Tetrahydroxy stilbene glycoside ameliorates neuroin-flammation for Alzheimer's disease via cGAS-STING / 中国药理学与毒理学杂志

OBJECTIVE Alzheimer's disease(AD)is the most common neurodegenerative disease worldwide.Neuroinflammation is a potential target for the patients with AD.It is attributed to activated microglia and the release of various inflammatory mediators from infec-tion,ischemia and toxin accumulation.Accumulating evi-dence has indicated that the cGAS-STING pathway driven neuroinflammation in neurological disease.TSG is a main natural active ingredient that derived from polyg-onum multiflorum.Previous research from our group found that TSG has beneficial effects of anti-aging,anti-inflammatory action and improving memory function in APP/PS1 transgenic AD mice.Here,we investigated the effects of TSG on cognitive impairment and neuroinflam-mation in APP/PS1-AD mice and explore the underly-ing mechanism by which TSG ameliorates memory func-tion in the cGAS-STING-mediated inflammatory response.METHODS The Morris water mace test and the novel object recognition test were performed to test the effects of TSG on spatial learning and cognitive and memory abil-ity in APP/PS1 double transgenic AD mice model.In addi-tion,real-time quantitative PCR,Western blotting,ELISA analysis,and flow cytometry to examine gene and pro-tein expression of cGAS-STING related pro-inflammatory cytokines and chemokines.Statistical analyses were ana-lyzed using the SPSS 25.0 package by analysis of vari-ance(ANOVA).Neuman-Keuls or Tukey's multiple-com-parisons test were conducted as ANOVA justified post hoc comparisons between group means.RESULTS We demonstrated that AD transgenic mice exhibited cognitive deficits accompanied by the elevated serum and brain inflammation.The expressions of serum inflammatory cytokines and the activation of microglia in cerebral cor-tex and hippocampus were suppressed after TSG treat-ment,which was probably attributable to the decrease of cyclic GMP-AMP synthase(cGAS)and stimulator of interferon genes(STING)triggered immune response.Additionally,the data showed that TSG treatment reduced the expression level of inflammatory cytokines(IL-1β,TNF-α,IFN-β,IFN-α)in microglial cells BV2 primed with LPS and IFN-γ.CONCLUSION TSG implicated the health benefits in preventing cognitive disorders by inhib-iting neuroinflammation via cGAS-STING signalling path-way in AD.

Tetrahydroxy stilbene glycoside protects mice from acetaminophen-induced liver injury: study based on metabonomics / 中国临床药理学与治疗学

AIM: To explore the pharmaceutical effects of tetrahydroxy stilbene glycoside (TSG) on acute liver injury induced by acetaminophen (APAP) using method of non-targeted metabonomics. METHODS: SPF C57BL/6 mice were randomly divided into the group of APAP-induced model and the group of TSG intervention groups (n=15). After intragastric administration of TSG for 7 days, the mice were injected once by APAP via intraperitoneal injection and the livers were taken 6 hours later. RESULTS: H&E staining, MDA and SOD tests showed that the injection of APAP could cause hepatic injury, but TSG could reduce the severity of liver injury. The results of metabolite detection showed that there were significant changes in ABC transporter, choline metabolism, central carbon metabolism, galactose and alanine amino acid metabolism in TSG groups compared with APAP model group. CONCLUSION: TSG protects against acute liver injury induced by APAP, mainly by improving lipid peroxidation and disorder of energy metabolism.

