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World Journal of Gastroenterology 2014年第10期20卷 2641-2652页

作者： Atsuki Yamamoto Tomokazu Itoh Reishi Nasu Ryuichi Nishida pharmaceutical research laboratories Sakai Chemical Industry Co. Ltd. Kawachinagano Osaka 586-0006 Japan KATAYAMA SEIYAKUSYO co. Ltd.Hirakata Osaka 573-1132 Japan kaigen pharma co. Ltd.Doshomachi Chuo-ku Osaka 541-0045 Japan

AIM: To investigate the effects of sodium alginate (AL-Na) on indomethacin-induced small intestinal lesions in rats.

关键词： Sodium alginate Non-steroidal anti-inflammatory drugs Gastrointestinal muco.al injury Mucin Bacterial translocation

A practical synthesis of (-)fosfomycin from its enantiomer

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Chinese Chemical Letters 2008年第11期19卷 1297-1300页

作者： Meng Zhang Zheng Yu Ji Jun Li Da Li Yin Beijing co.lab pharma co. Ltd. Beijing 102600 China Institute of Materia Medica Peking Union Medical College Beijing 100050 China

（＋）-cis-（1S, 2R）-Epoxypropylphosphonic acid, the enantiomer of fosfomycin, which is the industrial side-product in the preparation of the antibiotic fosfomycin, was co.verted into （-）fosfomycin by a seven-step procedure. The esterification of the dihydroxyphosphonic intermediate was the key step. The title co.pound was obtained in good yield and its optical purity was up to the medicine quality standard of Chinese pharmaco.oeia.

关键词： Fosfomycin Enantiomer Phosphonate

Synthesis, Antibacterial Activities and Theoretical Studies of Benzopyranoco.marin Derivatives

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Chinese Journal of Structural Chemistry 2015年第10期34卷 1606-1611页

作者：鲁光英方军 Boch pharma.Technology (Shanghai) co.Ltd

Three benzopyranoco.marins（OBH, OMH and ODH） were synthesized and characterized via IR, ^1H NMR and HRMS. The HB energy in OBH, OMH and ODH was performed with the density functional theory（DFT） [B3LYP/6-31G＊] method. The in vitro antibacterial activity of OBH, OMH and ODH against drug-sensitive S. aureus（S. aureus ATCC 29213） strain, MRSA strain（MRSA XJ 75302）, drug-sensitive S. epidermidis strain（S. epidermidis ATCC 14990） and methicillin-resistant S. epidermidis strain（MRSE XJ 75284） was evaluated by observing the minimum inhibitory co.centration. The results showed that among the three co.pounds, ODH exhibited the most potent antibacterial activity.

关键词： benzopyranoco.marin density functional theory Staphyloco.cus aureus minimum inhibitory co.centration

Rat embryonic stem cells create new era in development of genetically manipulated rat models

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World Journal of Stem Cells 2015年第7期7卷 1054-1063页

作者： Kazushi Kawaharada Masaki Kawamata Takahiro Ochiya Research and Development Division DS Pharma Biomedical Co. Ltd. Division of Molecular and Cellular Medicine National Cancer Center Research Institute

Embryonic stem(ES) cells are isolated from theinner cell mass of a blastocyst, and are used for the generation of gene-modified animals. In mice, the transplantation of gene-modified ES cells into recipient blastocysts leads to the creation of gene-targeted mice such as knock-in and knock-out mice; these gene-targeted mice co.tribute greatly to scientific development. Although the rat is co.sidered a useful laboratory animal alongside the mouse, fewer genemodified rats have been produced due to the lack of robust establishment methods for rat ES cells. A new method for establishing rat ES cells using signaling inhibitors was reported in 2008. By co.sidering the characteristics of rat ES cells, recent research has made progress in improving co.ditions for the stable culture of rat ES cells in order to generate gene-modified rats efficiently. In this review, we summarize several advanced methods to maintain rat ES cells and generate gene-targeted rats.

关键词： Embryonic stem cells Transgenic rat

Analysis of co.dyceps by multi-co.umn liquid chromatography

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Acta pharmaceutica Sinica B 2017年第2期7卷 202-207页

作者： Zhengming Qian Shaoping Li Institute of Chinese Medical Sciences University of MacaoMacaoChina Key Laboratory of State Administration of Traditional Chinese Medicine Sunshine Lake Pharma Co.Ltd.Dongguan 523850China

co.dyceps is a famous traditional Chinese medicine (TCM) that has been used in China for hundreds of years. In the present study a multi-co.umn liquid chromatography (MC-LC) system was developed for the qualitative analysis of macromolecules and micromolecules in co.dyceps. The MC-LC system includes a size exclusion pre-co.umn, a size exclusion co.umn (SEC) and a reversed phase co.umn (RP) which were co.trolled by co.umn-switching valves. The sample was separated by the size exclusion pre-co.umn into two fractions (macromolecules and micromolecules). These fractions were further separated on SEC and RP co.umns, respectively. A diode array detector (DAD) and a mass spectrometer (MS) were used to detect the co.ponents. This MC-LC method was utilized for analysis of co.dyceps samples. Two macromolecular peaks and 15 micromolecular peaks were found in co.dyceps, and 11 of the micromolecular peaks were identified as adenosine-5'-monophosphate (AMP), phenylalanine, uridine, hypoxanthine, inosine, guanine, guanosine, deoxyadenosine-5'-monophosphate (dAMP), adenosine, adenine and co.dycepin (or its isomer). This method is useful for quality co.trol of co.dyceps. (C) 2017 Chinese pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

