Journal of Chinese Pharmaceutical Sciences

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2014, 23(6): 343-346.

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Chemistry of the Chinese herbal medicine Puerariae Radix (Ge-Gen): A review

Wei Song, Yanjiao Li, Xue Qiao, Yi Qian, Min Ye

2014, 23(6): 347-360. DOI: 10.5246/jcps.2014.06.048

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Puerariae Radix (Ge-Gen in Chinese) is a popular traditional Chinese herbal medicine derived from the dried roots of Pueraria lobata (Willd.) Ohwi or P. thomsonii Benth. It shows significant pharmacological activities in the treatment of cardiovascular diseases, hypertension, and diabetes. This review summarizes progress in the chemistry study of Pueraria species, mainly covering the classes of flavonoids, puerosides, coumarins, triterpenoids, and triterpene saponins. Qualitative and quantitative chemical analyses are also covered.

Panax notoginseng saponins protect against chronic ethanol-induced hepatic steatosis

Renbo Ding, Jiaolin Bao, Yiwei Cao, Chengwei He, Yitao Wang, Jianbo Wan

2014, 23(6): 361-368. DOI: 10.5246/jcps.2014.06.049

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Chronic alcohol consumption induces hepatic steatosis, the early stage of alcoholic liver disease (ALD). The aim of present study is to investigate the protective effect of Panax notoginseng saponins (PNS) against chronic ethanol-induced hepatic steatosis in vivo. Mice were pair-fed a modified Lieber-DeCarli liquid diet containing alcohol or isocaloric maltose dextrin as control diet with or without PNS (200 mg/kg, BW) for 8 weeks. Animals supplemented with PNS were protected against hepatic lipid accumulation induced by chronic ethanol exposure. Accordingly, PNS could significantly decrease the elevation of plasma triglyceride, plasma enzyme activities, i.e. alanine aminotransferase (ALT) and aspartate aminotransferase (AST), and hepatic TNF-α and IL-6 levels which were induced by chronic alcohol exposure. In addition, PNS markedly reduced the lipolysis of white adipose tissue (WAT) that stimulated by alcohol feeding through the inhibiting protein expression of phosphorylation of hormone-sensitive lipase (p-HSL), rather than total HSL. Furthermore, alcohol exposure also enhanced fatty acid uptake capacity in liver by elevated hepatic CD36 expression, which could attenuated by PNS treatment. These results demonstrate that PNS supplementation protects against chronic ethanol-induced hepatic steatosis, which is associated with ameliorating dysfunctional lipid metabolism of WAT and the reduced inflammatory cytokines. Our findings suggested that PNS might be potential to be developed as an effective agent for the treatment of chronic alcoholic steatosis.

Characterization of proanthocyanin-related leucoanthocyanidin reductase and anthocyanidin reductase genes in Lycium ruthenicum Murr.

Xiaofei Shen, Shaohua Zeng, Min Wu, Chunzhao Liu, Ying Wang

2014, 23(6): 369-377. DOI: 10.5246/jcps.2014.06.050

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Proanthocyanidins (PAs) are a set of important phytochemical compounds in Lycium ruthenicum Murr. However, PA biosynthesis in L. ruthenicum remains unclear. In this study, leucoanthocyanidin reductase (LAR) and anthocyanidin reductases (ANR) involved in PA biosynthesis wereretrieved from L. ruthenicum EST database. Polymerase chain reaction (PCR) results confirmed that LrLAR and LrANR encoded a protein composed of 333 and 338 amino acids, respectively. Phylogenetic analysis showed that LrLAR and LrANR were clustered with known LAR and ANR proteins of other plants, respectively. Quantitative reverse-transcription PCR (qRT-PCR) results indicated that both genes expressed in a sharp increase manner from unripe stage to color break stage and were down-regulated increasingly hereafter, and that both expression levels are extremely low in young leaves, mature leaves, stems, and roots compared with fruits. Phytochemical assay revealed that the content of total PA in fruit was higher than that in young leaves, mature leaves, stems, and roots, and that the total PA level was increased sharply and then relatively stable hereafter during fruit ripening. Our results lay a foundation for uncovering the PA biosynthesis and further engineering manipulation in L. ruthenicum.

