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New dammarane-type triterpenoid saponin, named 22( R )-notoginsenoside Ab1 ( 1 ), together with thirteen known dammarane-type triterpenoid saponins ( 2 - 14 ) was isolated from the EtOH extract of black ginseng and their structures were elucidated on the basis of one- and two-dimensional NMR (including 1 H-NMR, 13 C-NMR, HSQC, HMBC, ROESY) and calculated ECD. Among them, compounds 1-2 and 6 - 8 were isolated for the first time from ginseng and black ginseng. Besides, the absolute structure of 22( R )- and 22( S )- notoginsenoside Ab1 were distinguished by ECD for the first time.

To elucidate the medicinal nature of black ginseng (BG) by comparison of the effects of four Chinese herbs with different medicinal natures on the deficiency-heat syndrome rat model which was established by intragastric administration of traditional Chinese drugs with hot nature, the appearance indexes, biochemical indexes, and pathological sections of thyroid and stomach were examined. In addition, the seven short-chain fatty acids (SCFAs) in rat feces were also determined by headspace gas chromatography-mass spectrometry to reveal the action mechanism of the drugs with different natures. Results indicated that all the 4 drugs could exhibit similar actions in regulating the biochemical indexes of triiodothyronine (T3), thyroxine (T4), thyrotropin-releasing hormone (TRH), thyroid-stimulating hormone (TSH), and corticosterone (CORT) representing the hypothalamus-pituitary-thyroid (HPT) and hypothalamus-pituitary-adrenal (HPA) axes of the animal. However, cold-natured cortex phellodendri (HB) and ginseng leaves (GLs) showed stronger downregulation of the AChE activity of the nervous system. Red ginseng (RG) and BG tested exhibited stronger upregulation of the liver Na + -K + -ATPase activity. Principal component analysis (PCA) showed that GLs are similar to those of HB which belongs to the cold-nature drug, whereas BG showed closer to RG which attributes to a warm-nature drug. Thus, BG could be ascribed to a warm-nature drug. Further research disclosed that RG and BG mainly regulated the acetic acid and GL and HB primarily modulated the isovaleric acid and hexanoic acid in rat feces, which could be the features of drugs with warm or cold nature on the regulation of SCFAs in rats. It is for the first time that the medicinal nature of BG and its effect on the SCFAs were examined., Competing Interests: The authors declare that there are no conflicts of interest regarding the publication of this paper., (Copyright © 2022 Mei-Yu Wan et al.)

Hydroxysafflor yellow A (HSYA) from safflower (Carthamus tinctorius L.) possesses several medicinal properties. However, it is unknown whether HSYA is effective in the treatment of rheumatoid arthritis (RA). Hence, we investigated the effects of HSYA on the inflammation and synovial damage in rats with collagen-induced arthritis (CIA) by subjecting them to treatment with different doses of HSYA. Our results revealed that HSYA could significantly reduce paw swelling, pathological manifestations, and serum cytokine levels in rats with CIA. The HSYA-treated groups showed increased antioxidant enzyme activity in the serum and decreased expression of inflammatory mediators in the synovial tissues. Furthermore, HSYA treatment inhibited extracellular signal-regulated kinase (ERK) signalling pathway activation. Notably, the highest dose of HSYA (20 mg/kg) exhibited the best effects against RA symptoms. Therefore, our findings suggest that HSYA alleviates the inflammatory response and synovial damage in rats with CIA by inhibiting the ERK signalling pathway., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2021 Elsevier Inc. All rights reserved.)

Objective: The research indicated that the nature of Chinese medicine is mainly related to body's substance and energy metabolism. The purpose of the study is to elucidate the substance basis for warm nature of Poria cocos (called Fuling (FL) in Chinese)., Methods: In terms of the effects of its separated fractions on the substance and energy metabolism in rat models of cold-deficiency with Aconiti Lateralis Radix Praeparata (called Fuzi (FZ) in Chinese), with hot nature, as reference drug. Biochemical indexes in the material metabolism, energy metabolism, endocrine system, nervous system and nucleotide system were determined, then analyzed by additive, cluster and principal component analysis (PCA)., Results: The medicinal natures of oligosaccharides and amino acids fractions were attributable to plain and crude polysaccharides, volatile oils and triterpenoids fractions were attributable to mild warm ., Conclusion: The nature of FL was regarded as mild warm based on the old records of Chinese medicine and fractions of crude polysaccharides, volatile oils and triterpenoids might be the main substance basis for the warm nature of FL. It is the first time that substance basis of FL was elucidated from view point of medicinal nature., Competing Interests: The authors declare no conflict of interests., (© 2020 Tianjin Press of Chinese Herbal Medicines. Published by ELSEVIER B.V.)

Tagetespatula L. is a widely cultivated herbal medicinal plant in China and other countries. In this study, two new 2, 3-dihydrobenzofuran glucosides ( 1 , 2 ) and fourteen known metabolites ( 3 - 16 ) were isolated from the stems and leaves of T. patula (SLT). The chemical structures of the isolated compounds were characterized comprehensively based on one- and two-dimensional NMR spectroscopy and high resolution mass spectrometry. Absolute configurations of compounds 1 and 2 were determined by ECD calculations. Compounds 1 and 2 exhibited moderate in vitro inhibitory activities against human gastric cancer cell lines (AGS) with IC 50 values of 41.20 μmol/L and 30.43 μmol/L, respectively. The fingerprint profiles of stems and leaves of T. patula with three color types of flowers (Janie Yellow Bright, Jinmen Orange, Shouyao Red and Yellow color) were established by high-performance liquid chromatography (HPLC). Ten different batches of stems and leaves were examined as follow: Shouyao Red and Yellow color (1, 2, 3), Janie Yellow Bright (4, 5, 6, 7) and Jinmen Orange (8, 9, 10). Twenty-two common peaks were identified with similarity values ranging from 0.910 to 0.977. Meanwhile, the average peak area of SLT in the three types of flowers was different and it was the highest in Janie Yellow Bright.

