The genus Dioscorea L. (Dioscoreaceae), a review of traditional uses, phytochemistry, pharmacology, and toxicity.

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Dioscorea, a member of the Dioscoreaceae family, comprises approximately 600 species and is widely distributed across temperate and tropical regions such as Asia, South Africa, and North America. The traditional medicinal uses of Dioscorea have been documented in Asian and African pharmacological systems. In Asia, this genus is traditionally used to treat respiratory illnesses, rheumatism, diabetes, diarrhea, dysentery, and other conditions. In Africa, this genus has been used to treat human immunodeficiency virus and ring worms. However, the traditional medicinal practices in North America rarely mention the use of this genus. AIM OF THE STUDY: The aim of this review is to comprehensively review the genus Dioscorea, focusing on its traditional uses, phytochemical constituents, pharmacological activities, and potential toxicities. The research also aims to highlight the valuable bioactive compounds within Dioscorea and emphasize the need for further investigations into acute and chronic toxicity, activity mechanisms, molecular markers, and other relevant factors to contribute to the discovery of novel pharmaceuticals. MATERIALS AND METHODS: A search for available information on Dioscorea was conducted using scientific databases, including PubMed, ISI-WOS, Scopus, and Google Scholar, as well as recent academic publications from reputable publishers and other literature sources. The search was not limited by language and spanned the literature published between 1950 and 2022. RESULTS: This article provides a comprehensive review of the Dioscorea genus, focusing on its traditional uses, phytochemical constituents, pharmacological activities, and potential toxicities. Extensive research has been conducted on this genus, resulting in the isolation and examination of over 1000 compounds, including steroids, terpenoids, and flavonoids, to determine their biological activities. These activities include anti-tumor, anti-inflammatory, immunomodulatory, neuroprotective, hypoglycemic, and hypolipidemic effects. However, some studies have indicated the potential toxicity of high doses of Dioscorea, highlighting the need for further investigations to assess the safety of this genus. Additionally, this review explores potential avenues for future research and discusses the challenges associated with a comprehensive understanding of the Dioscorea genus. CONCLUSIONS: Based on the existing literature, it can be concluded that Dioscorea is a valuable source of bioactive compounds that have the potential to treat various disorders. Future research should prioritize the investigation of acute and chronic toxicity, activity mechanisms, molecular markers, and other relevant factors. This review provides a comprehensive analysis of the Dioscorea genus, emphasizing its potential to enable a deeper exploration of the biological activity mechanisms of these plants and contribute to the discovery of novel pharmaceuticals.

Review of the Chemical Composition and Biological Activities of Essential Oils from Artemisia Argyi, Artemisia Princeps, and Artemisia Montana.

BACKGROUND: Artemisia argyi Lévl. et Van., Artemisia princeps Pamp., and Artemisia montana Pamp., which are the sources of mugwort, have been popular across East Asian countries for nearly 2000 years now. Essential oils are the major chemical component obtained from them, exhibiting a variety of biological activities. OBJECTIVE: This review mainly focuses on the chemical composition and biological activities of A. argyi essential oil (AAEO), A. princeps essential oil (APEO), and A. montana essential oil (AMEO), with a special focus on their common and specific characteristics. The traditional use, distribution, and botany of A. argyi, A. princeps, and A. montana have also been summarized. In addition, the pharmacokinetics of AAEO was involved. METHODS: We collected literature from online and offline databases by entering the following keywords: mugwort, wormwood, A. argyi, A. princeps, A. montana, essential oil, and volatile oil. No language limitation was present in our search. RESULTS: A. argyi, A. princeps, and A. montana were used as traditional medicine, food, and health care products for a long time in Asia. They are widely distributed in most parts of China, Korea, and Japan. AAEO, APEO, and AMEO composed of monoterpenes, sesquiterpenes and their derivatives, alkanes, olefins, etc. Most of the specific compounds of AAEO were monoterpenoids, nearly half of the specific compounds of APEO were aliphatic hydrocarbons, and the sesquiterpenes were the typical specific compounds of AMEO. The mugwort essential oil showed multiple biological activities, such as anti-microbial, anti-inflammatory, antioxidant, antitumor, anticoagulation, sedative, and insecticide. CONCLUSION: The present review provided insight into the chemical composition and biological activity of AAEO, APEO, and AMEO. The comprehensive literature showed that they possessed wide application prospects in various fields. However, they should be studied in more depth. The underlying bioactive mechanisms should be elucidated and their toxicity and quality control should be determined.