Effect of TSG on GSK3β，PKA and PP2A of APP/PS1/Tau Triple-transgenic Mice Dementia Model / 中国实验方剂学杂志

Objective:To observe the effect of tetrahydroxy stilbene glycoside （TSG） on the expression of glycogen synthase kinase 3<italic>β </italic>（GSK3<italic>β</italic>）， cyclic adenosine monophosphate-dependent protein kinase （PKA） and Serine/threonine phosphatase 2A（PP2A） in the brain of amyloid precursor protein/presenilin-1/Tau （APP/PS1/Tau） triple-transgenic mice dementia model. Method:A total of forty-five 8-month-old APP/PS1/Tau transgenic mice were randomly divided into model group， positive control group （Huperzine-A， 0.15 mg·kg^-1）， low， medium and high dose TSG groups （TSG， 0.033，0.1，0.3 g·kg^-1）， with 9 mice in each group， and another nine C5B7L/6J mice of the same age were selected as normal control group. After 60 days of intragastric administration， the general structure of hippocampal neurons was observed by hematoxylin-eosin （HE） staining， immunohistochemical （IHC） was used to detect the expression of PKA protein in the brain of mice in each group， the mRNA expression levels of GSK3<italic>β</italic>， PKA and PP2A were detected by real time quantitative reverse transcription polymerase chain reaction （Real-time PCR）， and protein expression levels of GSK3<italic>β</italic> and PP2A were detected by Western blot. Result:Compared with the normal control group， the apoptosis level of neurons in the model group was significantly increased， the protein and mRNA expression levels of GSK3<italic>β</italic> and PKA were significantly increased （<italic>P</italic><0.05， <italic>P</italic><0.01）， and the protein and mRNA expression levels of PP2A were significantly decreased （<italic>P</italic><0.05， <italic>P</italic><0.01）. Compared with the model group， the apoptosis level of neurons in each treatment group was significantly down-regulated， the protein and mRNA expression levels of GSK3<italic>β</italic> and PKA were significantly down-regulated （<italic>P</italic><0.05， <italic>P</italic><0.01）， and the protein and mRNA expression levels of PP2A were significantly increased （<italic>P</italic><0.05， <italic>P</italic><0.01）. Conclusion:The mechanism of TSG in the treatment of Alzheimer's disease （AD） may be related to lowering the transcription and expression of GSK3<italic>β</italic> and PKA， increasing the transcription and expression of PP2A.

Chemical constituents of Schoenoplectus tabernaemontani / 中草药

Objective: To study the chemical constituents of the rhizomes of Schoenoplectus tabernaemontani. Methods: Compounds were isolated and purified by a combination of column chromatography including silica gel, polyamide and Sephadex LH-20. Their structures were elucidated by physiochemical properties and NMR analysis. Results: Twelve compounds were obtained from water extract of the rhizome of S. tabernaemontani and identified as 5,7,2',4'-tetrahydroxy-3, 5'-dimethoxyflavone (1), tricin (2), hesperetin (3), quercetin (4), luteolin (5), eriodictyol (6), apigenin (7), naringenin (8), chrysin (9), 5,7-dihydroxychromone (10), catechin (11) and tricin-7-O-β-D-glucoside (12), respectively. Conclusion: Compound 1 is a new flavone named schoenin. Compounds 2-5 and 7-12 are isolated from the Cyperaceae for the first time. Compound 6 is isolated from the genus Scirpus for the first time.

Developing spectrum-toxicity relationship with rough set theory for hepatotoxicity material basis of Polygonum multiflorum / 中国中药杂志

Idiosyncratic hepatotoxicity of Polygonum multiflorum has attracted a great attention in the world. The most toxic part of idiosyncratic hepatotoxicity was screened by MTT assay and flow cytometry, which was the 50% ethanol elute by macroporous adsorptive resins from alcohol-extraction of P. multiflorum. The fingerprints were collected by HPLC from 50% ethanol elute of crude and processed P. multiflorum from different habitats, then 14 common peaks were determined. Spectrum-toxicity relationship was analyzed by rough set theory(RST). Two main chemical components were predicted for idiosyncratic hepatotoxicity, in which TSG was the greater contributor. Idiosyncratic hepatotoxicity of TSG was tested in vitro, and the results indicated that TSG was the most important constituent contributed to idiosyncratic hepatotoxicity of P. multiflorum. The study showed the discovery of the main chemical components for idiosyncratic hepatotoxicity, and RST was effective for analyzing the spectrum-toxicity relationship, which could be a new method used in the effective/toxic constituents field of traditional Chinese medicine.

