Mori Ramulus (Chin.Ph.)-the Dried Twigs of Morus alba L./Part 1: Discovery of Two Novel Coumarin Glycosides from the Anti-Hyperuricemic Ethanol Extract.

In Traditional Chinese Medicine (TCM), Mori ramulus (Chin.Ph.)-the dried twigs of Morus alba L.-is extensively used as an antirheumatic agent and also finds additional use in asthma therapy. As a pathological high xanthine oxidase (XO, EC 1.1.3.22) activity is strongly correlated to hyperuricemy and gout, standard anti-hyperuremic therapy typically involves XO inhibitors like allopurinol, which often cause adverse effects by inhibiting other enzymes involved in purine metabolism. Mori ramulus may therefore be a promissing source for the development of new antirheumatic therapeutics with less side effects. Coumarins, one of the dominant groups of bioactive constituents of M. alba, have been demonstrated to possess anti-inflammatory, antiplatelet aggregation, antitumor, and acetylcholinesterase (AChE) inhibitory activities. The combination of HPLC (DAD) and Q-TOF technique could give excellent separating and good structural characterization abilities which make it suitable to analyze complex multi-herbal extracts in TCM. The aim of this study was to develop a HPLC (DAD)/ESI-Q-TOF-MS/MS method for the identification and profiling of pharmacologically active coumarin glycosides in Mori ramulus refined extracts for used in TCM. This HPLC (DAD)/ESI-Q-TOF-MS/MS method provided a rapid and accurate method for identification of coumarin glycosides-including new natural products described here for the first time-in the crude extract of M. alba L. In the course of this project, two novel natural products moriramulosid A (umbelliferone-6-ß-d-apiofuranosyl-(1→6)-ß-d-glucopyranoside) and moriramulosid B (6-[[6-O-(6-deoxy-α-l-mannopyranosyl)-ß-d-glucopyranosyl]oxy]-2H-1-benzopyran-1-one) were newly discovered and the known natural product Scopolin was identified in M. alba L. for the first time.

Health risk assessment of potentially harmful elements in subsidence water bodies using a Monte Carlo approach: An example from the Huainan coal mining area, China.

Enrichment of potentially harmful elements in surface water results in ecological risk to the surrounding environment. Assessing the environmental risk of these elements is of great importance. In this study, surface water samples from 6 different subsidence water bodies in the Huainan coal mining area were collected. The concentrations of Cu, Ni, Pb, Cd, Co, Cr, V, Fe, Mn and Zn were measured by atomic absorption spectrophotometry, and those of As and Hg were analyzed by atomic fluorescence spectrometry. Then, human health risks through the ingestion and dermal contact pathways were assessed and analyzed on the basis of a Monte Carlo simulation. The mean and 95th percentile risks were reported. The results showed that the total carcinogenic risk values in every subsidence water body summed for Cr, Ni and As via two exposure pathways were greater than the maximum acceptable level (1 × 10-4), and Xinji'er water body had the highest carcinogenic risk. Among three elements, Ni was the highest contributor to carcinogenic risk. All non-carcinogenic health risk (hazard quotients) values except for one water area of Co (Xinji'er) were less than 1; however, the total non-carcinogenic health risks of two water bodies (Xinji'er, Xinjiyi) summed for all the elements based on mean concentrations were higher than 1. Xinji'er had the highest hazard index. The extent of the impacts of the total hazard quotients followed the order of Co > As > Cd > Hg > Pb > V >Fe > Ni > Mn > Zn > Cr. Furthermore, the total hazard quotients of Co and As via ingestion pathway summed for the six subsidence water areas were greater than 1, which should be a concern.

Emission characteristics for gaseous- and size-segregated particulate PAHs in coal combustion flue gas from circulating fluidized bed (CFB) boiler.

