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高等学校化学学报 2016年第11期37卷 1993-1998,2143-2151页

作者：胡栋宝周北斗玉溪师范学院资源环境学院玉溪653100 莆田学院药学与医学技术学院莆田351100

在研究天然产物绝对构型的过程中,筛选了一些绝对构型未确定的生物碱类化合物,利用密度泛函理论(DFT)在不同的计算水平下得出其旋光和碳氢谱数据.理论值与实测值对比分析结果表明,二者基本符合,从而鉴定出这些化合物的绝对构型.

关键词：天然产物生物碱密度泛函理论(DFT) 旋光绝对构型

Biological investigation of phenyl benzoate, benzophenone, and xanthone compounds

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Journal of Chinese Pharmaceutical Sciences 2022年第10期31卷 738-745页

作者： beidou zhou Chun Lei Xuemei Liao Hang Zhu Zhipeng Ruan Yuanyuan Fang Guifen Xu Yuli Chen School of Pharmacy and Medical Technology Putian UniversityKey Laboratory of Pharmaceutical Analysis and Laboratory Medicine(Putian University)Fujian Provincial UniversityPutian 351100China School of Pharmacy FujianMedical UniversityFuzhou350108China Fujian Tianquan Pharmaceutical Co. Ltd.Longyan 364000China

In the present study, we evaluated the antitumor, anti-tyrosinase, anti-pancreatic lipase, antibacterial, antifungal, and anti-α-glycosidase activities for all or a subset of 20 known compounds. They included 8 phenyl benzoates, 10 benzophenones, and 2 xanthones. Phenyl benzoate compounds 1–8 did not exhibit evident antitumor activity, which was consistent with existing theories. Compounds 16, 17, and 18 exhibited moderate anti-tyrosinase activity. In addition, compounds 11 and 18 exhibited moderate inhibitory activity against Candida albicans, and compound 20 exhibited stronger anti-α-glycosidase activity than quercetin, with an IC_(50)of approximately 2.45 μM. These results demonstrated that compounds 11, 16–18, and 20 were promising leads for further structural modification.

关键词： Phenyl benzoate Benzophenone Xanthone Antibacterial Antifungal α-Glycosidase

Investigation on Chemical Components of Higher Fungus Phellinus rhabarbarinus(Berk.) G. Cunn.

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Agricultural Science & Technology 2016年第9期17卷 1990-1992页

作者：胡栋宝周北斗玉溪师范学院资源环境学院云南玉溪653100 莆田学院药学与医学技术学院福建莆田351100

Five compounds including 2 benzene derivatives, 2 terpenoids and 1 sterol were separated by various separation methods such as positive silica gel, Sephadex LH-20 and Rp-18 gel from higher fungi Phellinus rhabarbarinus （Berk.） G. Cunn. Their structures were elucidated on the basis of nuclear magnetic resonance （NMR） spectroscopy and other methods. All the compounds were separated from this higher fungus for the first time.

关键词： Phellinus rhabarbarinus (Berk.) G. Cunn. Chemical component Structural identification

Syntheses of phenyl benzoate compounds and their bioactivity investigation

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Journal of Chinese Pharmaceutical Sciences 2021年第11期30卷 874-882页

作者： beidou zhou Jiali Li Baocheng Huang Zihan Yu Zetong Ma Zhipeng Ruan Qihong Cai Dongbao Hu School of Pharmacy and Medical Technology Putian UniversityKey Laboratory of Pharmaceutical Analysis and Laboratory Medicine(Putian University)Fujian Province UniversityKey Laboratory of Medical Microecology(Putian University)Fujian Province UniversityPutian UniversityPutian 351100China School of Chemical Biology and Environment Yuxi Normal UniversityYuxi 653100China

Eight phenyl benzoate compounds were synthesized in one step, and then their antioxidant, anti-tyrosinase, and anti-pancreatic lipase activities were evaluated in the present study. The total yields ranged from 31% to 85%. Compound 4 c exhibited a stronger antioxidant activity compared with Trolox, with half maximal inhibitory concentrations(IC50) of approximately 13.06 μM, and the antioxidant mechanism was further studied using computational chemistry. Compounds 1 c–5 c exhibited minimal anti-tyrosinase activity. Compounds 4 c, 5 d, 6 c and 6 d exhibited weak anti-pancreatic lipase activity, with an inhibition rate of 33.52%, 15.76%, 18.37% and 20.77%, respectively. These results demonstrated that all compounds had reference significance, especially compound 4 c.