Isolation of chemical ingredients from Aster ageratoides and their anticomplement and anti-inflammatory activities / 中草药

Objective To isolate and identify chemical ingredients with anti-complement activity from Aster ageratoides and investigate the key targets and anti-inflammatory activities of obtained compounds with good anti-complement activity. Methods Using silica gel column, sephadex LH-20 column, Medium Pressure Liquid Chromatography system, and Semi-preparative HPLC, chemical ingredients that displayed anti-complement activity were isolated. Their chemical structures were identified by 1H-NMR and 13C-NMR and their anti-complement activities and targets were investigated by erythrocyte hemolysis in vitro. In addition, using LPS-stimulated RAW264.7 cells, we investigated the anti-inflammatory activity of compound 2. Results A total of 14 compounds were obtained from A. ageratoides and identified as oleanolic acid (1), quercetin (2), kaempferol (3), 3,5,7,3’-tetrahydroxy- 4’-methoxyflavone (4), kaempferol-7-O-α-L-rhamnopyranoside (5), quercetin-3-O-β-D-glucopyranoside (6), kaempferol-3-O-α-L- rhamnoside (7), quercetin-3-O-α-L-rhamnoside (8), kaempferide-3-O-β-D-glucopyranoside (9), kaempferol-3-O-β-D- glucopyranoside (10), kaempferol-7-O-β-D-glucopyranoside (11), kaempferol-3-O-β-D-glucopyranoside-7-O-β-D-glucopyranoside (12), kaempferide-3-O-α-L-rhamnoside-(1→6)-β-D-glucopyranoside (13), and rutin (14). They all exhibited anti-complement activity to some certain degree and good structure-activity relationship. The targets of compounds 1 and 2 were C1q, C5, and C9 and C1q, C2, C5, and C9, respectively. The anti-inflammatory experiments indicated that compound 2 exhibited a significant biological activity, which significantly suppressed the release of NO, TNF-α, and IL-6 and expressions of iNOS and COX-2. Conclusion A total of 14 compounds were obtained and they all displayed anticomplement activity, of which compounds 1, 4, 6, 9, 12, and 13 are firstly discovered in A. ageratoides. Compound 2 exhibited a significant anti-inflammatory activity.

Analysis of HPLC Characteristic Chromatogram of Standard Pieces of Polygoni Multiflori Radix / 中国实验方剂学杂志

Objective: To establish HPLC characteristic chromatogram of standard pieces of Polygoni Multiflori Radix, and compare with the HPLC characteristic chromatograms of original pieces, raw materials and control materials of Polygoni Multiflori Radix. Method: HPLC analysis was carried out on a Waters BEH-C18 column (4.6 mm×250 mm, 5 μm) with the mobile phase of methanol(A)-0.1%phosphoric acid(B) for gradient elution (0-20 min, 15%-30%A; 20-35 min, 30%-40%A; 35-55 min, 40%-75%A; 55-75 min, 75%-100%A) at a flow rate of 0.8 mL·min-1. The detection wavelength was set at 270 nm and the column temperature was maintained at 30℃. The injection volume was 10 μL. Moreover, similarity and cluster analysis of HPLC characteristic chromatograms of four samples of Polygoni Multiflori Radix were performed. Result: HPLC characteristic chromatogram of standard pieces of Polygoni Multiflori Radix composed of seven peaks was established. The similarity was 0.999 between characteristic chromatograms of standard pieces and original pieces, which was better than similarities among characteristic chromatograms of raw materials, control materials and original pieces. There was no obvious difference on number of peaks between characteristic chromatograms of standard pieces and original pieces, while an obvious difference on number of peaks between chromatograms of control materials and original pieces was found. In addition, standard pieces, original pieces and control materials could generally gather into one class, while raw materials could generally gather into another class. Conclusion: Compared with the raw materials and control materials, the established HPLC characteristic chromatogram of standard pieces can better reflect the internal quality of original pieces, which can be used for the quality control of decoction pieces of Polygoni Multiflori Radix.