[Correlations between appearance traits and internal quality of Bupleurum scorzonerifolium roots based on theory of "quality evaluation through morphological identification"].

It is generally believed that high-quality Bupleurum scorzonerifolium roots possess specific morphological characteristics, being red, robust, and long with strong odor. However, the scientific connotation of these characteristics has not been elucidated. According to the theory of "quality evaluation through morphological identification", we studied the correlations between appearance traits(the RGB value of root surface, root length, root diameter, dry weight, and ratio of phloem to xylem) and content of main chemical components(volatile oils, total saponins, total flavonoids, total polysaccharides, and seven saikosaponins) of B. scorzonerifolium roots. Epson Scanner and ImageJ were used to scan the root samples and measure the appearance traits. Ultraviolet spectrophotometry and HPLC were employed to determine the content of chemical components. The correlation, regression, and cluster analyses were performed to study the correlations between the appearance traits and the content of chemical components. The results showed that the content of volatile oils and saikosaponins were significantly correlated with RGB value, root length, and root diameter, indicating that within a certain range, the roots being redder, longer, and thicker had higher content of volatile oils and saikosaponins. According to the appearance traits and chemical component content, the 14 samples from different producing areas were classified into four grades, and the differences in morphological traits and chemical component content were consistent among different grades. The findings in this study demonstrate that appearance traits(RGB value, root length, and root diameter) can be used to evaluate the quality of B. scorzonerifolium roots. Meanwhile, this study lays a foundation for establishing an objective quality evaluation method for B. scorzonerifolium roots.

Study on molecular mechanism of volatiles variation during Bupleurum scorzonerifolium root development based on metabolome and transcriptome analysis.

Bupleurum scorzonerifolium Willd. is a medicinal herb. Its root has a high content of volatile oil (BSVO), which shows a variety of biological activities. Currently, BSVO in the injectable form is used for treating fever in humans and livestock. The yield and quality of volatile oils depends on the developmental stages of plants. However, the changes in BSVO yield and quality during root development in Bupleurum scorzonerifolium and the underlying molecular regulatory mechanisms remain unclear. This knowledge gap is limiting the improvement in the quality of BSVO. In the present study, B. scorzonerifolium root was collected at germinative, vegetative, florescence, fruiting and defoliating stages. The yield of BSVO, metabolic profile of volatile components and transcriptome of root samples at various developmental stages were comprehensively determined and compared. BSVO continuously accumulated from the germinative to fruiting stages, and its level slightly decreased from the fruiting to defoliating stages. A total of 82 volatile components were detected from B. scorzonerifolium root, of which 22 volatiles were identified as differentially accumulated metabolites (DAMs) during the root development. Of these volatiles, fatty acids and their derivatives accounted for the largest proportion. The contents of most major volatiles were highest at the fruiting stage. A large number of differentially expressed genes (DEGs) were detected during B. scorzonerifolium root development, of which 65 DEGs encoded various enzymes and transcription factors regulating the biosynthesis of fatty acids and their derivatives. In further analysis, 42 DEGs were identified to be significantly correlated with DAMs, and these DEGs may be the key genes for the biosynthesis of volatiles. To the best of our knowledge, this is the first study to comprehensively report the changes in the composition and content of volatiles and underlying mechanism during B. scorzonerifolium root development. This study provided important reference for future studies to determine the harvest time of B. scorzonerifolium roots and improve the quality of BSVO.

New insights into immunomodulatory properties of lactic acid bacteria fermented herbal medicines.