关键词： Phenyl benzoate Synthesis Antioxidant Anti-tyrosinase Anti-pancreatic lipase

3-香叶基-2,4,5-三甲氧基苯甲酸甲酯的合成

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南昌大学学报（理科版） 2017年第1期41卷 62-65页

作者：周北斗童玉贵阮志鹏许桂芬莆田学院药学与医学技术学院福建莆田351100 莆田出入境检验检疫局福建莆田351100

以2,4,5-三甲氧基苯甲醇作为起始原料,经过叔丁基二甲基氯硅烷保护苄位羟基、香叶基的选择性取代、脱除硅保护基、沙瑞特试剂氧化苄位羟基成醛基、亚氯酸钠氧化醛基成羧基和甲酯化反应制得目标分子3-香叶基-2,4,5-三甲氧基苯甲酸甲酯。... 详细信息

以2,4,5-三甲氧基苯甲醇作为起始原料,经过叔丁基二甲基氯硅烷保护苄位羟基、香叶基的选择性取代、脱除硅保护基、沙瑞特试剂氧化苄位羟基成醛基、亚氯酸钠氧化醛基成羧基和甲酯化反应制得目标分子3-香叶基-2,4,5-三甲氧基苯甲酸甲酯。各中间体和目标分子都经核磁共振氢碳谱、红外光谱和高分辨质谱确证结构。六步总产率为31%。

关键词：香叶基苯甲酸甲酯合成

Synthesis of prenylated and geranylated xanthones and their bioactivities

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Journal of Chinese Pharmaceutical Sciences 2020年第8期29卷 564-576页

作者： beidou zhou Zihan Yu Yugui Tong Jiali Li Baocheng Huang Rongrong Wei Zhimin Weng Xin Wang Zhipeng Ruan Jian Lin Caihong Xu Jianbo Liu School of Pharmacy and Medical Technology Putian UniversityKey Laboratory of Pharmaceutical Analysis and Laboratory Medicine(Putian University)Fujian Province UniversityPutian 351100China Putian Entry-exit Inspection and Quarantine Bureau Putian 351100China The Affiliated Hospital(Group)of Putian University Putian 351100China Lianhe Chemical Technology Co. Ltd.Taizhou 318020China

Nine prenylated and geranylated xanthones were synthesized in two steps with total yields ranging from 11%to 36%.All of the compounds were first ***,the antitumor,anti-tyrosinase,anti-pancreatic lipase,antifungal and antibacterial activities of all or part of compounds 1–9 were *** 9 exhibited clear antitumor activity,and its cytotoxicity against MCF-7 and MDA-MB-231 cells was stronger compared with *** 1–4 and 6–7 also exhibited certain activity other than the antitumor activity described *** results demonstrated that compounds 1–4,6–7 and 9 were very promising leads for further structural modification.

关键词： Xanthone Antitumor activity Anti-tyrosinase Antifungal activity Antibacterial activity

福建霉素A和B的合成在有机化学教学中的应用

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保山学院学报 2017年第2期36卷 31-33页

作者：周北斗许桂芬吴毕莎莆田学院药学与医学技术学院莆田学院环境与生物工程学院福建莆田351100

适时适度地介绍福建霉素A和B的结构特征、生物活性和合成过程,阐述了臭氧化、碘代、钯催化的交叉偶联、金属氢化物的还原、狄尔斯-阿尔德等反应及其相关的知识点,为福建霉素A和B的合成被引入有机化学教学中奠定基础,使科研促进教学被有... 详细信息

适时适度地介绍福建霉素A和B的结构特征、生物活性和合成过程,阐述了臭氧化、碘代、钯催化的交叉偶联、金属氢化物的还原、狄尔斯-阿尔德等反应及其相关的知识点,为福建霉素A和B的合成被引入有机化学教学中奠定基础,使科研促进教学被有效地实践。

关键词：福建霉素合成有机化学教学应用

A New Method for Deriving High-Vertical-Resolution Wind Vector Data from the L-Band Radar Sounding System in China

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Advances in Atmospheric Sciences 2024年第11期41卷 2192-2202页

作者： Fang YUAN Zijiang zhou Jie LIAO National Meteorological Information Center China Meteorological AdministrationBeijing 100081China