The partitioning behavior of polycyclic aromatic hydrocarbons (PAHs) between gaseous and particulate phases from coal-fired power plants (CFPPs) is critically important to predict PAH removal by dust control devices. In this study, 16 US-EPA priority PAHs in gaseous and size-segregated particulate phases at the inlet and outlet of the fabric filter unit (FFs) of a circulating fluidized bed (CFB) boiler were analyzed. The partitioning mechanisms of PAHs between gaseous and particulate phases and in particles of different size classes were investigated. We found that the removal efficiencies of PAHs are 45.59% and 70.67-89.06% for gaseous and particulate phases, respectively. The gaseous phase mainly contains low molecular weight (LMW) PAHs (2- and 3-ring PAHs), which is quite different from the particulate phase that mainly contains medium and high molecular weight (MMW and HMW) PAHs (4- to 6-ring PAHs). The fractions of LMW PAHs show a declining trend with the decrease of particle size. The gas-particle partitioning of PAHs is primarily controlled by organic carbon absorption, in addition, it has a clear dependence on the particle sizes. Plot of log (TPAH/PM) against logDp shows that all slope values were below -1, suggesting that PAHs were mainly adsorbed to particulates. The adsorption effect of PAHs in size-segregated PMs for HMW PAHs is more evident than LMW PAHs. The particle size distributions (PSDs) of individual PAHs show that most of PAHs exhibit bi-model structures, with one mode peaking in the accumulation size range (2.1-1.1 µm) and another mode peaking in coarse size range (5.8-4.7 µm). The intensities of these two peaks vary in function of ring number of PAHs, which is likely attributed to Kelvin effect that the less volatile HMW PAH species preferentially condense onto the finer particulates. The emission factor of PAHs was calculated as 3.53 mg/kg of coal burned, with overall mean EFPAH of 0.55 and 2.98 mg/kg for gaseous and particulate phase, respectively. Moreover, the average emission amount of PAHs for the investigated CFPP was 1016.6 g/day and 371073.6 g/y, respectively.

Particle-Associated Polycyclic Aromatic Hydrocarbons (PAHs) in the Atmosphere of Hefei, China: Levels, Characterizations and Health Risks.

Airborne PM2.5 and PM10 samples were collected in summertime (August 2015) and wintertime (December 2015-January 2016) in an industrial complex area in Hefei, China. The average concentrations of PM2.5 and PM10 (90.5 and 114.5 µg/m3, respectively) were higher than the regulated levels of China National Ambient Air Quality Standard (grade I) and the WHO Ambient (outdoor) Air Quality and Health Guideline Value. Seasonal variations in PM2.5/PM10 indicated that the secondary sources of particulate matters, formed by gas-to-particle conversion, were enhanced in summer due to longer time of solar radiation and higher temperature. The total concentrations of PM2.5- and PM10-associated PAHs were 5.89 and 17.70 ng/m3 in summer as well as 63.41 and 78.26 ng/m3 in winter, respectively. Both PM2.5- and PM10-associated PAHs were dominated by 4- to 6-ring PAHs, suggesting that the fossil fuel combustion and vehicle emissions were the primary sources of PAHs in atmospheric particulate matters in Hefei. The total concentration of PAHs had a slightly higher correlation coefficient with PM2.5 (R = 0.499, P < 0.05) than PM10 (R = 0.431, P > 0.05), indicating the higher association tendency of PAHs with PM2.5. The coefficient of divergence analysis showed that the compositions of PAH were quite different between summer and winter. Total BaP equivalent concentration (BaP-TEQ) for particulate-bound PAHs in winter (58.87 ng/m3) was higher than that in summer (5.53 ng/m3). In addition, particulate-bound PAHs in winter had an inhalation cancer risk (ICR) value of 2.8 × 10-3, which was higher than the safe range (10-4-10-6).

Characteristic and Source of Atmospheric PM10- and PM2.5-bound PAHs in a Typical Metallurgic City Near Yangtze River in China.