Recent studies have revealed that the property of drug is mainly associated with the body's substance and energy metabolism. The present study aimed to evaluate the drug property of Poria, called Fuling (FL) in traditional Chinese medicine (TCM), in terms of its effects on the substance and energy metabolism in rat models of cold-deficiency and heat-deficiency syndromes, compared with Aconiti Lateralis Radix Praeparaia, called Fuzi (FZ) in TCM, with hot property, and Anemarrhenae Rhizoma, called Zhimu (ZM) in TCM, with cold property, as reference drugs, respectively. The appearance score, toe and rectal temperatures of the animals treated were assessed at different time points. Several indices in vivo correlated with substance and energy metabolism (glucokinas, phosphoglycerate kinase, cytochrome c reductase, cytochrome c oxydase, and Na + -K + -ATPase), endocrine system (triiodothyronine, thyroxine, and 17-hydroxycorticosteroid), nervous system (acetylcholin esterase), and cyclic nucleotide system were determined. The changes in appearance score and indices in vivo suggested the successful establishment of cold-deficiency and heat-deficiency syndrome models. FZ reversed the decreased levels of indices (substance and energy metabolism and endocrine system) and alleviated the syndrome of cold-deficiency model, and ZM showed obviously therapeutic effect on heat-deficiency syndrome (appearance score, substance and energy metabolism, and endocrine system). FL could alleviate cold-deficiency syndrome and raise the decreased levels of glucokinas, phosphoglycerate kinase, cytochrome c reductase and triiodothyronine in cold-deficiency model, but had no significant effect on heat-deficiency syndrome. Drug property of FL was inferred as trending to "flat and warm", which still need further study. It was advisable to adopt both cold-deficiency and heat-deficiency models to study the drugs with "flat" property., (Copyright © 2018 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

The chemical constituents of 95% EtOH extract of yacon leaves were separated to yield two new sesquiterpene lactones, together with three known compounds. The two new compounds were characterized to be 8β-angeloyloxy-13-methoxyl-11, 13-dihydromelampolid-14-oic acid methyl ester (1) and 8β-(3-methylbut-2-enoyl) oxy-13-methoxyl-11, 13-dihydromelampolid-14-oic acid methyl ester (2) on the basis of NMR spectra, HR-MS and other spectroscopic methods. The cytotoxicity of compounds 1-5 were evaluated on human hepatoma cell Bel-7402 and all the compounds showed moderate cytotoxicity.

Arctigenin is a phenylpropanoid dibenzylbutyrolactone lignan compound possessing antitumor, anti-inflammatory, anti-influenza, antioxidant, antibacterial, and hypoglycaemic activities. Our previous study demonstrated that arctigenin exerts neuroprotective effects both in vitro and in vivo in a Parkinson's disease model. However, the exact mechanism through which arctigenin improves amyloid beta-induced memory impairment by inhibiting the production of the hyperphosphorylated tau protein is unknown. Amyloid β 1-42 was slowly administered via the intracerebroventricular route in a volume of 3 µL (≈ 410 pmmol/mouse) to mice. The mice were administered arctigenin (10, 40, or 150 mg/kg) or vehicle starting from the second day after amyloid β 1-42 injection to the end of the experiment. Behavioural tests were performed from days 9 to 15. On day 16 after the intracerebroventricular administration of amyloid β 1-42 , the mice were sacrificed for biochemical analysis. Arctigenin (10-150 mg/kg) significantly attenuated the impairment of spontaneous alternation behaviours in the Y-maze task, decreased the escape latency in the Morris water maze test, and increased the swimming times and swimming distances to the platform located in the probe test. Arctigenin attenuated the level of phosphorylated tau at the Thr-181, Thr-231, and Ser-404 sites in the hippocampus, and increased the phosphorylation levels of phosphatidylinositol-3-kinase, threonine/serine protein kinase B, and glycogen synthase kinase-3 β . Arctigenin effectively provides protection against learning and memory deficits and in inhibits hyperphosphorylated tau protein expression in the hippocampus. The possible mechanism may occur via the phosphatidylinositol-3-kinase/protein kinase B-dependent glycogen synthase kinase-3 β signalling pathway., (Georg Thieme Verlag KG Stuttgart · New York.)

The chemical constituents of 60% EtOH extract of yacon leaves were separated to yield a new compound, together with four known compounds, which were isolated for the first time from yacon. The new compound was characterised and named as chlorodalin (1) on the basis of NMR (1D and 2D), HR-MS and other spectral methods. The cytotoxic activities of 1-5 were evaluated on two human tumour cell lines and the new compound showed significant cytotoxic activity.

In the present study, two new compounds, together with six known compounds, were isolated from rhizome of Atractylodes macrocephala Koidz by a series of silica gel, ODS column chromatography, and preparative HPLC. Their structures were characterized as atractylenolide II (1), atractylenolide I (2), biepiasterolid (3), isoatractylenolide I (4), atractylenolide III (5), 3β-acetoxyl atractylenolide I (6), (4E,6E,12E)-tetradeca-4,6,12-triene-8,10-diyne-13,14-triol (7), (3S,4E,6E,12E)-1-acetoxy-tetradeca-4,6,12-triene-8,10-diyne-3,14-diol (8) on the basis of 1D, 2D NMR, and circular dichroism analyses. Among them, compounds 6 and 8 were novel compounds. In addition, their neuroprotective activity against MPP + -induced SH-SY5Y cells was evaluated by MTT colorimetry. The results showed that all these compounds have definite protective effect on MPP + -induced SH-SY5Y cells.