Neuroprotective Effect of Tetrahydroxy Stilbene Glucoside on Aβ25-35-induced Neuron Synapses via CREB/BDNF Signaling Pathway / 中国实验方剂学杂志

Objective: To investigate the neuroprotective effect and mechanism of tetrahydroxy stilbene glucoside (TSG) on β-amyloid protein 25-35 (Aβ25-35)-induced neuron synapses damage. Method: Primary neurons were isolated and purified from cerebral cortex of suckling mouse. Then neurons were divided into control group, model group (incubation with Aβ25-35) and TSG groups (after incubation with Aβ25-35, add 6.25, 12.5, 25, 50, 100 μmol·L-1 TSG). Cell counting kit-8 (CCK-8) and Lactate dehydrogenase (LDH) methods were used to observe the viability of neuron, immunocytochemical staining was performed to determine the expressions of synapsin-1 (SYN-1), and the concentration of postsynaptic density-95 (PSD-95) and synaptophysin (SYP) were detected by enzyme-linked immunosorbent assay (ELISA) method. The level of cyclic adenosine monophosphate response element binding protein (CREB) and brain-derived neurotrophic factor (BDNF) mRNA were determined by reverse transcription-polymerase chain reaction (RT-PCR) and the level of CREB, Phosphorylated CREB (p-CREB) and BDNF proteins were determined by immunocytochemical staining or Western blot (WB). Result: Compared with normal group, the cell survival rate of model group was significantly reduced, LDH release was significantly increased (PPPPPPP-1,25 μmol·L-1 TSG can significantly enhance the expression of SYN-1(PPPPConclusion: TSG possesses the neuroprotective effect on Aβ25-35-induced neuron synapses, the mechanism may be associated with the activation of CREB/BDNF signaling pathway.

Chemical constituents from roots of Rosa cymosa / 中草药

To study the chemical constituents from the roots of Rosa cymosa. Methods: The chemical constituents were isolated and purified by silica gel chromatography repeatedly from the roots of R. cymosa, and their structures were identified by spectral analysis and chemical Methods:. Results: Sixteen compounds were isolated from the roots of R. cymosa and identified as 2-acetyl tormentic acid (1), 2-oxo-pomolic acid (2), 2α,3α,19α-trihydroxy-olean-12-en-28-O-β-D-glucopyranoside (3), kaji-ichigoside F1 (4), rosamultin (5), 23-hydroxy-tormentic acid (6), arjunetin (7), 2α,3α,19α,23-tetrahydroxy-urs-12-en-28-O-β-D-glucopyranoside (8), 1β, 3α,19α,23-tetrahydroxy-urs-12-en-28-O-β-D-glucopyranoside (9), catechin (10), 3,4-dihydroxyphenylethyl alcohol 8-O-β-D- glucoside (11), 3,4,5-trimethoxyphenyl-1-O-β-apiofuranosyl (1’’→6’)-β-glucoside (12), 4-hydroxy-3-methoxy-1-phenyl-O-(6’- O-galloyl)-β-D-glucopyranoside (13), ethyl gallate (14), 3,4,5-trimethoxyphenyl-β-D-glucopyranoside (15), and 3,4,5-trimethoxy- benzyl-β-D-glucopyranoside (16). Conclusion: Compounds 9, 11-13, 15, 16 were obtained from this genus for the first time, and compounds 3, 9, 11-16 were obtained from this plant for the first time.

One new diterpenoid alkaloid from roots of Aconitum sinomontanum / 中草药

Objective: To study the chemical constituents from the roots of Aconitum sinomontanum. Methods: Silica gel, Sephadex LH-20 column chromatography, high performance liquid chromatography, and other chromatographic techniques were used for separation and purification. The structures were elucidated by physiochemical methods and spectral data. Results: Five compounds were isolated from the 80% ethanol extract in the roots of A. sinomontanum, and their structures were identified as 6β,7β,8β,15α- tetrahydroxy-1α,14α,16β,18β-tetramethoxy-aconitan-19-en (1), delcosine (2), lepenine (3), napelline (4), and kirinine B (5). Conclusion: Compound 1 is a new compound named sinomontanum J. Compounds 2-5 are isolated from A. sinomontanum for the first time.