The characteristics of atmospheric PM10- and PM2.5-bound polycyclic aromatic hydrocarbons (PAHs) were investigated in Tongling city, China. Results showed that the total concentrations of PM10- and PM2.5-bound PAHs exhibited distinct seasonal and spatial variability. The metallurgic sites showed the highest PAH concentrations, which is mainly attributed to the metallurgic activities (mainly copper ore smelting) and coal combustion as the smelting fuel. The rural area showed the lowest concentrations, but exhibited significant increase from summer to autumn. This seasonal fluctuation is mainly caused by the biomass burning at the sites in the harvest season. The diagnostic ratio indicated that the main PAHs sources were vehicle exhausts, coal combustion and biomass burning. The total BaP equivalent concentration (BAP-TEQ) was found to be maximum at DGS site in winter, whereas it was minimum at BGC site in summer. Risk assessment indicates that residential exposure to PAHs in the industrial area, especially in the winter season, may pose a greater inhalation cancer risk than people living in living area and rural area.

Comparative effects of biochar-nanosheets and conventional organic-amendments on health risks abatement of potentially toxic elements via consumption of wheat grown on industrially contaminated-soil.

Potentially toxic elements (PTEs) discharge to the soil environment through increased anthropogenic activities is a global threat. These PTEs can have harmful and chronic-persistent health effects on exposed populations through food consumption grown on contaminated soils. Efforts to investigate the transformation mechanism and accumulation behavior of PTEs in soil-plant system and their adverse health-effects have focused extensively in previous studies. However, limited studies address biochar nanosheets (BCNs) as a potential soil amendment to reduced humans health risks through dietary intake of food-crop grown on PTE-contaminated soil. Here, we showed how BCNs cutback health hazards of PTEs through impacts on bioavailability and phytoaccumulation of PTEs, and their daily intake via consumption of wheat. When BCNs amendment was compared with both conventional organic amendments (COAs) and control, it significantly (P ≤ 0.05) reduced bioavailability and uptake of PTEs by wheat plants. Based on risk assessment results, the hazard indices (HIs) for PTEs in all treatments were <1, however, BCNs addition significantly (P ≤ 0.05) reduced risk level, when compared to control. Furthermore, the cancer risks for Cd, Cr and Ni over a lifetime of exposure were higher in all treatments than the tolerable limit (1.00E-4 to 1.00E-6), however BCNs addition significantly suppressed cancer risk compared to control. Conclusively, our results suggest that BCNs can be used as soil amendment to reduce potential risks of PTEs through consumption of food grown in PTE-contaminated soils.

GOLPH2-regulated oncolytic adenovirus, GD55, exerts strong killing effect on human prostate cancer stem-like cells in vitro and in vivo.

GOLPH2 (also called GP73) is a Golgi glycoprotein, which has been identified as a novel tumor marker upregulated in various cancers, including prostate cancer (PCa). GD55 is a novel GOLPH2-regulated oncolytic adenovirus that exhibits a strong killing effect on hepatoma cells. Here, we investigate the antitumor effect of GD55 on prostate cancer stem cell (CSC)-like cells in vitro and in vivo. Prostate CSC-like sphere cells were acquired and enriched by culturing DU145, LNCap or P3 prostate cancer cells in suspension. The prostate CSC-like sphere cells were capable of self-renewal, differentiation and quiescence, displaying tumorigenic feature and chemo-resistance to 5-FU, doxorubicin and DDP. Treatment with GD55 (1, 5, 10 MOI) dose-dependently suppressed the viability of DU145 sphere cells, which was a more pronounced compared to its cytotoxic action on the parental DU145 cells. In a mouse xenograft prostate CSC-like model, intratumoral injection of GD55 markedly suppressed the growth rate of xenograft tumors and induced higher levels of cell death and necrosis within the tumor tissues. Our results demonstrate that GD55 infection exerts strong anticancer effects on prostate CSC-like cells in vitro and in vivo, and has a potential to be used in the clinical therapy of PCa.

Combination of oncolytic adenovirus and luteolin exerts synergistic antitumor effects in colorectal cancer cells and a mouse model.

