Journal of Chinese Pharmaceutical Sciences

Alpinia zerumbet, a ginger plant with a multitude of medicinal properties: An update on its research findings

Eric Wei Chiang Chan, Siu Kuin Wong, Hung Tuck Chan

2017, 26(11): 775-788. DOI: 10.5246/jcps.2017.11.088

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In this review, the botany and uses of Alpinia zerumbet (yan shan jiang) are described, and the current knowledge of its phytochemistry, pharmacological properties, and clinical trials is summarized. An important ginger crop in East Asia, A. zerumbet has many uses, both medicinal and non-medicinal. Leaves are used to produce essential oils and herbal teas. Rhizomes are consumed as spices, and stem fibers are made into paper, fabrics, and handicrafts. In Brazil, tea from A. zerumbet leaves is believed to have hypotensive, diuretic, and anti-ulcerogenic properties. This species possesses many medicinal properties due to its chemical constituents, including flavonoids, phenolic acids, phenylpropanoids, kava pyrones, sterols, and terpenoids. Extracts of A. zerumbet display antioxidant, antimicrobial, insecticidal, anthelmintic, tyrosinase and melanogenesis inhibitory, anti-atherogenic, anti-aging, anti-glycation, integrase and neuraminidase inhibitory, lifespan prolongation, hair growth promotion, anticancer, antidepressant, anxiolytic, anti-obesity, analgesic, anti-inflammatory, hypolipidemic, anti-ulcerogenic, anti-platelet, osteoblastic, osteogenic, thrombolytic, and cardiacarrhythmogenic activities. Essential oils of A. zerumbet leaves have antimicrobial, larvicidal, antinociceptive, hypotensive, vasorelaxant, myorelaxant, antispasmodic, antidepressant, anxiolytic, anti-neuraminidase, anti-atherogenic, anti-aging, anti-melanogenic, anti-tyrosinase, cytoprotective, cardiodepressive, antipsychotic, analgesic, anti-inflammatory, and tissue healing activities.Clinical trials conducted in Brazil showed that extracts of A. zerumbet have hypotensive and diuretic effects whereas topical application of the essential oil has positive therapeutic effects on patients with fibromyalgia. Spanning two continents of Asia and South America, A. zerumbetis truly a multi-purpose ginger plant with promising medicinal properties.

Simultaneous quantification of flavonol glycosides, terpene lactones, polyphenols and carboxylic acids in Ginkgo biloba leaf extract by UPLC-QTOF-MSE based metabolomic approach

Yiyi Zhao, Hongzhu Guo, Yougen Chen, Xintong Fu

2017, 26(11): 789-804. DOI: 10.5246/jcps.2017.11.089

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In the present study, we established an ultra performance liquid chromatography coupled with time-of-flight mass spectrometry (UPLC-QTOF-MS^E) method to simultaneously quantify 33 components in Ginkgo bilobaleaf extracts (GBEs), including 17 flavonol glycosides, five terpene trilactones (TTLs), four polyphenols and seven carboxylic acids. This optimized method was successfully applied to analyze the explicit compositions of GBE samples collected from different places. Furthermore, the data were processed through unsupervised principal component analysis (PCA) and supervised orthogonal partial least squared discrimination analysis (OPLS-DA) to evaluate the quality and compare the differences between the samples according to the contents of the 33 chemical constituents. Bilobalide, protocatechuic acid, shikimic acid, quinic acid, ginkgolide B, ginkgolide J, kaempferol-3-O-rutinoside, isorhamnetin-3-O-rutinoside, quercetin-3-O-α-L-rhamnopyranocyl-2''-(6'''-p-coumaroyl)-β-D-glucosideand rutin were recognized as characteristic chemical markers that contributed most to control the quality of GBEs. Based on the fact that GBEs should be standardized with the characteristic components as quality control chemical markers, it is most important to maintain the quality of GBEs stable and reliable, and this method also provided a good strategy to further rectify and standardize the GBEs market.