Ethnopharmacological Relevance: Huanglian Jiedu Decoction (HJD), the classical recipe for relieving fever and toxicity, has been used for treating sepsis in China for sixteen years. However, the effective components of HJD have not been elucidated until now. Therefore, there is a need to elucidate the effective components of HJD against sepsis on animal models induced by endotoxin (LPS). The affinity force of the effective components of HJD with lipid A was evaluated by a biosensor., Materials and Methods: Lipid A is regarded as the bioactive center of LPS and is always used as a drug target. In order to obtain the effective components of HJD against sepsis, seven fractions from HJD were tested by a biosensor method for assessing the affinity for lipid A. After further separation, the components were isolated from high lipid A-binding fractions and their affinities to lipid A were assessed with the aid of a biosensor. Their activities were then assayed by an in vivo experiment administered through a tail vein injection. The levels of LPS, TNF-α, and IL-6 from the blood were found and pathology experiments were performed., Results: Three out of the seven fractions exhibited high lipid A-binding affinities. Berberine, baicalin and geniposide were obtained from the three high lipid A-binding fractions. The animal experiments indicated that the levels of LPS, TNF-α and IL-6 in the medicated treatment groups were much lower than that of the model group ((**)P<0.01). The medicated treatment groups exhibited stronger protective activities on varying organs in the animal model., Conclusions: Berberine, baicalin and geniposide could neutralize LPS by binding with lipid A and then reduce the release of IL-6 and TNF-α induced by LPS. Furthermore, berberine, baicalin and geniposide exhibited protective activities on varying organs compared to the animal model established by the LPS-induced. These results validate that the components from HJD neutralized LPS and then depressed the release of IL-6 and TNF-α induced by LPS. This gives further evidence that HJD would be a suitable treatment for sepsis and protecting vital organs., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

Because of the rapid action and high bioavailability, traditional Chinese medicine injections (TCMIs) had been widely used in clinical critical field. In recent years, with the increasing reports of clinical adverse reaction, more and more attention was paid to them, and acute allergic reaction was the main adverse reaction. Acute allergic reaction included type-I anaphylaxis reaction and anaphylactoid reaction, the latter had been found in a variety of TCMIs and accounted for 77% of adverse reaction. But the mechanism of anaphylactoid reaction was not completely understood, the standard animal model for TCMIs was not established, and the technical guidance for anaphylactoid reaction was not formulated. Thus the three aspects included mechanism, evaluation index and evaluation methods of TCMIs for anaphylactoid were reviewed. Five ways including direct stimulating pathway, complement pathway, coagulation pathway, kallikrein-kinin pathway and acute allergic pathway were the main mechanism of anaphylactoid reaction; whole animal model and cell model were the main evaluation methods; the occurrence index and effect index were reviewed for the evaluation index analysis.

Four new iridoids (1, 2, 12, and 13), together with nine known iridoids (3-11), were isolated from the male flowers of Eucommia ulmoides Oliver and were characterized as 3β-methoxyartselawnin C (1), 6β-hydroxyl-1β,3β-dimethoxyartsclaenin III (2), 3,4-dihydro-3β-ethoxyasperuloside (12) and 3,4-dihydro-3β-ethoxydesacetylasperuloside (13) by extensive analyses of their 1D and 2D NMR spectroscopy and mass spectra. All of the isolated compounds were assayed for the promoting proliferation of skin fibroblasts cell (ESF-1) and compounds 4 and 7 (5 μM) significantly stimulated the proliferation of ESF-1 cells.

Polysaccharides from Baizhu were separated by preparative hydrophilic interaction liquid chromatography on an XAmide column and its components were characterised as inulin-type polysaccharides with structures of α-D-glucopyranosyl-[-(1 → 2) -β-D-fructofuranosyl-](n -1)-(1 → 2) -β-D-fructofuranoside (n = 3-20) by a combinatory application of electrospray-ionisation mass spectrometry, nuclear magnetic resonance and IR, as well as the chemical analysis of monosaccharide composition. In addition, the contents of nystose and 1F-fructofranosylnystose in the crude and purified Baizhu polysaccharides were determined to be 5.81%, 4.92% and 0.70%, 0.84% (w/w), respectively. In addition, MTT assay indicated that the Baizhu polysaccharides could effectively promote spleen lymphocyte transformation for the enhancement of organism immunity. It is for the first time that inulin-type polysaccharides were discovered in Baizhu and its immuno-enhancing activity was reported, which is a vigorous evidence to explain the efficacy of Baizhu.

Nine triterpenes compounds were isolated from the male flowers of Eucommia ulmoides by recrystallization and chromatographic techniques over silica gel, Sephadex LH-20, and RP-18 gel. Their chemical structures were identified on the basis of spectral analysis and as 3-oxo-12-en-ursane-28-O-α-L-arabinofuranosyl (1 --> 6) -β-D-glucopyranoside (1), 2α, 3β-dihydroxyurs-12-en-28-oic acid(28 --> 1) -β-D-glucopyranosyl ester (2), ursolic acid (3), α-amyrin (4), uvaol (5), ursolic acid acetate (6), 3-O-acetate oleanoic acid (7), betulinic acid (8), and betulinol (9). Compound 1 was a new compound, and compounds 2, 4-7 were isolated from the Eucommiu genus for the first time. Cytotoxic activity was tested for all the compounds against K562 and HepG2 cells. The results showed that only compound 3, exhibited cytotoxic activity.

Six dammarane-type saponins were extracted from steamed Panax notoginseng. Their chemical structures were identified spectroscopically as ginsenosides Rh1 (1), Rg1 (2), 20 (S)-Rg3 (3), 20 (R)-Rg3 (4), Rb3 (5), and Rb1 (6). Compounds (0.1-10 μM) were tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 (5) showed the most significant activity with an IC50 of 8.2 μM. This compound also inhibited the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells had been treated with TNF-α (10 ng/mL).