In recent years, oncolytic viruses have attracted increasing interest due to their potent antitumor effects. Luteolin, a natural product, has additionally been observed to exhibit various pharmacological antitumor activities. Previously, a novel dual­targeting oncolytic adenovirus, complement decay­accelerating factor (CD55)­tumor necrosis factor ligand superfamily member 10 (TRAIL), was constructed, which exhibited significant growth inhibitory effects in various types of tumor cell. The present study investigated whether the combination of luteolin and CD55­TRAIL was able to exert a synergistic antitumor effect in colorectal carcinoma (CRC) cells. The cytotoxicity and tumor cell apoptosis mediated by combination treatment in CRC cells were detected via an MTT assay, Hoechst staining and western blotting, respectively. Tumor growth in vivo was examined in a CRC mouse xenograft model following various treatments. The results demonstrated that the addition of luteolin enhanced oncolytic adenovirus­mediated enhanced green fluorescent protein, early region 1A and TRAIL expression. The combination of CD55­TRAIL with luteolin synergistically inhibited tumor growth and promoted CRC cellular apoptosis in vitro and in vivo. Additionally, the combination of CD55­TRAIL with luteolin significantly decreased cytotoxicity in lung/bronchial normal epithelial cells, compared with single treatment. Therefore, the combination of CD55­TRAIL with luteolin may be a novel efficient therapeutic strategy for CRC in the future.

Mechanical Behavior of Recycled Aggregate Concrete-Filled Steel Tubular Columns before and after Fire.

Recycled aggregate concrete (RAC) is an environmentally friendly building material. This paper investigates the mechanical behavior of recycled aggregate concrete filled steel tube (RACFST) columns exposed to fire. Two groups of 12 columns were designed and tested, under axial compression, before and after fire, to evaluate the degradation of bearing capacity due to fire exposure. Six specimens were subjected to axial compression tests at room temperature and the other six specimens were subjected to axial compression tests after a fire exposure. The main parameters of the specimens include the wall thickness of the steel tube (steel content) and the type of concrete materials. Several parameters as obtained from the experimental results were compared and analyzed, including the load-bearing capacity, deformation capacity, and failure characteristics of the specimens. Meanwhile, rate of loss of bearing capacity of specimens exposed to fire were calculated based on the standards EC4 and CECS28:90. The results show that concrete material has a large influence on the rate of loss of bearing capacity in the case of a relatively lower steel ratio. While steel content has little effect on the rate of loss of bearing capacity of concrete-filled steel tube (CFST) columns after fire, it has a relatively large influence on the loss rate of bearing capacity of the RACFST columns. The loss of bearing capacity of the specimens from the experiment is more serious than that from the calculation. As the calculated values are less conservative, particular attention should be given to the application of recycled aggregate concrete in actual structures.

RGD-modified oncolytic adenovirus-harboring shPKM2 exhibits a potent cytotoxic effect in pancreatic cancer via autophagy inhibition and apoptosis promotion.

The M2 isoform of pyruvate kinase (PKM2) is a key driver of glycolysis in cancer cells and has critical 'non-metabolic' functions in some cancers; however, the role of PKM2 in pancreatic cancer remains unclear. The aim of the current study was to elucidate the role of PKM2 in pancreatic cancer progression and the potential of PKM2 as a therapeutic target. In this study, we observed that PKM2 is highly expressed in patients with pancreatic cancer and is correlated to survival. Elevated PKM2 expression promoted cell proliferation, migration and tumor formation. The inhibition of cell growth by silencing PKM2 is caused by impairment of the autophagy process. To test the potential effects of downregulating PKM2 as a clinical therapy, we constructed an RGD-modified oncolytic adenovirus containing shPKM2 (OAd.R.shPKM2) to knock down PKM2 in pancreatic cancer cells. Cells transduced with OAd.R.shPKM2 exhibited decreased cell viability, and, in a PANC-1 xenograft model, intratumoral injection of OAd.R.shPKM2 resulted in reduced tumor growth. Furthermore, OAd.R.shPKM2 induced apoptosis and impaired autophagy in PANC-1 cells. Our results suggested that targeting PKM2 with an oncolytic adenovirus produced a strong antitumor effect, and that this strategy could broaden the therapeutic options for treating pancreatic cancer.