Effects of 2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glycoside on Senile Plaques Formation and Inflammatory Response in APP/PS1 Mice / 中国康复理论与实践

@#Objective To observe the effects of 2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glycoside (TSG) on formation of senile plaques and beta amyloid (Aβ), as well as activation of microglia and astrocytes, in cortex and hippocampus of APP/PS1 double transgenic mice. Methods A total of 64 five-month-old APP/PS1 mice were randomly divided into model group (n=16), low-dose TSG (0.05 g/kg) group (n=16), high-dose TSG (0.1 g/kg) group (n=16), and donepezil group (n=16); other 32 same age wild type (WT) mice were randomly divided into normal control group (n=16) and high-dose TSG (0.1 g/kg) WT group (n=16). The normal control group and model group were given distilled water, and the other groups were given the corresponding drugs intragastrically. The mice were tested with object recognition test, the deposi-tion of plaques in brain was detected with Congo red staining, and the expression of Aβ40/42, ionized calcium bind-ing adapter molecule 1 (Iba1) and glial fibrillary acidic protein (GFAP) with immunohistochemistry after seven months of treatment (twelve-month-old). Results Compared with the model group, the discrimination index significantly increased (P<0.01), the deposition of plaques decreased in brain (P<0.05), and the expression of Aβ40/42, Iba1 and GFAP all significantly decreased in each treatment group (P<0.05). Conclusion TSG can improve learning and memory of APP/PS1 transgenic mice, reduce Aβ deposition and senile plaques, and reduce the inflammatory response, even in low-dose, which is similar to that of donepezil.

Chemical constituents of acrial part of Bupleunum malconense / 中草药

Objective: To investigate the chemical constituents in the dried acrial part of Bupleunum malconense. Methods: Column chromatography, such as silica gel, MCI, and Sephadex LH-20 were used to isolate the compounds. Spectroscopic methods such as 1H-NMR and 13C-NMR were used to elucidate their structures. Results: Eleven compounds were separated and identified as quercetin (1), quercetin-3-O-α-L-arabinofuranoside (2), eriodictyol (3), 3',4',5,7-tetrahydroxy-3-methoxyflavone (4), protocatechuic acid (5), quercetin-3-O-α-L-rhamnopyranoside (6), kaempferol (7), isorhanmetin (8), rutin (9), β-sitosterol (10), and daucosterol (11). Conclusion: All 11 compounds are isolated from the plants in B. malconense for the first time. Compounds 3 and 4 are isolated from the plants in genus Bupleunum L. for the first time.

Simultaneous determination of eight components in root of swertia kingii by hplc / 中草药