With the combined applications of steam distillation, water extraction and alcohol precipitation, liquid-liquid extraction and column chromatography over macroporous resin, a splitted-fractions method of the chemical constituents of Poria cocos was established. The unoverlapping property of the fractions of P. cocos was qualitatively analysed by using principal component analysis and cluster analysis. With angle cosine, squared euclidean distance and the overlapping analysis of peak area of crude herbs, the unoverlapping property of the fractions of P. cocos was half-quantitatively analysed. The chemical components of P. cocos was divided into the fractions of polysaccharide, petroleum ether, ethyl acetate, alcohol eluate from macroporous resin and water eluate from macroporous resin. Non similarity degree among each chemical fraction was above 80% and main chemical components were identified. The established method for splitting fractions of P. cocos has good stability and repeatability and all chemical components in P. cocos could be completely divided into six fractions. It is the first time that the author half-quantitatively analyse the unoverlapping property of the chemical fractions of P. cocos.

Background: Ginseng cultivated under mountainous forest, called "Lin-Xia-Shan-Shen" (LXSS) in China's Pharmacopoeia. In recent years, it has been quickly propelled to plant at a large scale., Objective: To study the profiles of ginsenosides and carbohydrate profiles of LXSS., Materials and Methods: The contents of ginsenosides and carbohydrates, such as soluble sugar, polysaccharide, pectin, and starch in LXSS, were determined. All the above components were profiled, and the correlations between them were analyzed., Results: The results indicated that the contents of total ginsenoside, protopanaxadiol, protopanaxatriol, Rg1, Re, Rb1, Rc, Rb2, Rd, starch, and pectin were negatively correlated with the growing years within 17 years. Among them, the content of starch was positively correlated with that of pectin. The total ginsenosides was positively correlated with starch and pectin, which cannot be found in garden ginseng, maybe resulting of fertilizer and other manual intervention in process of cultivation of garden ginseng., Discussion and Conclusions: The accumulation of ginsenosides and carbohydrate, especially starch and pectin, was different in garden ginseng and LXSS. This research may provide the scientific basis for germplasm evaluation, the cultivation and utilization of ginseng cultivated under mountainous forest.

Ethnopharmacological Relevance: Cuscuta chinensis (C. chinensis) is a well-known traditional Chinese herb that has been used to treat heart disease, diabetes, liver injury, cancer, and aging., Materials and Methods: Murine osteoblastic MC3T3-E1 cells were treated with various concentrations of C. chinensis water extraction at different time intervals. The antioxidant effect of C. chinensis on MC3T3-E1 cells was evaluated using MTT and TUNEL assays. The effect of C. chinensis on cell cycle was analyzed by flow cytometry with propidium iodide. Lipid peroxidation was measured by the HPLC method. The cellular redox status was determined from the reduced glutathione to oxidized glutathione ratio (GSH/GSSG) and the enzymes involved in glutathione metabolism, including glutathione reductase (GR), Glutathione S-transferase (GST), and Glucose-6-phosphate dehydrogenase (G6PD). The changes in relative mitochondrial transmembrane potential (ΔΨm) in the MC3T3-E1 cells were analyzed with rhodamine 123 staining. Western blot analysis was used to evaluate the levels of cytochrome c (cyto c), Bax, Bcl-2, caspase 3, Sirt3, and IDH2 expressions., Results: The C. chinensis water extraction protects tertiary butyl hydroperoxide (TBHP)-treated MC3T3-E1 cells from death in a dose-dependent manner. C. chinensis treatment significantly inhibited the reactive oxygen species (ROS) generation, malondialdehyde (MDA) production, and increased the activity of superoxide dismutase (SOD), GR, GST, and G6PD. The release of cyto c from mitochondria was reduced by C. chinensis, which increased the expression of antiapoptotic IDH2, Sirt3, and Bcl-2 and decreased the expression of Bax, cyto c, and caspase 3., Conclusions: C. chinensis modulated the oxidative stress-induced apoptosis in MC3T3-E1 cells, probably due to its antioxidant activity and functioning via mitochondria-dependent pathways., (Copyright © 2013 Elsevier Ireland Ltd. All rights reserved.)

Ginseng cultivated and grown naturally under mountainous forest is formally called "Lin-Xia-Shan-Shen" (LXSS) and grown in manual condition is called garden ginseng (GG) according to Chinese pharmacopoeia (2010 edition). Usually the growing condition of LXSS is similar to wild ginseng and mostly used in Chinese folks in ancient times. The antioxidant properties of LXSS with different growing years were evaluated by their inhibitions of thiobarbituric acid-reactive substance (TBA-RS) formation in liver homogenate and 2, 2-diphenyl-1-picrylhydrazyl (DPPH)-radical scavenging activity comparing with those of GG. The inhibitions of different polar extracts (n-butanol and water) of LXSS and GG on TBA-RS formation were also evaluated. The results showed that the antioxidant effects of LXSS were higher than those of GG and the TBARS formation inhibition of LXSS with longer growing years were stronger than those with shorter growing years, while the DPPH-radical scavenging activity of LXSS did not show significant difference with the change of the growing year. The results indicated that the inhibitory effect of TBA-RS formation and the DPPH-radical scavenging of LXSS were correlated with the contents of ginsenosides. In adddition, the starch contents of LXSS and GG were determined by micro-amount method with spectrophotometer. It showed that the starch content in GG was higher than that of LXSS whose starch decreased gradually with the growing year.