The COVID-19 pandemic has brought more attention to the immune system, the body's defense against infectious diseases. The immunomodulatory ability of traditional herbal medicine has been confirmed through clinical trial research, and has obvious advantages over prescription drugs due to its high number of potential targets and low toxicity. The active compounds of herbal drugs primarily include polysaccharides, saponins, flavonoids, and phenolics and can be modified to produce new active compounds after lactic acid bacteria (LAB) fermentation. LAB, primary source of probiotics, can produce additional immunomodulatory metabolites such as exopolysaccharides, short-chain fatty acids, and bacteriocins. Moreover, several compounds from herbal medicines can promote the growth and production of LAB-based immune active metabolites. Thus, LAB-mediated fermentation of herbal medicines has become a novel strategy for regulating human immune responses. The current review discusses the immunomodulatory properties and active compounds of LAB fermented herbal drugs, the interaction between LAB and herbal medicines, and changes in immunoregulatory components that occur during fermentation. This study also discusses the mechanisms by which LAB-fermented herbal medicines regulate the immune response, including activation of the innate or adaptive immune system and the maintenance of intestinal immune homeostasis.

Immunoregulatory mechanism studies of ginseng leaves on lung cancer based on network pharmacology and molecular docking.

Panax ginseng is one of the oldest and most generally prescribed herbs in Eastern traditional medicine to treat diseases. Several studies had documented that ginseng leaves have anti-oxidative, anti-inflammatory, and anticancer properties similar to those of ginseng root. The aim of this research was to forecast of the molecular mechanism of ginseng leaves on lung cancer by molecular docking and network pharmacology so as to decipher ginseng leaves' entire mechanism. The compounds associated with ginseng leaves were searched by TCMSP. TCMSP and Swiss Target Prediction databases were used to sort out the potential targets of the main chemical components. Targets were collected from OMIM, PharmGKB, TTD, DrugBank and GeneCards which related to immunity and lung cancer. Ginseng leaves exert its lung cancer suppressive function by regulating the several signaling proteins, such as JUN, STAT3, AKT1, TNF, MAPK1, TP53. GO and KEGG analyses indicated that the immunoreaction against lung cancer by ginseng leaves might be related to response to lipopolysaccharide, response to oxidative stress, PI3K-Akt, MAPK and TNF pathway. Molecular docking analysis demonstrated that hydrogen bonding was interaction's core forms. The results of CCK8 test and qRT-PCR showed that ginseng leaves inhibit cell proliferation and regulates AKT1 and P53 expression in A549. The present study clarifies the mechanism of Ginseng leaves against lung cancer and provides evidence to support its clinical use.

Dynamic changes of the main active constituents in valerian rhizome and root (Valeriana amurensis Smir. ex Kom.) during different harvest periods / Cambios dinámicos de los principales constituyentes activos del rizoma y raíz valeriana (Valeriana amurensis Smir. Ex Kom.) durante diferentes períodos de cosecha

Valeriana amurensis Smir. ex Kom. widely distributed in the northeast region of China and some region in Russia and Korea, and its underground parts (roots and rhizomes) being used to cure nervous system diseases such as insomnia. The active components including the essential oil and iridoids of underground parts were investigated in different harvest periods in order to evaluate the quality for the roots and rhizomes of V. amurensis. The content of the essential oil was obtained by hydrodistillation and bornyl acetate in the oil was quantitated by GC-EI. The iridoids, valepotriates were determined by potentiometric titration and the main component, valtrate was quantitated by HPLC-UV. The factors of biomass were considered in the determination of collection period. Statistical analysis of results showed that, the highest content of the essential oil per plant was 22.69 µl in withering period and then 21.58 µl in fruit ripening period, while the highest contents of bornyl acetate, valepotriates and valtrate per plant were 2.82 mg, 31.90 mg and 0.98 mg in fruit ripening period separately. Fruit ripening period was decided as the best harvest period for the content of active constituents and output of drug, and it would provide scientific basis for the artificial cultivation of V. amurensis.