Objective To establish an HPLC method for simultaneously determining eight components, such as sweroside, gentiopicroside, isoorientin, 1,3,7,8-tetrahydroxy-xanthone-1-O-β-D-glucopyranosyl, swertianolin, 1,3,7,8-tetrahydroxy-xanthone, demethylbellidifolin, and 1,5,8-trihydrox-3-methoxyxanthone in the root of Swertia kingii. Methods Chromatographic analysis was achieved on an Agilent Zorbax ODS column (250 mm × 4.6 mm, 5 μm) by gradient elution of acetonitrile-0.5% phosphoric acid in water at 30 ℃. The flow rate was 1.0 mL/min and the detection wavelength was 254 nm. Results The calibration curves of all the eight constituents showed good linearity in a relatively wide concentration range. The linear ranges of swertiamarin, gentiopicroside, isoorientin, 1,3,7,8-tetrahydroxy-xanthone-1-O-β-D-glucopyranosyl, swertianolin, 1,3,7,8-tetrahydroxy-xanthone, demethylbellidifolin, and 1,5,8-trihydrox-3-methoxyxanthone were 3.84-96.00 μg/mL (r = 0.999 6), 3.36-84.00 μg/mL (r = 0.999 2), 5.92-148.00 μg/mL (r = 0.999 8), 4.81-118.00 μg/mL (r = 0.999 2), 4.32-108.00 μg/mL (r = 0.999 3), 4.16-104.00 μg/mL (r = 0.999 2), 5.12-128.00 μg/mL (r = 0.999 4), 4.80-120.00 μg/mL (r = 0.999 6), respectively. The average recoveries were 99.59% (RSD 0.99%), 98.95% (RSD 3.37%), 98.61% (RSD 1.87%), 99.63% (RSD 1.93%), 99.31% (RSD 1.21%), 99.50% (RSD 1.62%), 99.80% (RSD 0.54%), and 98.50% (RSD 1.87%). Conclusion This method is simple, efficient, accurate, and reproducible, and can be used for the determination of eight constituents in root of Swertia kingii. This will promote the comprehensive usage of this plant.

Effects of aqueous extract of Polygoni Multiflori Radix and its main constituents on expression of mRNA of CYP1A2, CYP2C9, and CYP2E1 in human liver L02 cells / 中草药

Objective To analyze the main chemical constituents and their contents in aqueous extract of Polygoni Multiflori Radix (PMR, root of Polygonum multiflorum), and to elucidate the effects of aqueous extract of PMR and its main constituents on the expression of the mRNA of CYP1A2, CYP2C9, and CYP2E1 in human liver L02 cells. Methods The main chemical constituents and their content in aqueous extract of PMR were determined by HPLC. The cytotoxicity of aqueous extract of PMR and its main constituents on L02 cells was determined by MTT assay. The mRNA expression of CYP1A2, CYP2C9, and CYP2E1 in L02 cells were detected by quantitative real-time PCR. Results There were four main well-separated chromatographic peaks standing for tetrahydroxy stilbene glucoside, emodin-8-O-β-D-glucoside, emodin and physcion in aqueous extract of PMR. The content of thesecomponents in aqueous extract of PMR was (1.14 ± 0.03)%, (0.106 9 ± 0.001 6)%, (0.010 8 ± 0.000 9)%, (0.003 55 ± 0.000 19)%, respectively. The cytotoxicity of aqueous extract of PMR and emodin on L02 cells at 24 h was dose-dependent, and the concentration of 50% inhibition was 7.290 mg/mL and 0.082 mmol/L respectively. Tetrahydroxy stilbene glucoside, emodin-8-O-β-D-glucoside and physcion did not show significant cytotoxicity on L02 cells in the experimental concentrations. Aqueous extract of PMR and emodin significantly inhibited the expression of mRNA of CYP1A2, CYP2C9, and CYP2E1 in L02 cells. Emodin-8-O-β-D-glucoside inhibited the expression of mRNA of CYP1A2 and CYP2C9. Tetrahydroxy stilbene glucoside inhibited the expression of mRNA of CYP1A2 but activated the expression of mRNA of CYP2C9. Physcion inhibited the expression of mRNA of CYP1A2 and CYP2C9 in a dose-dependent manner, but inhibited the expression of mRNA of CYP2E1 in low concentration and activitated the expression of mRNA of CYP2E1 in high concentration. Conclusion The inhibition of aqueous extract of PMR on the expression of mRNA of CYP1A2, CYP2C9, and CYP2E1 in L02 cells is the combined effect of all components in it. The main four components all inhibit the expression of mRNA of CYP1A2. The anthraquinone is the main component inhibiting the expression of mRNA of CYP2C9. The free anthraquinone is the main component inhibiting the expression of mRNA of CYP2E1.