Aim: To investigate the chemical constituents from the leaves of Broussonetia papyrifera., Methods: The chemical constituents were isolated and purified by macroporous adsorptive resin D101, silica gel, and ODS column chromatography and preparative HPLC. Their structures were elucidated on the basis of 1D and 2D NMR analyses. In addition, their cytotoxic activity against human hepatoma carcinoma cells (HepG-2) were evaluated by the MTT method. Furthermore, RP-HPLC and colorimetric methods were used for the analysis of cosmosiin and total flavonoids., Results: A new lignan, together with five known compounds were obtained, and their structures were characterized as (+)-pinoresinol-4'-O-β-D-glucopyranosyl-4″-O-β-D-apiofuranoside (1), cosmosiin (2), luteolin-7-O-β-D-glucopyranoside (3), liriodendrin (4), 3, 5, 4'-trihydroxy-bibenzyl-3-O-β-D-glucoside (5), and apigenin-6-C-β-D-glucopyranside (6). Furthermore, RP-HPLC and colorimetric methods were established for the analysis of cosmosiin and total flavonoids., Conclusion: Compound 1 was a new lignan, and compounds 5 and 6 were isolated for the first time from the title plant. Compounds 1, 4 and 6 showed definite activities against HepG-2, while the other compounds didn't show inhibitory effects. The optimal harvest time of B. papyrifera (L.) Vent. is September., (Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Arctiin, an important lignan compound in Fructus Arctii, has been reported to possess various kinds of bioactivities. Previous studies on the pharmacokinetic of arctiin after oral administration showed that it had a rapid absorption phase followed by a sharp but lasting disappearance. To gain deep insight into the action mechanism of arctiin, the excretion and metabolism of arctiin in vivo should be further studied. In this paper, three metabolites were isolated and identified in rat feces as (-)-enterolactone (M-1), (-)-arctigenin (M-2) and [(2R,3R)-2-(3'-hydroxybenzyl)-3-(3″,4″-dimethoxybenzyl)-butyrolactone] (M-3). Based on the structures of three metabolites, possible metabolic pathways of arctiin in rats are proposed. At the same time, the cumulative excretion rate of arctiin and its metabolites in rat urine and feces were determined, indicating that arctiin was excreted 19.84% in urine and 1.80% in feces, respectively, enterolactone, the most main metabolite, was excreted 35.80% in feces. These results provide very important information for understanding the metabolism and excretion of arctiin in vivo and speculating its action mechanism, they can provide useful information and reference for further metabolic investigations on arctiin in humans., (Copyright © 2013 Elsevier B.V. All rights reserved.)

Objective: To determine the plasma protein binding rate of arctiin and arctigenin., Method: The ultrafiltration combined with HPLC was employed to determine the plasma protein binding rate of arctiin and arctigenin as well as rat plasma and healthy human plasma proteins., Result: The plasma protein binding rate of arctiin with rat plasma at the concentrations of 64. 29, 32.14, 16.07 mg x L(-1) were (71.2 +/- 2.0)%, (73.4 +/- 0.61)%, (78.2 +/- 1.9)%, respectively; while the plasma protein binding rate of arctiin with healthy human plasma at the above concentrations were (64.8 +/- 3.1)%, (64.5 +/- 2.5)%, (77.5 +/- 1.7)%, respectively. The plasma protein binding rate of arctigenin with rat plasma at the concentrations of 77.42, 38.71, 19.36 mg x L(-1) were (96.7 +/- 0.41)%, (96.8 +/- 1.6)%, (97.3 +/- 0.46)%, respectively; while the plasma protein binding rate of arctigenin with normal human plasma at the above concentrations were (94.7 +/- 3.1)%, (96.8 +/- 1.6)%, (97.9 +/- 1.3)%, respectively., Conclusion: The binding rate of arctiin with rat plasma protein was moderate, which is slightly higher than the binding rate of arctiin with healthy human plasma protein. The plasma protein binding rates of arctigenin with both rat plasma and healthy human plasma are very high.

A high-performance liquid chromatography (HPLC) technique was developed for the determination of arctigenin in plasma and various organs of rats after the oral administration of 30, 50 and 70 mgkg(-1) of arctigenin to the Sprague-Dawley rats. Results showed that the validated HPLC method was simple, fast, reproducible and suitable to the determination of arctigenin in rat plasma and organ tissue and one-compartmental model with zero-order absorption process can well describe the changes of arctigenin concentration in the plasma. The concentration of compound was highest in the spleen, less in the liver and the least in the lung.

(-)-Arctigenin, an important active constituent of the traditional Chinese herb Fructus Arctii, was found to exhibit various bioactivities, so it can be used as a good lead compound for further structure modification in order to find a safer and more potent medicine. (-)-Arctigenin derivatives 1-5 of (-)-arctingen were obtained by modifying with ammonolysis at the lactone ring and sulphonylation at C (6') and C (6″) and O-demethylation at CH3O-C (3'), CH3O-C (3″) and CH3O-C (4″), and their anticancer bioactivities were examined.

Two new oleanane-type pentacyclic triterpenoid saponins were isolated from the husks of Xanthoceras sorbifolia Bunge and their structures were elucidated as 3-O-β-D-glucopyranosyl (1 → 6)-β-D-glucopyranosyl-28-O-α-L-rhamnopyranosyl (1 → 2) [β-D-glucopyranosyl (1 → 6)] β-D-glucopyranosyl-21β,22α-dihydroxyl-olean-12,15-diene and 3-O-β-D-glucopyranosyl (1 → 2)-β-D-glucopyranosyl-28-O-α-L-rhamnopyranosyl (1 → 2) [β-D-glucopyranosyl (1 → 6)] β-D-glucopyranosy-21β,22α-dihydroxyl-olean-12-ene. Meanwhile, the cytotoxic activities of these two compounds were tested on human gastric cancer cell (SGC-7901) and hepatoma carcinoma cell (HepG-2).

The pharmacokinetic profile of arctiin, the major active lignan in fruits of Arctium lappa L., was investigated. Its main meta"bolite arctigenin was identified by an LC-MS method, and an HPLC-UV technique was developed for the simultaneous quantification of the metabolite and arctiin in plasma and organs. Chromatographic separation was performed on an Agilent™ C₁₈ HPLC column with acetonitrile and water by linear gradient elution. Arctiin and arctigenin were identified on-line by LC-MS. The pharmacokinetics and tissue distribution of arctiin and arctigenin were determined for the first time by using a simple, selective, and accurate HPLC method. The AUC0-t values of arctigenin were larger compared with arctiin after oral administration of arctiin. The concentration of the metabolite was significantly higher than the concentration of arctiin in the stomach and small intestine in rats after oral administration of arctiin, indicating that the stomach and small intestine were the major organs of arctiin metabolism. These findings could provide support for the clinical studies conducted with Fructus Arctii., (Georg Thieme Verlag KG Stuttgart · New York.)