Valeriana amurensis Smir. ex Kom. Se distribuye ampliamente en la región noreste de China y en algunas regiones de Rusia y Corea, y sus partes subterráneas (raíces y rizomas) se utilizan para curar enfermedades del sistema nervioso como el insomnio. Se investigaron los componentes activos, incluidos el aceite esencial y los iridoides de las partes subterráneas de V. amurensis en diferentes períodos de cosecha para evaluar la calidad de las raíces y rizomas. El contenido del aceite esencial se obtuvo mediante hidrodestilación y el acetato de bornilo en el aceite se cuantificó por GC-EI. Los iridoides, valepotriatos se determinaron mediante valoración potenciométrica y el componente principal, el valtrato se cuantificó por HPLC-UV. Los factores de biomasa fueron considerados en la determinación del período de recolección. El análisis estadístico de los resultados mostró que el mayor contenido de aceite esencial por planta fue de 22,69 µl en el período de marchitación y luego de 21,58 µl en el período de maduración de la fruta, mientras que el mayor contenido de acetato de bornilo, valepotriatos y valtrato por planta fue de 2.82 mg, 31.90 mg y 0,98 mg, respectivamente, en el período de maduración de la fruta por separado. Se definió el período de maduración de la fruta como el mejor período de cosecha para el contenido de constituyentes activos y la producción de droga, lo cual proporcionaría una base científica para el cultivo artificial de V. amurensis.

Transcriptomic analysis in Anemone flaccida rhizomes reveals ancillary pathway for triterpene saponins biosynthesis and differential responsiveness to phytohormones.

Anemone flaccida Fr. Schmidt is a perennial medicinal herb that contains pentacyclic triterpenoid saponins as the major bioactive constituents. In China, the rhizomes are used as treatments for a variety of ailments including arthritis. However, yields of the saponins are low, and little is known about the plant's genetic background or phytohormonal responsiveness. Using one-quarter of the 454 pyrosequencing information from the Roche GS FLX Titanium platform, we performed a transcriptomic analysis to identify 157 genes putatively encoding 26 enzymes involved in the synthesis of the bioactive compounds. It was revealed that there are two biosynthetic pathways of triterpene saponins in A. flaccida. One pathway depends on ß-amyrin synthase and is similar to that found in other plants. The second, subsidiary ("backburner") pathway is catalyzed by camelliol C synthase and yields ß-amyrin as minor byproduct. Both pathways used cytochrome P450-dependent monooxygenases (CYPs) and family 1 uridine diphosphate glycosyltransferases (UGTs) to modify the triterpenoid backbone. The expression of CYPs and UGTs were quite different in roots treated with the phytohormones methyl jasmonate, salicylic acid and indole-3-acetic acid. This study provides the first large-scale transcriptional dataset for the biosynthetic pathways of triterpene saponins and their phytohormonal responsiveness in the genus Anemone.

Identification and characterization of major constituents in Juglans mandshurica using ultra performance liquid chromatography coupled with time-of-flight mass spectrometry (UPLC-ESI-Q-TOF/MS).

The present study was designed to identify and characterize the major constituents in Juglans mandshurica Maxim. A simple, efficient and sensitive ultra performance liquid chromatography coupled with time-of-flight mass spectrometry (UPLC-ESI-Q-TOF/MS) method was established and validated under positive and negative ion modes. The separation was performed on a Waters ACQUITY UPLC BEH C18 column (2.1 mm × 100 mm, 1.7 µm) by gradient elution with a mobile phase (Phase A: 0.1% aqueous formic acid solution, Phase B: 0.1% formic acid acetonitrile solution). A total of 165 compounds were rapidly selected by Targeted and Non-Targeted Peak Finding approaches, and then tentatively identifled by comparing with reference substances or inferred through mass spectrometry fragment ion analysis and literature data. These compounds included 68 naphthalenequinones, 20 diarylheptanoids, 29 flavonoids, 20 triterpenes, and 28 phenolic acids. In conclusion, the present study provided an effective approach to identifying components in complex matrices of herbal medicines such as Juglans mandshurica Maxim.

Comparison of the chemical profiles of fresh-raw and dry-processed Juglans mandshurica.