Bioavailability evaluation, uptake of heavy metals and potential health risks via dietary exposure in urban-industrial areas.

A verity of human activities i.e. urbanization and industrialization have been resulted serious environmental contaminations by heavy metals in all over the world. The settlement of populations in urban and nearby industrial areas for economic development has significant share in their exposure to these metallic contaminants. Depending on the nature and type of the pollutants, targeted urban-industrial environments can have harmful and chronic health risk impacts on exposed local inhabitants and may require detoxification, healing and remedial therapy. Consequently, environmental monitoring as well as human health risk assessments of urban environments under industrial influence are key dominant features. We believe this work will provide new insights into the studies of metals exposure and associated health risks in emerging industrials cities of developing countries. Present study aimed to study the bioavailability of metals, quantify the changeability in soil and vegetable metal concentrations and estimation of human health risks via dietary exposure, focusing on urban-industrial environment. Soil and vegetable samples were collected in six random sites within the urban, periurban and industrial areas and analyzed for metal concentrations. In addition, risk assessment model proposed by US-EPA was employed to estimate the potential health risk of heavy metals via dietary intake. Results indicated that the heavy metal concentrations were noteworthy in periurban and urban-industrial areas. However, contamination levels varied with the type of vegetable, and the point source pollution such as traffic, urban wastes and industrial effluent. According to the estimated THQ and HI values for non-carcinogenic risk, little or no negative impact of heavy metals was observed on local inhabitants. However, the concentrations of Cr, Cd, Pb and Ni were nearly closed to the permissible limits described by US-EPA in urban-industrial areas. Conclusively, some efficient remedial strategies should be focus to overcome the increasing levels of Cr, Cd, Pb and Ni in this study area to protect the health of local inhabitants.

The importance of evaluating metal exposure and predicting human health risks in urban-periurban environments influenced by emerging industry.

The human population boom, urbanization and rapid industrialization have either directly or indirectly resulted in the serious environmental toxification of the soil-food web by metal exposure from anthropogenic sources in most of the developing industrialized world. The present study was conducted to analyze concentrations of Cd, Cr, Cu, Mn, Ni, Pb, and Zn in soil and vegetables in the urban-periurban areas influenced by emerging industry. Vegetables and their corresponding soil samples were collected and analyzed for heavy metals contents from six random sites. According to the results, the potential health risks from metals to the local communities were assessed by following the methodology described by the US-EPA. In general, the total non-carcinogenic risks were shown to be less than the limits set by the US-EPA. However, the potential risk of developing carcinogenicity in humans over a lifetime of exposure could be increased through the dietary intake of Cd, Cr and Ni. In some cases, Pb was also marginally higher than the safe level. It was concluded that some effective remedial approaches should be adopted to mitigate the risks of Cd, Cr, Ni and Pb in the study area because these metal levels have exceeded the safe limits for human health. However, new studies on gastrointestinal bioaccessibility in human are required to heighten our understanding about metals exposure and health risk assessment.

Variations of emission characterization of PAHs emitted from different utility boilers of coal-fired power plants and risk assessment related to atmospheric PAHs.