Two new triterpenoid saponins (1, 2) and a known saponin (3) were isolated from the husks of Xanthoceras sorbifolia Bunge., and their structures were elucidated as 3-O-β-D-glucopyranosyl(1 → 6)-[angeloyl(1 → 2)]-β-D-glucopyranosyl-28-O-α-L-rhamnopyranosyl(1 → 2)-[β-D-glucopyranosyl(1 → 6)]-β-D-glucopyranosyl-21β,22α-dihydroxyl-olean-12-ene (1), 3-O-β-D-glucopyranosyl-28-O-[β-D-glucopyranosyl(1 → 2)]-β-D-glucopyranosyl-21β,22α-dihydroxyl-olean-12-ene (2), and 3-O-β-D-glucopyranosyl-28-O-[α-L-rhamnopyranosyl(1 → 2)]-β-D-glucopyranosyl-21β,22α-dihydroxyl-olean-12-ene (3), on the basis of the spectral analysis of NMR and chemical methods. Cytotoxic assay indicated that none of them showed obvious inhibitory effect on the proliferation of two human tumor cell lines.

Two new amide alkaloids were isolated from the alkaloidal fraction of Datura metel L. Their structures were elucidated as (E)-methyl 4-(3-(4-hydroxyphenyl)-N-methylacrylamido) butanoate and 6,7-dimethyl-1-D-ribityl-quinoxaline-2,3(1H,4H)-dione-5'-O-β-D-glucopyranoside on the basis of spectroscopic methods including HRESIMS, 1D and 2D NMR. Tropane alkaloids have for a long time been considered as characteristic ingredients of D. metel. However, the presence of amide alkaloids in D. metel was reported for the first time in this study., (Crown Copyright © 2010. Published by Elsevier B.V. All rights reserved.)

In our search for bioactive anti-psoriasis compounds from the flower of Datura metel L, we isolated four new withanolide glucosides, baimantuoluosides D, E, F and G (1-4). The structures of the new compounds are (5alpha,6alpha,7beta,22R)-5,6,7,27-tetrahydroxy-1-oxowitha-2,24-dien-27-O-beta-D-glucopyranoside (1), (5alpha,6beta,7alpha,22R)-5,6,7,27-tetrahydroxy-1-oxowitha-2,24-dien-27-O-beta-D-glucopyranoside (2), (5alpha,6beta,7alpha,12beta,22R)-5,6,7,12,27-pentahydroxy-1-oxowitha-2,24-dien-27-O-beta-D-glucopyranoside (3), and (5alpha,6beta,22R)-5,6,27-trihydroxy-1-oxowitha-2,24-dien-27-O-beta-D-glucopyranoside (4) on the basis of chemical and physicochemical evidence.

Two new lupane type saponins, along with one known saponin were isolated from leaves of Oplopanax horridus (Devil's Club). The structures of the two new compounds were elucidated as 3alpha-hydroxy-lup-20(29)-ene-23, 28-dioic acid-3-O-beta-D-glucopyranoside (2) and 24-nor-3-oxo-lup-20(29)-en-28-oic acid-28-O-alpha-L-rhamnopyranosyl(1''' --> 4")-beta-D-glucopyranosyl(1" --> 6')-beta-D-glucopyranoside (3) on the basis of spectroscopic analysis and chemical evidence. The known compound was identified as 3alpha-hydroxy-lup-20(29)-ene-23, 28-dioic acid (1) by comparison of its spectral data with those reported. Compound 1 was isolated for the first time from the title plant.

Objective: To compare the pharmacokinetics about Ermiao capsules and ermiao pellet, and observe the changes in plasma concentration with different formulations in animals from the perspective of pharmacokinetics., Methods: After the rabbits were administered with Ermiao capsules and ermiao pellet through ig. HPLC was used to determine berberine in blood plasma at different times, DAS 2.0 procedure was used to process concentration-time data., Results: In the rabbit plasma samples,the linear range of berberine was 0.00427-0.427 microg/mL, it has a high extract recovery rate,and day-day precision RSD was less than 10%. The whole blood concentration-time course of berberine in Ermiao capsules was fitted to be a two-compartment model, and berberine in Ermiao pellet was fitted to be a one-compartment model., Conclusion: This essay establishes a method for determine berberine in rabbit plasma, provided the pharma cokinetic parameters for rational administration of ermiao capsules, and also provided the pharmacokinetic study method of compounds.

The extract from the leaves of Smallantus sonchifolius (yacon) was found to show potent anti-diabetic activity. Two new diterpenes, named ent-kaurane-3beta,16beta,17, 19-tetrol (1) and ent-kaurane-16beta,17,18,19-tetrol (2), were isolated from the extract, together with six known compounds. The structures of the new compounds were determined on the basis of chemical and physicochemical evidence.

Cordyceps militaris (L.) Link is an entomopathogenic fungus parasitic to Lepidoptera larvae, and is widely used as a folk tonic or invigorant for longevity in China. Although C. militaris has been used in traditional Chinese medicine for millennia, there is still a lack convincing evidence for its anti-aging activities. This study was performed to investigate the effects of polysaccharides from cultivated fruiting bodies of C. militaris (CMP) on mitochondrial injury, antioxidation and anti-aging activity. Fruiting bodies of C. militaris were cultivated artificially under optimized conditions. The spectrophotometric method was used to measure thiobarbituric acid reactive substances (TBARS), mitochondrial swelling, and activities of scavenging superoxide anions in vitro. D-galactose (100 mg/kg/day) was injected subcutaneously into back of the neck of mice for 7 weeks to induce an aging model. The effects of CMP on the activities of catalase (CAT), surperoxide dismutase (SOD), glutathione peroxidase (GPx) and anti-hydroxyl radicals were assayed in vivo using commercial monitoring kits. The results showed that CMP could inhibit mitochondrial injury and swelling induced by Fe²(+)-L-Cysteine in a concentration- dependent manner and it also had a significant superoxide anion scavenging effect. Moreover, the activities of CAT, SOD, GPx and anti-hydroxyl radicals in mice liver were increased significantly by CMP. These results indicate that CMP protects mitochondria by scavenging reactive oxygen species (ROS), inhibiting mitochondrial swelling, and increasing the activities of antioxidases. Therefore, CMP may have pharmaceutical values for mitochondrial protection and anti-aging. CMP was the major bioactive component in C. militaris.