The processing of Juglans mandshurica Maxim. is important to reduce its toxicity and enhance its efficacy. Simple, efficient, and sensitive ultra-high performance liquid chromatography coupled with a time-of-flight mass spectrometry based chemical profiling approach was proposed to rapidly evaluate the chemical difference between fresh and dry samples. Under the optimized ultra-high performance liquid chromatography and quadrupole time-of-flight tandem mass spectrometry conditions, 81 significantly different compounds were rapidly discovered using principal component analysis, and then tentatively identified by comparison with reference substances or inferred through mass spectral fragment ion analysis and literature data. These compounds included 35 naphthoquinones, 11 diarylheptanoids, nine flavonoids, eight triterpenes, 12 phenolic acids, and six aliphatics. The results demonstrated that chemical reactions occurring during processing could be used to elucidate the processing mechanism of Juglans mandshurica Maxim. This study provides a novel approach to identifying complicated components of various complex mixtures in fresh-raw and dry-processed traditional Chinese medicines, which could be used as a valid analytical method to further understand the processing mechanisms of these medicines, as well as providing intrinsic quality control of the medicines and their processed products.

Zisheng Shenqi decoction ameliorates monosodium urate crystal-induced gouty arthritis in rats through anti-inflammatory and anti-oxidative effects.

Based on traditional Chinese medicinal theories on gouty arthritis, Zisheng Shenqi decoction (ZSD), a novel Chinese medicinal formula, was developed due to its multiple functions, including reinforcing renal function, promoting blood circulation and relieving pain. In the present study, the effect of ZSD on monosodium urate (MSU) crystal-induced gouty arthritis in rats was investigated and the underlying mechanisms were examined. The data from these investigations showed that the injection of MSU crystals into the ankle joint cavity caused significant elevations in ankle swelling and inflammatory cell infiltration into the synovium, whereas these abnormal changes were markedly suppressed by oral administration of ZSD (40 mg/kg) for 7 days. Mechanically, ZSD treatment prevented MSU crystal­induced inflammatory responses, as evidenced by downregulation in the expression levels of NACHT domain, leucine­rich repeat and pyrin domain containing protein (NALP) 1 and NALP6 inflammasomes, decreased serum levels of tumor necrosis factor­α and interleukin­1ß, and inhibited activation of nuclear factor­κB. In addition, ZSD administration markedly enhanced the anti-oxidant status in MSU crystal­induced rats by the increase in the activities of superoxide dismutase and glutathione peroxidase, and the levels of reduced glutathione. These results indicated that ZSD effectively prevented MSU crystal-induced gouty arthritis via modulating multiple anti­oxidative and anti­inflammatory pathways, suggesting a promising herbal formula for the prevention and treatment of gouty arthritis.

[Determination of eight heavy metals and two main ingredients of safflower planted in linzhi of Tibetan].

The eight heavy metals and two essential constitutes of safflowers planted in linzhi which lies in Southern Tibet were analyzed by ICP-MS and by HPLC respectively. Heavy metals of safflower in the region were at the lower level and the essential constitutes were at the higher level. The better quality of safflower here was assisted by the excellent climate in tibet.

Constituents from Zhuyeqing Liquor with hepatoprotective effect on alcohol-induced HepaG 2 toxicity.

An unprecedented new skeleton compound (1R, 10R, 11S)-10,11-dimethyl-4-formyl-2,9-dioxa-bicyclo [5.4.0] undeca-4,6-dien-3-one (1), monoterpenoids and monoterpene glycoside picrocrocinic ester (2), epijasminoside B (3) and 6'-O-(3-methoxyl-4-hydroxyl-coumaroyl)-epijasminoside B (4), along with 26 known compounds, were obtained from Zhuyeqing Liquor. These compounds were identified mainly by analyzing their NMR, HR-ESI-MS and CD data. The isolated compounds were screened against alcohol induced HepaG 2 toxicity for hepatoprotective assay. Compounds 10, 19, 21 and 26 displayed the highest potency against alcohol induced HepaG 2 toxicity with the cell viability ratio 41.21, 56.91, 67.69 and 70.32% respectively.

Screening for differentially expressed genes in endophytic fungus strain 39 during co-culture with herbal extract of its host Dioscorea nipponica Makino.