Coal-fired power plants (CFPPs) represent important source of atmospheric PAHs, however, their emission characterization are still largely unknown. In this work, the concentration, distribution and gas-particle partitioning of PM10- and gas-phase PAHs in flue gas emitted from different coal-fired utility boilers were investigated. Moreover, concentration and distribution in airborne PAHs from different functional areas of power plants were studied. People's inhalatory and dermal exposures to airborne PAHs at these sites were estimated and their resultant lung cancer and skin cancer risks were assessed. Results indicated that the boiler capacity and operation conditions have significant effect on PAH concentrations in both PM10 and gas phases due to the variation of combustion efficiency, whereas they take neglected effect on PAH distributions. The wet flue gas desulphurization (WFGD) takes significant effect on the scavenging of PAH in both PM10 and gas phases, higher scavenging efficiency were found for less volatile PAHs. PAH partitioning is dominated by absorption into organic matter and accompanied by adsorption onto PM10 surface. In addition, different partitioning mechanism is observed for individual PAHs, which is assumed arising from their chemical affinity and vapor pressure. Risk assessment indicates that both inhalation and dermal contact greatly contribute to the cancer risk for CFPP workers and nearby residents. People working in workshop are exposed to greater inhalation and dermal exposure risk than people living in nearby vicinity and working office.

Lupane- and Friedelane-Type Triterpenoids from Celastrus stylosus.

Two new triterpenoids, 30-hydroxylup-20(29)-ene 3ß-caffeate (1) and 24-nor-friedelan-6α,10-dihydroxy-1,2-dioxo-4,7-dien-29-oic acid (2), together with eight known compounds 3-10, were isolated from the roots of Celastrus stylosus. The structures of these compounds were elucidated on the basis of spectroscopic analyses. To the best of our knowledge, this represents the first study on the chemical constituents of C. stylosus. The antiproliferative activities of the triterpenoids against six human cancer cell lines (PANC-1, A549, PC-3, HepG2, SGC-7901, and HCCLM3) were evaluated. Compounds 3, 4, and 10 exhibited comparable activities against PC-3 and HCCLM3 cell lines as the positive control taxol.

A phytosterol enriched refined extract of Brassica campestris L. pollen significantly improves benign prostatic hyperplasia (BPH) in a rat model as compared to the classical TCM pollen preparation Qianlie Kang Pule'an Tablets.

In Qinghai Province, the Brassica campestris L. pollen preparation Qianlie Kang Pule'an Tablet (QKPT) is traditionally used for BPH therapy. However, in QKPT the content of supposedly active phytosterols is relatively low at 2.59%, necessitating high doses for successful therapy. Therefore, a phytosterol enriched (4.54%) refined extract of B. campestris pollen (PE) was developed and compared with QKPT in a BPH rat model. Six groups of rats (n=8 each), namely sham-operated distilled water control, castrated distilled water control, castrated QKPT 2.0g/kg, castrated PE 0.1g/kg, castrated PE 0.2g/kg, and castrated PE 0.4g/kg, were intragastrically treated with the respective daily doses. Testosterone propionate (0.3mg/day) was administered to all castrated rats, while the sham-operated group received placebo injections. After 30 days, the animals were sacrificed and prostates as well as seminal vesicles excised and weighted in order to calculate prostate volume index (PVI) as well as prostate index (PI) and seminal vesicle index (SVI), defined as organ weight in g per 100g body weight. Compared with sham-operated controls, PI (p<0.01), PVI (p<0.01), and SVI (p<0.01) were all significantly increased in all castrated, testosterone treated rats. After treatment with PE at 0.4 and 0.2g/kg or QKPT at 2.0g/kg per day, both indices were significantly reduced (p<0.01) as compared to the castrated distilled water control. For PE at 0.1g/kg per day only PI was significantly reduced (p<0.05). At the highest PE concentration of 0.4g/kg per day both PI and SVI were also significantly reduced when compared to the QKPT group (p<0.05). Both PE and QKPT demonstrated curative effects against BPH in the applied animal model. In its highest dose at 0.4g/kg per day, PE was clearly superior to QKPT.

Polycyclic aromatic hydrocarbons in sediments from the Old Yellow River Estuary, China: occurrence, sources, characterization and correlation with the relocation history of the Yellow River.