关键词： co.dycepie Macromocules Micromolecules Multi-co.umn Size exclusion co.umn

An update on electrostatic powder co.ting for pharmaceuticals

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Particuology 2017年第2期15卷 1-7页

作者： Qingliang Yang Yingliang Ma Jesse Zhu Kwok Chow Kaiqi Shi Particle Technology Research Centre Department of Chemical and Biochemical Engineering University of Western Ontario London Ontario N6A 589 Canada Powder pharma co.tings Mississauga Ontario LSR 2Y9 Canada Ningbo Weston Powder pharma co.tings co. Ltd. Ningbo Zhejiang 315042 China

Derived from dry powder co.ting of metals, electrostatic powder co.ting for pharmaceuticals is a technology for co.ting drug solid dosage forms. In this technology, co.ting powders, co.taining co.ting polymers, pigments, and other excipients, are directly sprayed onto the surface of the solid dosage forms through an electrostatic gun without using any organic solvent or water. The deposited co.ting powders are further cured to form a co.ting film. Electrostatic powder co.ting technology has many advantages co.pared to other pharmaceutical co.ting methods. It can eliminate the limitations caused by the organic solvent in solvent co.ting such as environmental issues and health problems. And electrostatic powder co.ting technology also surpasses aqueous co.ting due to its shorter processing time and less energy co.sumption, leading to a lower overall co.t. Furthermore, the utilization of electrical attraction can promote the movement of co.ting powders towards the substrate, leading to an enhanced co.ting powder adhesion and co.ting efficiency, which make it more promising co.pared to other dry co.ting technologies. The objective of this review is to summarize the co.ting principles, apparatus, and formulations of different electrostatic powder co.ting technologies, giving their advantages and limitations and also analyzing the future application in the industry for each technology

关键词： Electrostatic powder co.ting Solid dosage forms Plasticizers Powder adhesion Film formation Curing

Polyphenol-Rich Olive Mill Wastewater Extract and Its Potential Use in Hair Care Products

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Journal of co.metics, Dermatological Sciences and Applications 2021年第4期11卷 356-370页

作者： Lisa-Marie Sittek Thomas M. Schmidts Peggy Schlupp RSC pharma GmbH & co. KG Giessen Germany

In this work, the influence of phenol-enriched olive mill wastewater (OMWW) extract on hair growth was investigated in vitro on human follicle dermal papilla cells. OMWW has already shown great potential for use in skincare products, and its high polyphenol co.tent is predestined to have a positive effect on hair growth. The studies included caffeine, a positive modulator of hair growth, and dihydrotestosterone, which causes hair loss in vivo, as co.trols. The impact of the investigated co.pounds on hair growth was evaluated by studies on cell viability and proliferation, the release of growth factors (insulin-like growth factor-1 and vascular endothelial growth factor), and the reduction of reactive oxygen species formation. OMWW showed a positive influence on the proliferation of the human follicle dermal papilla cells. Moreover, the extract leads to a significantly increased secretion of insulin-like growth factor-1, and a co.siderable reduction in reactive oxygen species formation was observed. Overall, our results show that the investigated phenol-enriched OMWW extract is a promising ingredient for hair care to improve hair growth, prevent hair loss due to oxidative stress and maintain a healthy scalp.

关键词： Hair Growth Hair Loss Human Follicle Dermal Papilla Cells Caffeine Dihydrotestosterone IGF-1 VEGF Reactive Oxygen Species

Syntheses and Crystal Structures of 3,3'-(9,10-Anthrylene)bis-pentane-2,4-dione and 3-(2-Methoxy-1-naphthalenyl)-pentane-2,4-dione

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Chinese Journal of Structural Chemistry 2001年第6期20卷 439-443页

作者：席简忠张静等 Techpool Biochem. pharma. co. 广东广州 510520 南京大学江苏南京 210093 中科院成都有机化学所四川成都 610041

Two co.pounds 3,3'-(9,10-anthrylene)bis-pentane-2,4-dione 1 and 3-(2-methoxy-1-naphthalenyl)-pentane-2,4-dione 2 were synthesized by the direct arylation of pentane-2,4-diones in the presence of Mn(OAc)3 and H3PO4. Their crystal structures were determined by X-ray diffraction method. co.pound 1, C24H22O4, Mr = 374.4, crystallized in the monoclinic system, space group P21/a with a = 7.393(4), b = 14.308(5), c = 10.099(5) ? = 110.8(4)? V = 999.0 (9) 3, Z = 2, Dc = 2.49g/cm3, F(000) = 392, ?= 0.78cm-1, final R = 0.050 and Rw = 0.057 for 1144 observed reflections with I≥3.00 ?(I). The molecular backbone is the anthracene ring, and two acetoacetone groups are perpendicular to the anthracene ring at 9,10 positions. co.pound 2, C16H16O3, Mr = 256.3, crystallized in monoclinic system, space group C2 with a = 14.369(3), b = 7.480 (1), c = 15.878 (2) ? = 128.46(1)? V = 1336.3(4) ?, Z = 4, Dc = 1.27g/cm3, F(000) = 544, ?= 0.81cm-1. The structure was solved by direct methods and refined by full-matrix least-squares method, final R = 0.044 and Rw = 0.040 for 764 observed reflections with I ≥3.00(I). The acetoacetone group in co.pound 2 is also vertical to the naphthalene ring.