Strain 39 is an endophytic fungus which was isolated from Dioscorea nipponica Makino (DNM). After Strain 39 co-cultured with ethanol extract of DNM rhizomes for several days, the content of saponins in this culture mixture would be obviously increased. To analyze the mechanism of this microbial transformation, we used the differential display reverse transcription polymerase chain reaction (DDRT-PCR) method to compare the transcriptomes between Strain 39 cultured in normal PD medium and in PD medium which added ethanol extract of DNM rhizomes. We amplified 29 DDRT-PCR bands using 12 primer combinations of three anchored primers and five random primers, and six bands were re-amplified. Analysis of real-time PCR and sequence alignment showed that three clones were up-regulated in sample group: squalene epoxidase, squalene synthase, and catalase, one clone was expressed only in sample group. The possible roles and origins of the above genes were discussed, and the molecular mechanism of Strain 39 biotransformation was speculated. This study is the first report of the molecular biotransformation mechanism of saponins production by endophytic fungus of DNM.

A caryophyllane-type sesquiterpene, caryophyllenol A from Valeriana amurensis.

A new caryophyllane derivative, caryophyllenol A, and a new germacrane derivative, isovolvalerenal D, together with 11 known sesquiterpenoids, were isolated from a petroleum ether partition of the roots and rhizomes of Valeriana amurensis. Structure elucidation of caryophyllenol A and isovolvalerenal D was accomplished on the basis of various spectroscopic techniques including HRESIMS and 2D NMR analyses. The structure of caryophyllenol A was further confirmed by X-ray crystallography and using quantum-chemical ECD calculation adopting TDDFT method. Caryophyllenol A and other eight sesquiterpenoids were evaluated for sedative activity with the model of Drosophila melanogaster, and eight of them showed the effect of prolonging the total sleeping time (TST) of D. melanogaster, displaying significant sedative action.

Metabolomic profiling for identification of potential biomarkers in the protective effects of modified Sinisan against liver injury in dimethylnitrosamine treated rats.

Metabolomics is a new platform based on the comprehensive analysis of low molecular weight metabolites and provides a powerful approach to discover biomarkers in biological systems. Modified Sinisan (MSNS), a traditional Chinese medicine formula, displayed bright prospects in the prevention and therapy of liver injury. However, its molecular mechanism of hepatoprotective effects remains unclear. This paper was designed to explore the effects and potential mechanisms of MSNS against dimethylnitrosamine-induced liver injury. Global metabolic profiling was performed by ultra-performance liquid chromatography/electrospray ionization quadrupole time-of-flight mass spectrometry (UPLC/ESI-Q-TOF-MS) in conjunction with multivariate data analysis and pathway analysis. Eleven serum biomarkers were identified and pathway analysis results showed that phenylalanine, tyrosine and tryptophan biosynthesis, phenylalanine metabolism, tryptophan metabolism, retinol metabolism, tyrosine metabolism were perturbed by liver injury. More importantly, MSNS has showed satisfactory pharmacological effect on liver injury through partially regulating the perturbed pathways, correlates well to the biochemical and histopathological detection results. The present study proved that the robust metabolomics approach is promising for unraveling hepatoprotective effects of MSNS and these findings provide new insights into mechanisms of the liver injury, and its pathophysiologic processes.

Protective effects of Zhuyeqing liquor on the immune function of normal and immunosuppressed mice in vivo.

