Page 86 - 201810

·1694· 精细化工 FINE CHEMICALS 第 35 卷

的抑制 HeLa 细胞增殖的能力。 1982, 19: 1132-1133.
缬氨酸不仅是蛋白质的重要组成成分，也是很 [9] Liao Lianan (廖联安), Li, Zhengmin (李正名), Fang Hongyun (方红
云), et al. Synthesis and bioactivity of 5-Ivermectin B 1a esters[J].
多免疫抗菌素的重要组成成分 [23] ；缬氨酸能加快肿 Acta Chim Sinica (化学学报), 2002, 60(3): 468-474.
[4]
瘤患者的营养支持治疗 [24] ，能改善免疫机能 等作 [10] Brimble M A, Duncalf L J,Reid D C W, et al. Addition of
cyclopentadiene and 2-trimethylsilyloxyfuran to quinines
用；薄荷也具有抗炎镇痛、抗病毒等药理作用 [21-22] 。 bearingamenthyl ester chiral auxiliar[J]. Tetrahedron, 1998, 54:
但化合物 BHX 抑制肿瘤细胞的分子机理仍有待进 5363-5374.
一步研究。 [11] Tennant-Eyles R J, Fairbanks A J. Peptide templated glycosylation
reactions[J]. Tetrahedron: Asymmetry, 2000, 11: 231-243.
[12] Kim D K, Lee N, Kim Y W, et al. Synthesis and evaluation of amino
3 结论 acid esters of 6-deoxypenciclovir as potential prodrugs of
penciclovir[J]. Bioorganic & Medicinal Chemistry. 1999, 7(2):
本文首先以 DCC/DMAP 为催化剂，合成了 419-424.
BHX，并对 BHX 进行了最大电休克惊厥实验及体 [13] Li Qianrong (李前荣), Gu Chengzhi (顾承志), Yin Hao (尹浩), et al.
Synthesis of menthyl esters of N-benzoxycarbonylaminoacid using
外抑制 HeLa 细胞活性实验。在最大电休克惊厥实 DCC/DMAP[J]. Chinese Journal of Organic Chemistry (有机化学),
验中，当小鼠的 BHX 进药量为 100 mg/kg 时，与生 2005, 25(11): 1416-1419
[14] Qin Fanggang (秦方刚). Design, synthesis and evaluation of the
理盐水组及卡马西平组相比，化合物 BHX 在 MES
antiepileptic activities of α-asary-laldehyde and its derivatives[D].
模型上显示出与卡巴列平类似的生物抗癫痫活性； Xi’an: Northwest University (西北大学), 2015.
在体外抑制 HeLa 细胞活性实验中发现，BHX 具有 [15] Krall R J, Penry J K, White B G, et al. Antiepileptic drug
development: II. anticonvulsant drug screening[J]. Epilepsia, 1978,
显著的抑制肿瘤细胞增殖的能力。在后续研究中， 19(4): 409-428.
可以对 BHX 的抗癫痫活性及抗肿瘤活性进行更加 [16] Poter R J, Cereghino J J, Gladding G D, et al. Antiepileptic drug
深入的研究，揭示相关的分子机理，阐明相关的药 development program[J]. Clevland Clinic Quarterly, 1984, 51(2):
293-305.
理及毒理作用。也可采用戊四唑、3-巯基丙酸等经 [17] Zhang Rusong (张如松), Ye Yiping (叶益萍), Liu Xueli (刘雪莉).
典抗癫痫活性研究模型以及更多的肿瘤细胞模型继 Studies on in vitro antitumor activity of total steroidal glycoside from
the root of cynanchum auriculatum[J]. Chinese Traditional and
续深入研究 BHX 的生物活性。
Herbal Drugs (中草药), 2000, 30(8): 599-601.
[18] E Zheng (鄂怔). Tissue culture and molecular cytology (组织培养和
参考文献： 分子细胞学技术)[M]. Beijing: Beijing Press, 1995: 87
[1] Karau A, Grayson I. Amino acids in human and animal nutrition[J]. [19] Zhai Yanjun (翟延君), Cheng Fei (程飞),Wang Tianmin (王添敏), et
Advances in Biochemical Engineering, 2014, 143: 189-228. al. In vitro anticancer activity of taxifolin on human cervical cancer
[2] Takumi K, Namiki I, MichaelI R. et al. Branched-chain amino acids Hela cells and its mechanism[J]. Chinese Traditional Patent Medicine
as pharmacological nutrients in chronic liver disease[J]. Hepatology, (中成药), 2011, 33(12): 2052-2055.
2011, 54(3): 1063-1070. [20] Jing Xiaorong (井晓荣), Wang Chao (王超), Liang Qinchuan (梁
[3] Chipman D M, Duguleby R G, Tittmann K. Mechanisms of 秦川), et al. Advances in research on the relationship between
acetohydroxyacid synthases[J]. Chemical Biology, 2005, 9(5): cytokine lLevels and seizures[J]. Chinese Journal of Neurosurgical
475-481. Disease Research (中华神经外科疾病研究杂志), 2009, 8 (6):
[4] Chen Yi (陈熠), Peng Yi (彭艺), He Jianhua (贺建华), et al. Effects 561-563．
of valine on biochemical and immunological parameters and [21] Jing YuXia (景玉霞), Lan Wei (兰卫). The chemical composition
hormone levels in serum and milk of lactating sows[J]. China Feed and pharmacological effects of mentha canadensis[J]. Xinjiang
(中国饲料), 2009, (17): 15-20. Journal of Traditional Chinese Medicine (新疆中医药), 2012, 30(4):
[5] Wen Yajuan (温亚娟), Xiang Liling (项丽玲), Miao Mingsan (苗明 122-124．
三). Modern applied research on mentha haplocalyx[J]. Acta Chinese [22] Sheng Meifang (沈梅芳), Li Xiaomeng (李小萌), Shan Qiyuan (单
Medicine (中医学报), 2016, 31(12): 1963-1965. 琪媛 ). Research progress of chemical compositions and
[6] Wang Binqin (王炳琴), Li Zhichang (黎植昌). The preparation and pharmacological actions of mentha canadensis[J]. Chinese Archives
application of amino acid ester[J]. Amino Acids &Biotic Resources of Traditional Chinese Medicine (中华中医药学刊), 2012, 30(7):
(氨基酸和生物资源), 1995, 17(4): 40-45 . 1484-1486.
[7] Neises B, Steglich W. Simple method for the etherification of [23] Wang Juncheng (王均成), Wang Ke (王可), Zhang Chunyu (张春
carboxylic acids[J]. Angewandte Chemie International Edition, 1978, 宇). Advances in the application and breeding of L-valine [J].
17: 522-524. Fermentation science and Technology Newsletter (发酵科技通讯),
[8] Neises B, Andries T, Steglish W J. Racemisation-free esterification of 2012, 41(1): 30-34.
2-nitrohenylsulphenyl protected amino-acids by dicyclohexylcarbodi- [24] Katsurada, Naokki, Uchibori, et al. Process for producing L-valine
imide-4-dimethylaminopyridine[J]. Journal of Chemical Society, by fermentation: US5188948[P]. 1993-02-23.