关键词： crystal structure pentane-2,4-dione

Determination and stress studies on YK-1101,a potential histone deacetylase,by HPLC-UV and HPLC-TOF/MS methods

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Journal of pharmaceutical Analysis 2013年第3期3卷 168-172页

作者： Chen Zhou Wen-Yuan Liu Feng Feng Hai Ye Chun-Yong W Department of pharmaceutical Analysis China Pharmaceutical University Department of Natural Medicine Chemistry China Pharmaceutical University Yoko pharma co. Ltd.

YK- 1101, with its structure as S-（（E）-4-（（7S, 10S,Z）-4-ethylidene-7-isopropyl-2,5,8,12- tetraoxo -9-oxa- 16-thia-3,6,13,18-tetraazabicyclo[ 13.2.1 ]octadeca- 1 （17）, 15（ 18）-dien- 10-yl）but-3-en- 1 -y l） ethanethioate, is synthesized as a potential histone deacetylase inhibitor. Its quality and stability under various stress co.ditions are not fully understood. In this study, a high performance liquid chromatographic （HPLC） method was established and validated for the analysis of YK-1101 bulk drug samples. The chromatographic separation was performed on a C18 co.umn with acetonitrile and water as mobile phase in a gradient elution. Based on the established method, the stability studies of YK-1101 under various stress co.ditions were carried out. YK-1101 was shown to undergo degradation under basic and acidic stress co.ditions, while it was stable under oxidative, photolytic and thermal co.ditions. In addition~ a time of flight mass spectrometer （TOF/MS） was co.pled to HPLC for the characterization of major degradation products produced under basic and acidic stress co.ditions. Their degradation pathways were also discussed.

关键词： YK-1101 Degradation products Stress study Liquid chromatography Time of flight massspectrometer

Artificial Bear Bile:A Novel Approach to Balancing Medical Requirements and Animal Welfare

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Engineering 2024年第7期38卷 100-112页

作者： Yong Li Yuhong Huang Nan Feng Heping Zhang Jing Qu Shuanggang Ma Yunbao Liu Jiang Li Shaofeng Xu Ling Wang Mi Zhang Jie Cai Weiping Wang Ru Feng Hang Yu Bo Yu Dailiang Liang Heping Qin Suxiang Luo Yanfen Li Meifeng Li Ruihua Wang Chen Ma Yan Wang Xiaobo Cen Xiaoxian Xu Boli Zhang Xiaoliang Wang Shishan Yu State Key Laboratory of Bioactive Substance and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China The Seco.d Affiliated Hospital of Tianjin University of Traditional Chinese Medicine Tianjin 300250China Zhongshan Belling Biotechnology co. Ltd.Zhongshan 528437China Zhongshan Anshi Biopharmaceutical co. Ltd.Zhongshan 528437China WestChina-Frontier pharma Tech co. Ltd.Chengdu 610041China Tianjin University of Traditional Chinese Medicine Tianjin 301617China

Bear bile has been a valuable and effective medicinal material in traditional Chinese medicine(TCM)for over 13 ***,the current practice of obtaining it through bear farming is under scrutiny for its adverse impact on bear ***,we present a new approach for creating artificial bear bile(ABB)as a high-quality and sustainable alternative to natural bear *** study addresses the scientific challenges of creating bear bile alternatives through interdisciplinary co.laborations across various fields,including resources,chemistry,biology,medicine,pharmaco.ogy,and TCM.A co.prehensive efficacy assessment system that bridges the gap between TCM and modern medical terminology has been established,allowing for the systematic screening of therapeutic *** the utilization of chemical synthesis and enzyme engineering technologies,our research has achieved the environmentally friendly,large-scale production of bear bile therapeutic co.pounds,as well as the optimization and reco.position of ABB *** resulting ABB not only closely resembles natural bear bile in its co.position but also offers advantages such as co.sistent product quality,availability of raw materials,and independence from threatened or wild *** preclinical efficacy evaluations have demonstrated the equivalence of the therapeutic effects from ABB and those from co.mercially available drained bear bile(DBB).Furthermore,preclinical toxico.ogical assessment and phase I clinical trials show that the safety of ABB is on par with that of the currently used *** innovative strategy can serve as a new research paradigm for developing alternatives for other endangered TCMs,thereby strengthening the integrity and sustainability of TCM.

关键词： Artificial bear bile Chemical profile Formula optimization pharmaco.ynamic co.sistency Preclinical toxico.ogical assessment