Simultaneous determination of l-calycanthine, quercetin, and kaempferol in Chimonanthi Nitentis Folium by RP-HPLC

Rengeng Shu, Xiluan Yan, Shasha Li, Pengfei Tu

2017, 26(11): 805-810. DOI: 10.5246/jcps.2017.11.090

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A reversed-phase high-performance liquid chromatography (RP-HPLC) method was established for the simultaneous determination of three major constituents, l-calycanthine, quercetin, and kaempferol, in Chimonanthi Nitentis Folium. The RP-HPLC analysis was carried out using an Agilent HC-C₁₈ (4.6 mm×250 mm, 5 µm) column and a gradient mobile phase consisting of methanol and phosphate buffer (10:90→90:10, v/v) at a flow rate of 1.0 mL/min. The column temperature was 25 ºC and the detection wavelength was set at 239 nm from 0 to 15 min and 365 nm from 16 to 45 min. All calibration curves showed good linearity (R²≥0.9991) within test ranges. Relative standard deviations of repeated analyses were less than 2.64% (n = 6), and the recovery of this method was 97.47%-98.26%. The contents of these three analytes were determined for the samples from different harvest times. The results showed that the l-calycanthine content in herbs increases from 99.94 µg/g to 468.0 µg/g from April to July, whereas the content of quercetin and kaempferol was higher in April and May than that in June and July, which were consistent with the Chinese traditional medicine’s use of Chimonanthi Nitentis Folium in Spring. Herein, a simple, rapid and accurate analytical method is presented and successfully applied for the simultaneous quantitative analysis of alkaloids and flavones from Chimonanthus nitens Oliv.

Determination of a novel derivative of the PAC-1 anticancer agent in rat plasma by LC-MS/MS and its application to a pharmacokinetics study

Gangzhi Zhu, Qin Yi, Zhihong Fan, Yuehui Ma, Dandan Wang, Lei Wang, Zeneng Cheng

2017, 26(11): 811-818. DOI: 10.5246/jcps.2017.11.091

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A new and sensitive liquid chromatography-tandem mass spectrometry method was developed for the determination of SM-1 in rat plasma. After a simple protein precipitation, SM-1 and internal standard (gefitinib) were separated with gradient elution on a Waters XBridge C₁₈(50 mm×4.6 mm, 3.5 μm) using acetonitrile–methanol–10 mM ammonium acetate (37.5:37.5:25, v/v/v) as mobile phase. The triple quadruple mass spectrometer was set in positive electrospray ionization mode, multiple reaction monitoring was used for quantification. The precursors to produce ion transitions monitored for SM-1 and IS were m/z 407.3→203.4 and 447.3→128.3, respectively. The method validation was conducted over the curve range of 30–6000 ng/mL. The intra- and inter-day precisions were less than 4.7%, the average extraction recoveries ranged from 98.7% to 104.1% for each analyte. SM-1 was proved to be stable during sample storage preparation and analytical procedures. All the results met the acceptance criteria in accordance with the FDA guidance for bioanalytical method. Consequently, this method was successfully applied to determine SM-1 concentrations in rats after oral administrations at the doses of 200, 100 and even 50 mg/kg.

Design, preparation and activity evaluation of novel recombinant thrombolytic proteins

