-4 were obtained from Red Yeast Rice for the first time.
Biological Products
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chemistry
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Magnetic Resonance Spectroscopy
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Monascus
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Phenols
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chemistry
10.Natural products chemistry research 2010's progress in China.
Yang YE ; Xi-Qiang LI ; Chun-Ping TANG ; Sheng YAO
Chinese Journal of Natural Medicines (English Ed.) 2012;10(1):1-13
This article reviews the progresses made by Chinese scientists in the field of natural products chemistry in 2010. Selected compounds with unique structural features and/or promising bioactivities were described herein on the basis of structural types.
Biological Products
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chemistry
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pharmacology
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China
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Humans
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Molecular Structure
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Research