Chemical constituents of whole plants of Patrinia villosa (Thunb.) Juss / 中国药学杂志

OBJECTIVE: To study the chemical constituents of Whole Plants of Patrinia villosa (Thunb.) Juss. METHODS: Compounds were isolated by a combination of various chromatographic techniques including column chromatography over macroporous resin, Sephadex LH-20 and reversed-phase HPLC. Their structures were elucidated by physiochemical properties and spectral analysis. RESULTS: Nine compounds were isolated and identified as (E, 4R)-4-hydroxy-4, 5, 5-trimethyl-3-(3-oxobut-1-enyl)cyclohex-2-enone (1), vomifoliol (2), cis-4-hydroxymellein (3), dehydrovomifoliol (4), 3R, 5S, 6R, 7E, 9S-3, 5, 6, 9-tetrahydroxy-7-megastigmane (5), loliolide (6), 4-methoxybenzyl alcohol (7), sphenanthin A (8), and urea (9). CONCLUSION: Compounds 1-7 are isolated fromPatrinia genus for the first time.

Analyzing crude/processed root of Polygonum multiflorum from different habitats by UPLC fingerprint and mode identification methods / 中国中药杂志

To establish a content determination method for 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside (TSG) of the crude/processed root of Polygonum multiflorum from different habitats in China and set up the fingerprint by using UPLC. Various samples were pretreated by macro-porous resin. Then UPLC analysis was performed on Waters ACQUITY UPLC@BEH C18 chromatographic column (2.1 mm×50 mm, 1.7 μm) at (25±5) ℃. A binary gradient elution system was composed of acetonitrile (phase A) and 0.5% acetic acid solution (phase B). Detection was performed at the wavelength of 254 nm, and the mobile flow rate was set at 0.3 mL•min⁻¹. Results showed that the yield of extraction of the 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside from root of P. multiflorum was all over 25.0% after macro-porous resin separation; an exclusive UPLC fingerprint method of the crude/processed root of P. multiflorum from different habitats was successfully set up and 17 chromatographic peaks were calibrated. Cluster analysis can not entirely distinguish the crude one from the processed one, while principal component analysis absolutely can. 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside is the composition that has largest differences in variable importance in projection (VIP) between crude and processed root of P. multiflorum. The separating method can gain high-purity 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside, and the determination method is simple, sensitive, reliable and can be used in fast identifying the crude/processed root of P. multiflorum or as a method for overall quality control of root of P. multiflorum.

Influence of metal ions on stability of 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside contained in Polygoni Multiflori Radix / 药学学报

Decoction is one of the most commonly used dosage forms of traditional Chinese medicine. The stability of chemical constituents in decoction is closely related to the clinical efficacy and safety. There were few reports about the influence of metal ions in the stability of chemical constituents in traditional Chinese medicine. However, there is no evidence that metal ions in decoction water need to be controlled. In this study, 2,3,5,4'-tetrahydroxy stilbene-2-O-β-D-glucoside (THSG), one of the main constituents in Polygoni Multiflori Radix was studied. Ordinary tap water, deionized water, and water containing different metal ions were used to investigate and compare the influence on THSG . The results showed that after storage in a dark place at the room temperature for 10 days, the degradation of THSG was 7% in deionized water, while undetectable in tap water. The content of THSG could be decreased by different kinds of metal ions, and the effect was concentration- dependent. Moreover, Fe3+ and Fe2+ showed the greatest influence at the same concentration; and our study has shown that THSG decreased more than 98% in Fe3+ and Fe2+ solutions at 500 ppm concentration. In the same time we found out p-hydroxybenzaldehyde (molecular weight: 122.036 7) and 2,3,5-trihydroxybenzaldehyde-2- O-glycoside (molecular weight: 316.079 4) were the main degradation products of THSG in tap water and water containing Cu2+, Ca2+, Zn2+, Mg2+ and Al3+. The product of THSG dimer with a water molecule was found in water containing Fe3+ and Fe2+. The above results showed that the metal ions in water could significantly influence the stability of THSG in water, indicating that the clinical efficacy and safety of decoction would be affected if the metal ions in water were not under control. It's suggested that deionized water should be used in the preparation of decoction containing Polygoni Multiflori Radix in the clinic to avoid degradation of THSG. Meanwhile, decoction prepared by tap water should be taken by patients in a short time. Our investigation provides important information and reference about the influence of metal ions on the stability of decoctions in other traditional Chinese medicine that have unstable groups such as hydroxyls and unsaturated bonds, etc.