The inhibitory effect of smallanthaditerpenic acids A, B, C and D previously isolated from leaves of Smallanthus sonchifolius (yacon) on alpha-glucosidase were examined and their IC50 were determined to be 0.48 mg/mL, 0.59 mg/mL, 1.00 mg/mL, and 1.17 mg/mL respectively. In addition, a rapid, reliable RP-HPLC method for the analysis of chlorogenic acid, caffeic acid, and smallanthaditerpenic acids A and C in yacon leaves was established, and the variation in their contents in leaves from plants cultivated in different places and collected at different times of the year were compared. The established analytical method for determining smallanthaditerpenic acids A and C, chlorogenic acid and caffeic acid presented good results and could be used as a method for the quality control of S. sonchifolius leaves.

Two new saponins were isolated from husks of Xanthoceras sorbifolia Bunge and their structures were elucidated as 3-O-[beta-D-galactopyranosyl(1-->2)]-alpha-L-arabinofuranosyl(1-->3)-beta-D-methyl glucuronic acid-21-O-(3,4-diangeloyl)-alpha-L-rhamnose-3beta, 16alpha, 21beta, 22alpha, 28beta-pentahydroxyl-22-acetoxy-olean-12-ene(1) and 3-O-[beta-D-galactopyranosyl(1-->2)]-alpha-L-arabinofuranosyl(1-->3)-beta-D-methyl glucuronic acid-21,22-O-diangeloyl-3beta,15alpha,16alpha,21beta,22alpha,28beta-hexahydroxyl-olean-12-ene(2) on the basis of 1D and 2D NMR (including (1)H, (13)C-NMR, (1)H-(1)H COSY, HSQC, HMBC and DEPT), ESI-MS spectrometry and chemical methods., (2009 John Wiley & Sons, Ltd.)

Two new phenolic glycosides were isolated from the seeds of Cucurbita moschata. Their structures were elucidated as (2-hydroxy)phenylcarbinyl 5-O-benzoyl-beta-D-apiofuranosyl(1-->2)-beta-D-glucopyranoside (1) and 4-beta-D-(glucopyranosyl hydroxymethyl)phenyl 5-O-benzoyl-beta-D-apiofuranosyl(1-->2)-beta-D-glucopyranoside (2) on the basis of spectroscopic analysis and chemical evidence.

A new compound, named quinquefoloside-L(c) (1), together with nine known compounds, was isolated from leaves of Panax quinquefolium, and its structure was elucidated as 3beta,12beta, 20S-trihydroxy-25-methoxydammar-23-ene 3-O-beta-D-glucopyranosyl (1-->2)beta-D-glucopyranosyl-20-O-beta-D-xylopyanosyl (1-->6) beta-D-glucopyranoside (1), on the basis of MS, 1D-and 2D-NMR experiments as well as by chemical degradation. The cytotoxicity of these compounds against human breast cancer MCF-7 cell line was also tested by MTT method.

A new phenolic glycoside and three known compounds were isolated from the seeds of Cucurbita moschata. The structures of the new compound was elucidated as phenylcarbinyl 5-O-(4-hydroxy)benzoyl-beta-D-apiofuranosyl (1-->2)-beta-D-glucopyranoside on the basis of spectroscopic analysis and chemical evidence. Three known compounds were identified as 1-O-benzyl[5-O-benzoyl-beta-D-apiofuranosyl(1-->2)]-beta-D-glucopyranoside 2, cucurbitosides C 3 and A 4, by comparison of the spectral data with reported data. Compound 2 was isolated from this plant for the first time.

Seven compounds were isolated from roots and stems of Oplopanax elatus, of which compounds 3, 4, 5 and 6 were isolated for the first time from the title plant; compounds 1 and 2 are new compounds and characterised to be 3,3'-dimethoxy-4,9,9'-trihydroxy-4',7-epoxy-5'8-lignan-4,9-bis-O-beta-D-glucopyranoside and 5-methoxylariciresinol-4-O-beta-D-glucopyranoside on the basis of NMR spectra and CD spectrum.

Three novel compounds, together with five known ingredients, octacosanol, 3',4',5-trihydroxy-3,7-dimethoxyflavone, 3,4-dihydroxybenzaldehyde, isorhamnetin, and ent-kaurane-3beta,16beta,17-triol, were obtained from the leaves of Smallanthus sonchifolius (yacon), and their structures were elucidated as ent-kaurane-3beta,16beta,17,18-tertol (1), 3R,7E-9-butoxyl-megastigma-3-ol-3-O-beta-D-glucopyranoside (2), and 3S,5R,6Z-megastigma-6-en-3,5,8,9-tertol (3) on the basis of spectroscopic and chemical methods.

Two new saponins were isolated from leaves of Panax quinquefolium and their structures were elucidated as 3beta, 12beta, 20S-trihydroxy-25-methoxydammar-23-ene 3-O-{[beta-D-glucopyranosyl(1-->2)-beta-D-glucopyranosyl]-20-O-[alpha-L-arabinopyranosyl(1-->6)]-beta-D-glucopyranoside (1) and 3beta, 20S-dihydroxy-12beta, 23R-epoxydammar-24-ene 3-O-{[beta-D-glucopyranosyl(1-->2)-beta-D-glucopyranosyl]-20-O-[beta-D-xylopyanosyl(1-->6)]-beta-D-glucopyranoside (2) on the basis of (1)D and (2)D NMR (including (1)H, (13)C-NMR, (1)H-(1)H COSY, HSQC, TOCSY, HMBC, and NOESY), ESI-MS spectrometry and chemical methods., (Copyright (c) 2008 John Wiley & Sons, Ltd.)