Effects of (–)-5-hydroxy-equol on the lifespan and stress resistance of Caenorhabditis elegans

Conghui Zhang, Xiuling Wang, Xiaolin Liang, Honglei Zhang, Qinghong Hao

2014, 23(6): 378-384. DOI: 10.5246/jcps.2014.06.051

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Caenorhabditis elegans (C. elegans) was used as an animal model to study the effect of (–)-5-hydroxy-equol, a microbial metabolite of isoflavone genistein, on the lifespan, fecundity and resistance against thermal and oxidative stress. The results showed that (–)-5-hydroxy-equol not only significantly increased the lifespan of C. elegans but alsosignificantly enhanced the resistance against thermal and oxidative stress at the concentrations of 0.1 mmol/L and 0.2 mmol/L. However, the fecundity ofC.elegans was not obviously influenced after being exposed to the same concentrations of (–)-5-hydroxy-equol. Furtherstudieson comparative transcriptome analyses and the lifespan of daf-16 (mu86) mutant and daf-2 (e1370) mutantindicated that(–)-5-hydroxy-equol prolonged the lifespan of C.elegansthrough DAF-2/DAF-16 Insulin/IGF-1 signaling pathway.This is the first report that (–)-5-hydroxy-equol was able to increase the lifespan and improve the thermal and oxidative stress tolerance of C. elegans.

In vitro studies on the multi-target anti-Alzheimer activities of berberine-like alkaloids from Coptidis Rhizoma

Ying Hu, Yanfang Yang, Wenzhi Yang, Yingtao Zhang

2014, 23(6): 385-392. DOI: 10.5246/jcps.2014.06.052

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Coptidis Rhizoma, a well known heat-clearing Chinese Materia Medica, exhibited multi-target anti-Alzheimer effects in vitro through inhibition of Aβ42 aggregation, AChE, and BACE1. Six berberine-like alkaloids were found to be the major active constituents of Coptidis Rhizoma by HPLC analysis along with activity assays. A standard combination of the six major alkaloids was demonstrated to fully reproduce the in vitroeffects of Coptidis Rhizoma. Molecular docking studies revealed that berberine-like alkaloids could directly bind at the active sites of Aβ42, AChE, and BACE1 through hydrophobic interactions, aromatic stacking, and electrostatic interactions.

Characterization of principal compositions in the roots of Angelica sinensis by HPLC-ESI-MSn and chemical comparison of its different parts

Yanyan Wu, Lu Wang, Guangxue Liu, Feng Xu, Mingying Shang, Shaoqing Cai

2014, 23(6): 393-402. DOI: 10.5246/jcps.2014.06.053

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Angelicae Sinensis Radix, Danggui in Chinese, is an important traditional Chinese medicine derived from the roots of Angelica sinensis (Oliv.) Diels. HPLC-ESI-MSⁿ was applied to analyze the chemical constituents in the methanol extract of Danggui. A total of 24 compounds were identified or tentatively characterized based on their UV and mass spectra, containing 11 phenolic compounds, 12 phthalides and 1 amino acid. Three dicaffeoylquinic acids, 5-feruoylquinic acid and ferulic acid hexoside were detected in A. sinensis for the first time. According to Chinese medicine theories, the three parts of Danggui (Guitou, Guishen, Guiwei) have different therapeutic effects and their substantial evidence has not been clearly elucidated yet. In the present study, the chemical compositions of different parts of Danggui were investigated by using the established HPLC method. The result indicated that the content of tryptophan was getting lower and the contents of low polarity constituents like phthalides trended to get higher from Guitou to Guiwei. This might partly explain the therapeutic effects of different parts of Danggui.

