Journal of Chinese Pharmaceutical Sciences

Modification at Lys24 with fatty acid generates active calcitonin gene-related peptide with much improved plasma stability

Zibo Fan, Demin Zhou

2018, 27(9): 589-599. DOI: 10.5246/jcps.2018.09.060

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As a 37-amino acid vasoactive neuropeptide, calcitonin gene-related peptide (CGRP) is widely distributed in nervous systems. The studies and clinical applications of CGRP are limited by its peptide nature and short half-life. A series of peptide analogues of the α-form of CGRP were synthesized. Afterwards, by using in vitro metabolic and activity studies, we prepared two high affinity analogues with significantly improved plasma stability.

A novel aza-naphthoquinone inhibits tumor growth by inducing apoptosis

Li Lei, Yu Chen, Simin Yang, Xiangbao Meng, Siwang Yu

2018, 27(9): 600-607. DOI: 10.5246/jcps.2018.09.061

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Natural product menaquinone has been reported to exhibit antitumor activity mediated by inhibiting IDO-1 enzyme, and naphthoquinone compounds like pyranaphthoquinone have attracted extensive research interests since they share the naphthoquinone pharmacophores. In the present study, a novel series of aza-naphthoquinones was synthesized based on 6,7-dichloroquinoline-5,8-dione structure, and their cytotoxicities were screened using lung cancer cells. Among them CY-26-11was identified as the most potent one. CY-26-11 concentration-dependently induced apoptosis in A549 human lung adenocarcinomacells, as indicated by annexin-V staining. Further experimental data show that CY-26-11 down-regulated Bcl-2 while up-regulatedBax and Puma protein levels, and activated caspase-3. Finally, CY-26-11 significantly inhibited the growth of Lewis lung carcinomaxenografts in vivo without significant major toxicities. Taken together, our results demonstrate that CY-26-11 exhibited IDO-1-independent anti-tumor effects both in vitro and in vivo, providing a new anti-tumor mechanism for naphthoquinonecompounds.

Chemical constituents from the Moutan Cortex charcoal and their potential coagulation activities

Xiaolu Yang, Xingyang Xue, Yan Lin, Qiyun Huang, Maoyan Mo, Shumei Wang, Jiang Meng

2018, 27(9): 608-616. DOI: 10.5246/jcps.2018.09.062

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The chemical constituents of Cortex Moutan charcoal were studied in depth, and their coagulation activity was screened. The chemical constituents were isolated by polyamide, silica gel and Sephadex G-Sepharose chromatography purification,and their structures were identified by NMR spectroscopy and other analyses. A total of 10 compounds were obtained and identified as follows: 3-(2-furan)-1-(2-hydroxy-4-methoxy-phenyl)-2-propylene ketone (1), 2-(2,5-hydroxy-4-methyl phenyl) propionate ethyl ester (2), methyl tetradec-5-enoate (3), 1,4-diethylcyclohexane (4), catechol (5), methyl-4-hydroxybenzoate (6), 3-hydroxy-2-methyl-4-pyrone (7), 3,8-dihydroxy-2-metyl-chromone (8), 3β-hydroxy-olean-12-en (9), 1-monolinolein (10). Among them, compounds 1 and 2 were new natural products, and 3–10 were isolated from the Cortex Moutan charcoal for the first time. The potential coagulation activities of compounds were evaluated, and compounds 2, 9 and 10had strong hemostatic effects. While compounds 1 and 8 could significantly activate blood circulation.

A new alkaloid from Chaetomium globosum

Chuanjun Huang, Xiaorui Liu, Mi Zhang, Qiong Bie, Fanrong Zeng, Yanyan Wang, Chunmei Chen, Hucheng Zhu, Yonghui Zhang

2018, 27(9): 617-622. DOI: 10.5246/jcps.2018.09.063

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A new alkaloid, methyl 6-(isoprenyl)-1H-indole-3-carboxylate (1), was isolated from the solid culture broth of fungus Chaetomium globosum, together with five known compounds, including N-acetyl-L-tryptophan (2), xylariol B (3), 5-(methoxymethyl)-1H-pyrrole-2-carbaldehyde (4), ergosterol (5) and ergosta-4,6,8(14),22-tetraen-3-one (6). Their chemical structures were elucidated by spectroscopic data (UV, IR, HRESIMS, and NMR). In addition, it is the first report of compounds 2 and 3 from the fungus Chaetomium globosum.