BACKGROUND: Zhuyeqing Liquor (ZYQL), a well-known Chinese traditional health liquor, has various biological properties, including anti-oxidant, anti-inflammatory, immunoenhancement and cardiovascular protective effects. METHODS: The protective effects of Zhuyeqing Liquor (ZYQL) on the immune function was investigated in vivo in normal healthy mice and immunosuppressed mice treated with Cyclophosphamide (Cy, 100 mg/kg) by intraperitoneal injection on days 4, 8 and 12. ZYQL (100, 200 and 400 mg/kg) was administered via gavage daily for 14 days. The phagocytotic function of mononuclear phagocytic system was detected with carbon clearance methods, the levels of interleukin-6 (IL-6) and interferon-gamma (IFN-γ) in serum were detected with Enzyme linked immunosorbent assay (ELISA). Immune organs were weighed and organ indexes (organ weight/body weight) of thymus and spleen were calculated. Meanwhile, the activity of lysozyme (LSZ) in serum and the activity of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), catalase (CAT) in spleen tissue were measured. RESULTS: ZYQL significantly upgrades the K value for clearance of carbon particles in normal mice treated with ZYQL (400 mg/kg) and immunosuppressed mice treated with ZYQL (100, 200 and 400 mg/kg) together with Cy (100 mg/kg) in vivo. The treatment of ZYQL (100, 200 and 400 mg/kg) effectively increased the activity of serum lysozyme as well as promoted the serum levels of IL-6 and IFN-γ in normal mice and immunosuppressed mice. Furthermore, ZYQL (100, 200 and 400 mg/kg) had an antioxidant effects in immune system by enhancing the antioxidant enzyme activity of SOD, CAT and GSH-Px in vivo. In addition, ZYQL (100, 200 and 400 mg/kg) effectively elevated the Cy-induced decreased organ index (thymus and spleen). CONCLUSIONS: The present work shows that the dose-dependent administration of ZYQL is capable of influencing immune responses, which implying that its valuable functional health may be attributed partly to its protective effects for the immune function.

Identification of metabolites of FR429, a potential antitumor ellagitannin, transformed by rat intestinal bacteria in vitro, based on liquid chromatography-ion trap-time of flight mass spectrometry analysis.

FR429 is an ellagitannin with a potential antitumor activity, isolated and purified from Polygonum capitatum Buch.-Ham.ex D.Don, which is a traditional Miao-nationality herbal medicine in Guizhou and Yunnan of China. Our preliminary result of pharmacology study has indicated that the antitumor activity of FR429. However, the metabolism of FR429 has not been reported yet. In this study, LC-ion trap-time of flight mass spectrometry (LC-IT-TOF/MS) was used to characterize unpredictable metabolites of FR429 biotransformed by intestinal bacteria in vitro. Total thirteen metabolites were detected and characterized via comparisons of their accurate molecular masses and fragment ions of each MS(n) stage with those of the parent drug, and four of them were also elucidated by NMR. The results demonstrated that FR429 could be transformed by intestinal bacteria in vitro, mainly via hydrolysis and reduction reaction. This work provided a basis for the further study on the biotansformation of FR429 in vivo.

Bioactivity-guided fractionation and analysis of compounds with anti-influenza virus activity from Gardenia jasminoides Ellis.

Bioassay-guided fractionation of extracts from Fructus Gardeniae led to analysis of its bioactive natural products. After infection by influenza virus strain A/FM/1/47-MA in vivo, antiviral activity of the extracts were investigated. The target fraction was orally administered to rats and blood was collected. High-performance liquid chromatography coupled with photo diode array detector and electrospray ion trap multiple-stage tandem mass spectrometry was applied to screen the compounds absorbed into the blood. A structural characterization based on the retention time, ultraviolet spectra, parent ions and fragmentation ions was performed. Thirteen compounds were confirmed or tentatively identified. This provides an accurate profile of the composition of bioactive compounds responsible for the anti-influenza properties.

[Pharmacological effects of volatile oil of Valeriana amurensis on CNS].

OBJECTIVE: To study the pharmacological effects of volatile oil of Valeriana amurensis on central nervous system. METHODS: The pharmacological effects of volatile oil of Valeriana amurensis on the autonomic activities of mice, the sleeping synergistic action of mice with pentoharbital sodium at subthreshold and hypnotic dosages, the sleep phases of rats, the writhing response of mice caused by acetic acid and the convulsion of mice induced by thio-semicarbazide were investigated. RESULTS: The autonomic activities of mice were significantly inhibited by the volatile oil of Valeriana amurensis. The rate of falling sleep and the extension of sleeping time of mice were significantly increased by the synergic action of pentobarbital sodium with the volatile oil. The sleep phases of SWS2 and REMS of rats were obviously extended by the volatile oil of Valeriana amurensis. In addition, the frequency of writhing response of mice caused by acetic acid was reduced, and the convulsion of mice induced by thio-semicarbazide was antagonized with the administration of the volatile oil. CONCLUSION: The volatile oil of Valeriana amurensis has significantly sedative analgesic and anti-hyperspasmia effects.