Guizhen Hu, Xiaoyan Liu, Yuanjun Zhu, Yinye Wang

2017, 26(11): 819-826. DOI: 10.5246/jcps.2017.11.092

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Recombinant tissue plasminogen activator (rPA) has been used as a thrombolytic agent. However, considerable improvements have been done to prolong its plasma half-life (t_1/2) and reduce its side effects, such as intracranial hemorrhage. Based on these improvements, a mutant of rPA, mrPA, was designed by mutating its PAI-1 binding site to extend its t_1/2. Furthermore, a fusion protein conjugating mrPA with NR3 was designed, which was a rAcAp5 mutant with a platelet GPIIb/IIIa-binding RGD motif, to enhance the ability of targeted-thrombus and thrombolysis. The synthesized DNA sequences coding the two proteins were amplified by PCR, cloned into pET30a to construct recombinant plasmids pET30a-mrPA and pET30a-mrPA-NR3, and transformed into E. coli BL21 (DE3). The two proteins were expressed in inclusion bodies induced by isopropyl β-D-1-thiogalactopyranoside. After purified to qualified purity using one-step Ni affinity chromatography, the denatured proteins were refolded by dialysis. Their thrombolytic effects in vitro and in vivo were evaluated. In vitro 3.5 and 7 μmol/L of mrPA significantly reduced thrombus weight; 1.75, 3.5 and 7 μmol/L of mrPA-NR3 also significantly reduced the thrombus weight, and mrPA-NR3 displayed stronger thrombolytic effects than mrPA at 7 μmol/L. In vivo both mrPA and mrPA-NR3 showed significantly thrombolytic effect at 60−240 μmol/kg in thrombolytic model of inferior vena cava. Importantly, mrPA-NR3 exhibited more potent thrombolytic effect than both mrPA and rhM-tPA (positive control) at 240 μmol/kg. In addition, these two novel proteins did not increase bleeding time while they exerted thrombolytic effect. In conclusion, we engineered two novel proteins and proved that fusion protein had better thrombolytic effect than non-fusion protein, and the results suggest that dual thrombolytic mechanism or thrombus-target potentiated the thrombolytic effect of rPA and alleviated hemorrhage side reaction. This study may shed light on the development of novel thrombolytic agents with targeted thrombolysis and reduced side effects.

Synergistic effects of a curcumin analogue and docetaxel on growth inhibition of human prostate cancer cells

Daiying Zhou, Li Ding, Xi Wang, Juan Ma, Wolin Huang, Susan Goodin, Xi Zheng

2017, 26(11): 827-833. DOI: 10.5246/jcps.2017.11.093

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Cancer of the prostate gland is a leading cause of death. In the present study, we studied the effects and mechanisms of curcumin analogue E10, docetaxel or their combination on prostate cancer (PC)-3 cells. Treatment of PC-3 cells with E10 or docetaxel resulted in growth inhibition in a concentration-reliant fashion. Combinations of E10 and docetaxel inhibited the growth of PC-3 cells in a synergistic manner. Effects of a combination of E10 and docetaxel were associated with synergistic inhibition of the transcriptional activity of nuclear factor-kappa B (NF-κB), and robust reductions in the levels of B-cell lymphoma-2 (Bcl-2) were found in PC-3 cells treated with a combination of E10 and docetaxel. Our data indicated that the effects of E10 in combination with docetaxel on PC-3 cells were associated with inhibition of NF-κB and Bcl-2. Further studies using suitable animal models are necessary to determine the in vivo effect of this combination.

Synthesis and characterization of pyrimidines analogues as anti-Alzheimer’s agents

Yadav Rakesh, Maan Monika, Yadav Divya

2017, 26(11): 834-846. DOI: 10.5246/jcps.2017.11.094

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Pyrimidine derivatives have been reported as neuroprotective agents useful for the treatment of various neurodegenerativedisorders. In the present study, several pyrimidine analogues have been evaluated as neuroprotective agents in Morris water maze model. It was observed that pyrimidine derivatives 8–17 considerably improve learning, memory, and movement deficits in animal models. Biochemical estimations of brain serum of treated animals revealed suppression of oxidative and nitrosative stress, acetylcholinesterase activity, and other parameters which leads to neurodegeneration of brain. Of all the pyrimidine derivatives, thiomorpholine derivative 8 and piperazine ethanol derivative 17 were found to be the most active neuroprotective agents and produced effects comparable to standard drug rivastigmine in terms of behavioral, biochemical, and molecular aspects.

International Symposium on Frontiers of Natural and Biomimetic Drugs---Innovations on Drugs Driven by the Integration of Chemical Biology

Tao Liu, Suwei Dong, Zhenjun Yang, Lixin Yang, Zhu Guan

2017, 26(11): 847-849.

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