Enhanced immunomodulation and periodontal regeneration efficacy of subgingivally delivered progranulin-loaded hydrogel as an adjunct to non-surgical treatment for Class II furcation involvement in dogs.

AIM: To evaluate the effect of subgingival delivery of progranulin (PGRN)/gelatin methacryloyl (GelMA) complex as an adjunct to scaling and root planing (SRP) on an experimental periodontitis dog model with Class II furcation involvement (FI). MATERIALS AND METHODS: A Class II FI model was established, and the defects were divided into four treatment groups: (a) no treatment (control); (b) SRP; (c) SRP + GelMA; (d) SRP + PGRN/GelMA. Eight weeks after treatment, periodontal parameters were recorded, gingival crevicular fluid and gingival tissue were collected for ELISA and RT-qPCR, respectively, and mandibular tissue blocks were collected for micro computed tomography (micro-CT) scanning and hematoxylin and eosin (H&E) staining. RESULTS: The SRP + PGRN/GelMA group showed significant improvement in all periodontal parameters compared with those in the other groups. The expression of markers related to M1 macrophage and Th17 cell significantly decreased, and the expression of markers related to M2 macrophage and Treg cell significantly increased in the SRP + PGRN/GelMA group compared with those in the other groups. The volume, quality and area of new bone and the length of new cementum in the root furcation defects of the PGRN/GelMA group were significantly increased compared to those in the other groups. CONCLUSIONS: Subgingival delivery of the PGRN/GelMA complex could be a promising non-surgical adjunctive therapy for anti-inflammation, immunomodulation and periodontal regeneration.

The characterisation of the in vitro metabolism and transport of 6-hydroxykynurenic acid, an important constituent of Ginkgo biloba extracts.

6-Hydroxykynurenic acid (6-HKA) is a nitrogen-containing phenolic acid compound in Ginkgo biloba leaves. The pharmacological activities of 6-HKA have been reported and shown that 6-HKA has the potential to become a therapeutic drug and may play an important role in the treatment of nervous system diseases. However, there are few studies on the drug metabolism and transport of 6-HKA. The aim of this study is to investigate the in vitro metabolism of 6-HKA and its interaction with multiple important drug transporters.The in vitro metabolism experiments in the present study demonstrate that 6-HKA might not undergo phase-I or phase-II metabolism in hepatic microsomes/S9 of rats. In addition, some drug transporters, including OAT1/3, OCT2, MDR1, OATP1B1, MATE1/2K and OCTN2, were investigated. The cellular uptake assays indicate that 6-HKA exhibits inhibition to the transport of classical substrates mediated by OAT3, OCT2, MATE2K and OCTN2 but has no significant effect on the transport of substrates mediated by MDR1, OAT1, OATP1B1 or MATE1. Further investigation of cellular accumulation assays shows that 6-HKA might be the substrate of OAT3, but not OCT2 or OCTN2. The bidirectional transport study suggests that 6-HKA is not a substrate of MDR1.The information about the in vitro metabolism of 6-HKA and the interaction between 6-HKA and some transporters will help us to better understand the pharmacokinetic properties of 6-HKA and provide reference for its pharmacodynamics, DDIs and drug-food interactions studies.

Sediment Records of Polybrominated Diphenyl Ethers (PBDEs) from the Anhui Province Section of Yangtze River, China.

This study investigated the temporal changes of PBDEs in the sediment cores from the Anhui Province section of Yangtze River (YR), China. The dramatic increase of ∑Br3-Br9-BDEs and BDE-209 concentrations in cores in the period of ca. 1990-2008 was consistent with the booming of regional and national production and consumption of household appliances and electronics. Following declines in BDE-209 and ∑Br3-Br9-BDEs concentrations can be associated with the deceasing use of legacy commercial PBDE mixtures in recent years. Compared with the different regions around the world, sediments in the YR were moderately polluted by PBDEs. The levels and the detection rates of BDE-209 were highest among the detected PBDEs single congener. The composition analysis indicated that Deca-BDE, Octa-BDE, and Penta-BDE were the dominant forms in the YR. The increasing trends of both BDE-209 and ∑Br3-Br9-BDEs in the YR during 1990s and 2000s largely reflected the time periods for transferring PBDE sources from the developed countries to China. TOC and finer particles were strongly correlated with distributions of PBDEs in sediments.