Development and validation of a sensitive HPLC method for the determination of lisinopril in human plasma after derivatization with 4-fluoro-7-nitro-2,1,3-benzoxadiazole

Reza Ahmadkhaniha, Noushin Rastkari, Syed Husain Hashemi Mousavi, Effat Souri

2018, 27(9): 623-629. DOI: 10.5246/jcps.2018.09.064

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In this study, we developed a simple and sensitive HPLC method for the determination of lisinopril in human plasma. The sample clean-up was carried out by solid-phase extraction (SPE) using a cation-exchange (Strata-SCX^®) extraction cartridge. After a pre-column derivatization with 4-fluoro-7-nitro-2,1,3-benzoxadiazole, the reaction mixture was analyzed on an Agilent Zorbax SB^®-C₁₈ (150 mm×4.6 mm, 5 μm). The flow rate was set at 1.0 mL/min. Fluorescence detection was performed at an excitation wavelength of 470 nm and an emission wavelength of 530 nm. The mobile phase consisted of a mixture of methanol and 0.02 M sodium dihydrogen phosphate (pH = 3.0, 60:40, v/v). The average extraction recovery of lisinopril and fluvoxamine (internal standard) was >85%. The method exhibited a linear calibration curve over the concentration range of 1–1000 ng/mL with a correlation coefficient (r²) of ≥0.98 and a limit of quantification (LOQ) equal to 2 ng/mL. The within-run and between-run precisions were satisfactory with an RSD of 3.8%–13.7% (accuracy: from 95.0% to 96.4%) and 4.273%–14.3% (accuracy: from 94.4% to 98.5%), respectively.

Pharmaceutical practice and value of pharmacists under the new medical reform situation

Shuyun Feng, Jinhui Guo, Yizhong Lu

2018, 27(9): 630-636. DOI: 10.5246/jcps.2018.09.065

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Zero addition of drugs is an important aspect of medication reformation in the whole country, which is the end of the era of medicine. The role of pharmacists is changing from being medication dispensers to outcome-oriented and patient-focused care providers. However, it is still unclear how to play the role of pharmacists and carry out the related work in the new situation. Here, literature for relevant evidence was searched and summarized. Analysis results showed that there was a significant gap between pharmacy practice in China and developed countries. Evidence has supported pharmacists in their emerging role as care providers, that is available to improve the efficacy and quality of pharmaceutical care and ensure the safety of medicines for patients, but still more efforts are needed to promote new attitude toward more professional career, such as paying attention to the examination of outpatient prescription and medical orders, deeply clinical practice and individualized treatment, self-enhancement and public awareness of pharmacists. Collectively, the safety of patients can be ensured only by improving profession of pharmacists and showing the value of pharmacists. In doing so, pharmacy can develop rapidly, and pharmaceutical care with rational drug use can be realized.

Status quo of resource allocation of Chinese grass-roots food and drug administrations: from 2011 to 2016

Mengyuan Que, Ting Yin, Xiaoping Li, Bin Jiang

2018, 27(9): 637-643. DOI: 10.5246/jcps.2018.09.066

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County grass-root food and drug administrations (CGFDA) undertake the front-line supervision of food and drug safety, whose resource allocation is vitalto the regulation efficiency and performance. In this article, we aimed to analyze the status quo of resource allocation of CGFDA from the aspects of regulatory organization, staff, funding and equipment using officialpanel data from 2011 to 2016. The results illustrated that the total amount of regulatory resources of CGFDA was increased annually, reaching a rather large scale. However, many problems still existed in its allocation. Therefore, a series of measures should be taken to optimize the resource allocation of CGFDA, such as improving the network of institutional CGFDA, increasing the recruitmentrequirements on educational level and major, reallocating the structure of resources and guaranteeing the resource demand in less-developed areas.

Crystal structure of trans-3-phenyl-2-propenoic acid

Yucui Ma, Liang Xu, Cui Wu, Zhimao Chao

2018, 27(9): 644-648. DOI: 10.5246/jcps.2018.09.067

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The title compound of trans-3-phenyl-2-propenoic acid (C₉H₈O₂), a main active organic acid of cinnamon bark and styrax, was obtained by oxidization from trans-3-phenyl-2-propenaldehyde and characterized by X-ray diffraction analysis. It crystallizes in monoclinic system, space group P2₁/n with a = 5.55916(10), b = 17.4870(3), c = 7.70677(13) Å, V = 744.89(2) Å³, Z = 4, D_c= 1.321 g/cm³, M_r= 148.15, F(000) = 312, and μ = 0.764 mm^–¹. A total of 2661 reflections with 1447 unique ones (R_int = 0.0137) were collected, in which 1447 were observed (I>2σ(I)).There were two C₉H₈O₂ molecules in an asymmetric unit. The structural unit was a dimer formed by the hydrogen bonding of the oxygen atom of carbonyl group and the hydrogen atom of hydroxyl group. A 3D layer structure was formed through hydrogen bonds andVan der Walls’ forces.

Information from US FDA

http://www.fda.gov

2018, 27(9): 649-652.

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