The levels of 16 USEPA priority PAHs were determined in surface sediments and one dated sediment core from the abandoned Old Yellow River Estuary, China. Total PAH concentrations in the surface sediments ranged from 100.4 to 197.3 ng g(-1) dry weight and the total toxic equivalent quantity (TEQ(carc)) values of the carcinogenic PAHs were very low. An evaluation of PAH sources based on diagnostic ratios and principal component analysis suggested that PAHs in the surface sediments mainly derived from combustion sources. The total PAH concentrations altered significantly with year of deposition and showed quite different patterns of change compared with other studies: it is hypothesized that the principal cause of these changes is the relocation of the course of the Yellow River to the sea in 1976 and 1996.

Post-column mobile phase adjustment: a strategy to eliminate the contradiction between liquid chromatography and mass spectrometry in the determination of flavonoids in rat plasma.

Flavonoids are a group of important naturally occurring polyphenolic compounds with a wide range of biological effects. In this study, a sensitive liquid chromatography tandem mass spectrometry method was developed to simultaneously determine multiple active flavonoids, including quercetin (Que), kaempferol (Kae), apigenin (Api), isorhamnetin (Iso), luteolin (Lut), and naringenin (Nar), in rat plasma. To achieve a satisfied peak shape and LC separation, formic acid with the concentration between 0.05 and 0.2%, or in some case 5%, was generally used to acidify the LC mobile phase in reported studies. Here we found that even 0.05% formic acid could lead to strong mass signal suppression, and the absence of formic acid could reverse the signal suppression but cause serious peak tailing. There is an irreconcilable contradiction between liquid chromatography (LC) and mass spectrometry (MS). In order to simultaneously satisfy LC and MS, LC mobile phase with 0.00075% formic acid and post column mobile phase adjustment with 0.0677% ammonium solution in isopropanol were applied. Compared with the conventional method with mobile phase containing 0.05% formic acid, the mass signal response of Que, Kae, Api, Iso, Lut, Nar, and Oka increased 26.2, 18.6, 13.6, 23.5, 17.5, 15.6 and 15.4 fold, respectively. In addition, the post column mobile phase addition exhibited the better peak shape for the reduction of analytes longitudinal diffusion. The method has been fully validated according to FDA guidelines within the linear range between 0.328 ng mL⁻¹ and 168 ng mL⁻¹, and successfully applied to a pilot pharmacokinetic study of rats after administering 5.43 g kg⁻¹ Pollen of Brassica campestris.

Cardiovascular protection and antioxidant activity of the extracts from the mycelia of Cordyceps sinensis act partially via adenosine receptors.

Mycelia of cultured Cordyceps sinensis (CS) is one of the most common substitutes for natural CS and was approved for arrhythmia in China. However, the role of CS in ameliorating injury during ischemia-reperfusion (I/R) is still unclear. We examined effects of extracts from CS on I/R and investigated the possible mechanisms. Post-ischemic coronary perfusion pressure, ventricular function, and coronary flow were measured using the Langendorff mouse heart model. Oxidative stress of cardiac homogenates was performed using an ELISA. Our results indicate that CS affords cardioprotection possibly through enhanced adenosine receptor activation. Cardioprotection was demonstrated by reduced post-ischemic diastolic dysfunction and improved recovery of pressure development and coronary flow. Treatment with CS largely abrogates oxidative stress and damage in glucose- or pyruvate-perfused hearts. Importantly, observed reductions in oxidative stress [glutathione disulfide (GSSG)]/[GSSG + glutathione] and [malondialdehyde (MDA)]/[superoxide dismutase + MDA] ratios as well as the resultant damage upon CS treatment correlate with functional markers of post-ischemic myocardial outcome. These effects of CS were partially blocked by 8-ρ-sulfophenyltheophylline, an adenosine receptor antagonist. Our results demonstrate a suppressive role of CS in ischemic contracture. Meanwhile, the results also suggest pre-ischemic adenosine receptor activation may be involved in reducing contracture in hearts pretreated with CS.