Chemical constituents from Spiraea pubescens / 中草药

Objective: To investigate the chemical constituents from the ethanol extract of Spiraea pubescens. Methods: The compounds were isolated and purified by chromatography on silica gel, ODS, and preparative HPLC. Their structures were elucidated on the basis of chemical and spectroscopic methods, including MS, 1D, and 2D NMR spectral techniques. Results : Fourteen compounds were isolated and identified as β-sitosterol (1), tricosyl alcohol (2), stigmast-4-en-3-one (3), pentacosyl alcohol (4), stigmastanol (5), (+)-cyclo-olivil (6), (+)-africannal (7), (+)-lyoniresinol (8), 5-methoxy-(+)-isolariciresinol (9), (+)-isolariciresinol (10), (7R,8R)-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8-O-4'-neolignan (11), (6S,9R)-6-hydroxy-3-one-α-ionol-9-O-β-D-glucopyranoside (12), (+)-lyoniresinol 9-O-β-D-xylopyranoside (13), and (-)-lyoniresinol 9-O-β-D-xylopyranoside (14). Conclusion: Compounds 2-5 and 7-14 are isolated from the plants of Spiraea L. for the first time, and compounds 1 and 6 are obtained from this plant for the first time.

Chemical constituents from roots of Kadsura longipedunculata / 中草药

Objective: To study the chemical constituents from the roots of Kadsura longipedunculata. Methods: The constituents were isolated and purified by various chromatographic methods, and the structures were elucidated by spectroscopic analysis. Results: Sixteen compounds were isolated from the roots of K. longipedunculata and the structures were identified as pinobatol (1), leptolepisol B (2), 7S,8R-erythro-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8-O-4'-neolignan (3), 2,3-bis-(α-hydroxy-4-hydroxy-3-methoxybenzyl)-butane-1,4-diol (4), (7'S,8R,8'S)-4,4',9-trihydroxy-3,3',5-trimethoxy-9'-O-β-D-xylopyranosyl-2,7'-cyclo-lignan (5), aviculin (6), ent-isolariciresinol (7), lawsorosemarinol (8), (+)-anwulignan (9), isolariciresinol-2α-O-β-D-xyloside (10), procyanidin B3 (11), prodelphinidin B3 (12), (-)-gallocatechin (13), (+)-catechin (14), abscisic acid-β-D-glucopyranosyl ester (15), and (-)-oleuropeic acid 8-O-β-D-glucopyranoside (16). Conclusion: Compounds 1-8, 11-13, 15, and 16 are isolated from the plants of Kadsura Kaempf. ex Juss. for the first time.

A new triterpene natural product from stems and leaves of Panax ginseng / 中草药

Objective: To study the chemical constituents of saponins in the stems and leaves of Panax ginseng. Methods: The chemical constituents were isolated and purified by various chromatographic methods, and their structures were identified by NMR and MS data analysis. Results: Nine compounds were isolated and identified as 3β,6α,12β,25-tetrahydroxy-dammar-E-20(22)-ene-6-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside (1), sanchinoside B1 (2), 3β,6α,12β-dammar-E-20(22)-ene-3,6,12,25-tetraol (3), ginsenoside Rk3 (4), ginsenoside Rh4 (5), notoginsenoside T2 (6), 3β,6α,12β-dammar-20(21),24-diene-3,6,12-triol (7), ginsenoside Rk1 (8), and ginsenoside Rg5 (9). Conclusion: Compound 1 is a new natural product and the other eight compounds are all isolated from the stems and leaves of P. ginseng for the first time.