Four new diterpenoids, named smaditerpenic acid A-D, together with five known compounds, were isolated from the H(2)O extract of the leaves of Smallantus sonchifolius (yacon) cultivated in Liaoning, China and their structures were elucidated on the basis of one- and two-dimensional NMR (including (1)H, (13)C-NMR, (1)H-(1)H COSY, HSQC, TOCSY, HMBC, and ROESY), electrospray ionization mass spectrometry (ESI-MS), and chemical methods.

The aqueous ethanolic extract from the fresh cladodes of Opuntia dillenii HAW. was found to show anti-inflammatory activity. Two new alpha-pyrones, named opuntioside II (1) and opuntioside III (2), were isolated from the extract together with six known compounds. The structures of the new compounds were determined on the basis of chemical and physicochemical evidence.

To investigate the protective effect of ginsenoside Re (Re) against cerebral ischemia-reperfusion injury, adult male Wistar rats weighing 250-300 g were subjected to either sham surgery or middle cerebral artery occlusion (MCAO) for 2 h of brain ischemia and 2 h reperfusion. A fluorescence polarization assay was carried out for membrane fluidity of brain mitochondria. Lipid peroxidation [malondiadehyde (MDA) formation], superoxide dismutase (SOD) and glutathion peroxidase (GSH-Px) of rat brain were estimated by fluorometric methods. It was observed that Re (5, 10, 20 mg kg-1 p.o. pretreatment for 7 d, once a day) significantly improved the fluidity of mitochondrial membranes as demonstrated by a reduction of average microviscosity, ameliorated lipid peroxidation by raising the activities of SOD and GSH-Px, and reduced the content of MDA in rat brain. This study demonstrated a direct protective effect of Re against cerebral ischemia-reperfusion injury.

Three new A-ring lactone triterpenoid saponins, platycoside M-1 [3-O-beta-D-glucopyranosyl platycogenic acid A lactone], platycoside M-2 [3-O-beta-D-glucopyranosyl platycogenic acid A lactone 28-O-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside], and platycoside M-3 [3-O-beta-D-glucopyranosyl platycogenic acid A lactone 28-O-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside], were isolated from the roots of Platycodon grandiflorum A. DC. Their chemical structures were elucidated on the basis of their spectral data and chemical evidence.

Aim: To isolate triterpene saponins of polygalacic acid type from the roots of Platycodon grandiflorum (Jacq.) A. DC and to identify their structures., Methods: The compounds were separated by means of extraction, chromatography on silica gel, MPLC and HPLC, and their structures were elucidated on the basis of spectral analyses (FAB-MS, IR, 1H NMR, 13C NMR etc.)., Results: Three triterpene saponins were isolated from the roots of Platycodon grandiflorum. They were identified as 3-O-beta-D-laminaribiosyl polygalacic acid (I), 3-O-beta-D-glucopyranosyl polygalacic acid (II), polygalacin D (III), separately., Conclusion: Compound I is a new compound, compounds II, III are known triterpene saponins. The compound I and II were isolated from the plant for the first time, which is also the monodesmoside from the plant for the first time.

Five new triterpenoid saponins, platycoside H [3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-2beta,3beta,16alpha,23-tetrahydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside], platycoside I [3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-2beta,3beta,16alpha,23-tetrahydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside], platycoside J [3-O-beta-D-glucopyranosyl-2beta,3beta,16alpha,23-tetrahydroxyolean-12-en-28-oic acid 28-O-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-alpha-L-arabinopyranoside], platycoside K [3-O-beta-D-glucopyranosyl-(1-->3)-beta-D-glucopyranosyl-2beta,3beta,16alpha,23,24-pentahydroxyolean-12-en-28-oic acid], and platycoside L [3-O-beta-D-glucopyranosyl-(1-->6)-beta-D-glucopyranosyl-2beta,3beta,16alpha,23,24-pentahydroxyolean-12-en-28 oic acid], and three known triterpenoid saponins, platycoside F, platycoside B, and platycoside C, were isolated from the roots of Platycodon grandiflorum A. DC. Their chemical structures were elucidated on the basis of their spectral data and chemical evidence.

Objective: To study the chemical composition of Opuntia dillenii., Method: Many kinds of chromatography methods were used in the isolation procedure, while the structures of isolated compounds were determined on the aids of NMR and MS spectral analysis., Result: A new compound, together with five known compounds, was isolated form the 80% ethanolic extract of its stems., Conclusion: The new compound was characterized as opuntioside. Four compounds were obtained for the first from the genus Opuntia, and they were daucosterol, p-hydroxybenzoicacid, L-(-)-malic acid, (E)-ferulic acid. Opuntiol was also separated for the first from the plant.

Aim: To study the effects of ginsenoside-Ro on cell proliferation and cytokine production in murine splenocytes., Methods: The effect of ginsenoside-Ro on murine splenocytes proliferation was studied using [3H] thymidine incorporation assay. Effects of ginsenoside-Ro on the production of cytokines interleukin-2 (IL-2), interferon-gamma (IFN-gamma) and interleukin-4 (IL-4) from murine splenocytes were detected by ELISA method. Effects of ginsenoside-Ro on mRNA level of Th1 cytokine IFN-gamma and Th2 cytokine IL-4 were evaluated by reverse transcription polymerase chain reaction (RT-PCR) analysis., Results: Ginsenoside-Ro showed no mitogenic effect on unstimulated murine splenocytes. It enhanced the proliferation of Con A-induced murine splenocytes and the production of IL-2 at concentrations of 1-10 micromol x L(-1). Moreover, ginsenoside-Ro increased the production and expression of Th2 cytokine IL-4 and decreased the production and expression of Th1 cytokine IFN-gamma in Con A-induced murine splenocytes at concentrations of 2-10 micromol x L(-1)., Conclusion: Ginsenoside-Ro showed immunomodulatory effects by regulating the production and expression of Th1/Th2 cytokines in murine splenocytes.