Pharmacokinetic and tissue distribution studies of paeoniflorin and albiflorin in rats after oral administration of total glycosides of paeony by HPLC-MS/MS

Minmin Zhao, Meng Gao, Yulu Tian, Yingfeng Du, Chunying Wang, Huijun Xu, Lantong Zhang, Qiao Wang

2014, 23(6): 403-411. DOI: 10.5246/jcps.2014.06.054

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A simple, sensitive and specific high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method combined with solid phase extraction has been developed and validated for the simultaneous quantification of paeoniflorin and albiflorin in rats plasma and tissue homogenate after administration of total glycosides of paeony (TGP). Chromatographic separation was achieved on a C₁₈column (150 mm×4.6 mm, 5 μm) with mobile phase consisted of acetonitrile–0.05% formic acid aqueous (20: 80, v/v) at a flow rate of 0.5 mL/min. The analytes were detected with triple-quadrupole mass spectrometer using turbo ion spray with negative ionization in the multiple reaction-monitoring (MRM) modes. The results of method validationconformed to the requirements for the determination of biological samples. This method was successfully applied to the pharmacokinetics and tissue distribution study of TGP in rats. The results showed that paeoniflorin and albiflorin were absorbed and reached peak value quickly, and had the similar pharmacokinetic characteristics. Both of them underwent a rapid and wide distribution in the tissues throughout the whole body, among which stomach was the main distribution tissue. Moreover, they had the ability to cross the blood-brain barrier.

Resources and utilization of Taoist Medicinal Plants distributed in Wudang Mountain

Guangyi Yang, Hubiao Chen, Zhongzhen Zhao, Tao Yi, Jiyan Chen

2014, 23(6): 412-420. DOI: 10.5246/jcps.2014.06.055

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The purposes of this investigation were: (1) to document Taoist herbal medicine in Wudang District, including which plant species and the ways of processing and administrations; (2) to compare the utilization of medicinal herbs of Taoist medicine in Wudang Disctrict and Traditional Chinese Medicine (TCM). In this study, based on our botanical survey, 178 species medicinal plants belonging to 75 families were recorded by Wudang Taoist. Out of these, the most important species were Compositae, Labiatae, Liliaceae, Leguminosae, Berberidaceae, Polygonaceae, Rosaceae and Ranunculaceae. The study revealed that wine, tea and bath were most popular forms of administration in Taoist medicine. Our study is the first time to document Taoist medicinesystematically. Taoist medicine culture can have its characteristics and bring honor to the world cultural heritage–Wudang Mountains, and then make greater contributions for human health and longevity.

Two terpenoids and a polyketide from the endophytic fungus Trichoderma sp. Xy24 isolated from mangrove plant Xylocarpus granatum

Min Zhang, Ning Li, Ridao Chen, Jianhua Zou, Chunmei Wang, Jungui Dai

2014, 23(6): 421-424. DOI: 10.5246/jcps.2014.06.056

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Three known compounds were isolated from the endophytic fungus Trichoderma sp. Xy24 from a mangrove plant Xylocarpus granatum by using various column chromatography techniques. Their structures were identified as harzianone (1), trichoacorenol (2), and trichodimerol (3) by extensive spectroscopic analysis. Among them, 1 was a harziane diterpene, 2 wasa sesquiterpene alcohol, and 3 was a polyketide with a completely symmetric configuration. Compound 3 exhibited medium inhibitory activity with an IC₅₀ value of 74.6 μMusing a NA (H7N9)/MUNANA model.

Lignans from Pilea cavaleriei Levl subsp. cavaleriei

Yong Zhou, Hengchun Ren, Ridong Qin, Qingying Zhang, Hong Liang

2014, 23(6): 425-428. DOI: 10.5246/jcps.2014.06.057

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A new lignan glycoside, named (7S,8R,8′R)-(−)-lariciresinol-9-O-α-L-rhamnopyranosyl (1→2) β-D-glucopyranoside (1),was isolated from the ethanol extract of Pilea cavaleriei Levl subsp. cavaleriei, together with 17 known lignans (2−18). The structures of these compounds were elucidated by extensive spectroscopic analysis, including 1D NMR, 2D NMR and HR-ESI-MS. All the compounds were obtained from the genus Pilea for the ﬁrst time.

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