High-vertical-resolution radiosonde wind data are highly valuable for describing the dynamics of the meso-and microscale atmosphere. However, the current algorithm used in China's L-band radar sounding system for calculating highvertical-resolution wind vectors excessively smooths the data, resulting in significant underestimation of the calculated kinetic energy of gravity waves compared to similar products from other countries, which greatly limits the effective utilization of the data. To address this issue, this study proposes a novel method to calculate high-vertical-resolution wind vectors that utilizes the elevation angle, azimuth angle, and slant range from L-band radar. In order to obtain wind data with a stable quality, a two-step automatic quality control procedure, including the RMSE-F(root-mean-square error F) test and elemental consistency test are first applied to the slant range data, to eliminate continuous erroneous data caused by unstable signals or radar malfunctions. Then, a wind calculation scheme based on a sliding second-order polynomial fitting is utilized to derive the high-vertical-resolution radiosonde wind vectors. The evaluation results demonstrate that the wind data obtained through the proposed method show a high level of consistency with the high-resolution wind data observed using the Vaisala Global Positioning System and the data observed by the new beidou Navigation Sounding System. The calculation of the kinetic energy of gravity waves in the recalculated wind data also reaches a level comparable to the Vaisala observations.

关键词： L-band radar sounding system upper air high-vertical-resolution radiosonde wind vectors quality control polynomial fitting

Synthesis and antitumor, antityrosinase, and antiplatelet aggregation activities of xanthone

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Journal of Chinese Pharmaceutical Sciences 2019年第4期28卷 247-256页

作者：周北斗王欣翁智敏黄堡城马泽通于博阮丽琴胡栋宝莆田学院药学与医学技术学院药物分析与检验医学福建省高校重点实验室福建莆田351100 玉溪师范学院化学生物与环境学院云南玉溪653100

In the present study, five fluorine substituted and three chlorine substituted 1,3-dihydroxyxanthones were synthesized in one *** yields ranged from 48% to 72%.Among them, compounds 12 and 15–18 were reported for the first *** antitumor, antityrosinase and antiplatelet aggregation activities of all or part of compounds 1–19 were *** 1, 2, 4, 6–7, 10–15 and 19 exhibited enhanced cytotoxicity against certain cancer *** 10, containing 2,4-difluorophenyl at the C7 position, particularly exhibited superior antitumor *** inhibition rate of compound 18 against tyrosinase was approximately 22%.Compounds 1–3, 6, 9, 12 and 18, 19 exhibited obvious inhibitory platelet aggregation induced by ADP in ***, the effects of compounds 2 and 3 were more *** results demonstrated that compounds 1–4, 6–7, 9–15 and 19 were promising leads for further structural modification.

关键词： Xanthone Synthesis Antitumor Antityrosinase Antiplatelet aggregation

1,3,6,7-四甲氧基氧杂蒽酮的简易合成

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莆田学院学报 2016年第2期23卷 29-31,37页

作者：周北斗方圆圆陈玉丽林淑凤吕楠莆田学院药学与医学技术学院福建莆田351100

介绍1,3,6,7-四甲氧基氧杂蒽酮的简易合成。首先,2,4,5-三甲氧基苯甲酸在碘甲烷、氧化银和乙腈体系中回流,得到2,4,5-三甲氧基苯甲酸甲酯;其次,用正丁基锂与1,3,5-三甲氧基苯反应,生成的苯环碳负离子随即进攻2,4,5-三甲氧基苯甲酸甲酯... 详细信息

介绍1,3,6,7-四甲氧基氧杂蒽酮的简易合成。首先,2,4,5-三甲氧基苯甲酸在碘甲烷、氧化银和乙腈体系中回流,得到2,4,5-三甲氧基苯甲酸甲酯;其次,用正丁基锂与1,3,5-三甲氧基苯反应,生成的苯环碳负离子随即进攻2,4,5-三甲氧基苯甲酸甲酯的酯羰基,甲氧基离去,得到取代二苯甲酮化合物;再次,在Al Cl3催化下,取代二苯甲酮化合物邻近羰基的一个甲氧基水解,得到水解产物;最后,该水解产物在碳酸钾、甲醇和水体系中回流,环合得到1,3,6,7-四甲氧基氧杂蒽酮。四步总产率为23.2%。这种构建氧杂蒽酮的方法可以为其他该类化合物的合成提供参考。

关键词：氧杂蒽酮合成甲氧基