Ginkgo biloba and Its Constituent 6-hydroxykynurenic-acid as well as Its Proanthocyanidins Exert Neurorestorative Effects against Cerebral Ischemia.

Neuroprotective effects against cerebral ischemia/reperfusion (I/R) injury by Ginkgo biloba leaves are commonly attributed to the antioxidant activity of its proanthocyanidins. Furthermore, preliminary experiments identified 6-hydroxykynurenic acid (6-HKA) as a major contributor to this effect of extract of G. biloba leaves (EGb) prepared according to the Chinese Pharmacopoeia (ChP). In order to elucidate the specific contribution of both proanthocyanidins and 6-HKA to the overall neurorestorative effects of this extract according to ChP, EGb ChP was separated into pure 6-HKA and a newly developed Ginkgo proanthocyanidin extract (GPE), enriched in proanthocyanidins but not containing 6-HKA. Male Sprague-Dawley rats were divided into the groups: sham: 8; model (placebo): 25; GPE 80 mg/kg: 13; GPE 40 mg/kg: 13; GPE 20 mg/kg: 16; grape seed extract (negative control) 40 mg/kg: 18; nimodipine (positive control) 2 mg/kg: 8. All non-sham animals were subjected to cerebral I/R injury by occluding the middle cerebral artery with a nylon suture that was removed after 2 h of ischemia to establish reperfusion. For comparison, a parallel series of experiments were performed with 6-HKA. In these in vivo experiments, neurological dysfunctions were reduced by both GPE and 6-HKA, and both average infarct size and concentrations of malondialdehyde (MDA) and super oxide dismutase (SOD) were significantly ameliorated as compared to the model group. This data, therefore, demonstrates that the neuroprotective effects of EGb cannot be explained by a purely chemical antioxidative effect alone as has been previously proposed, especially with regards to the proanthocyanidins. A pharmacological neurorestorative effect of EGb on neurons and brain tissue itself seems to be a much more straightforward explanation for the presented observations. This effect is most likely explained by the synergistic action of both its numerous phenolic constituents (GPE) and 6-hydroxykynurenic acid (6-HKA), which could be identified as one major contributor to the observed activity.

[Similarities and differences between Ginkgo biloba and Panax notoginseng in treatment of ischemic cerebrovascular disease].

Ginkgo biloba and Panax notoginseng are both herb medicines for cerebrovascular disease, and play an active role in treating ischemic cerebrovascular disease(ICVD). Their mechanisms of action include antioxidant stress, nerve protection, vascular protection. According to the comparative study of literatures, G. biloba has a certain protective effect from the early stage of free radical formation throughout the whole process of causing cell inflammation and apoptosis in antioxidant stress; while P. notoginseng has mainly anti-inflammatory, anti-apoptosis effects. In the nerve protection and repair of nerve damage caused by glutamate, both could promote neurogenesis, repair damaged axons and protect nerve cells. In addition, G. biloba could also relieve neurotoxicity caused by glutamate damage, while P. notoginseng have a unique effect in repairing blood-brain barrier(BBB) and blood vessel regeneration. In clinic, they are used as auxiliary drugs in combination with thrombolytic therapy, and play curative effects in alleviating inflammation, eliminating edema, improving the cure rate and the prognosis. For cerebral diseases caused by chronic cerebral hypoperfusion, G. biloba could reduce inflammation and improve cognition. In addition, G. biloba could protect neurocyte by adjusting the secretion of dopamine in vivo, and has a certain effect on antidepressant diseases, which however needs further studies.

Novel Strategy of Gene Delivery System Based on Dendrimer Loaded Recombinant Hirudine Plasmid for Thrombus Targeting Therapy.

This study proposed a new nonviral gene delivery system for thrombus targeting therapy based on PEGlyation polyamides dendrimer (PAMAM) modified with RGDyC to condense the pDNA with recombinant hirudine (rHV) gene (RGDyC-rHV-EGFP). The RGDyC-mPEG-PAMAM was synthesized and characterized by 1H NMR, PAMAM/pDNA was characterized by particle size, zeta potential, cellular uptake, and gel retraction assay. The transfection was carried out between lipofectamine 2000 and PAMAM/pDNA on HUVEC cells at various N/P ratios. The antithrombotic effect in vivo was evaluated by venous thrombosis model on Wistar rats. It showed that the drug delivery system of RGDyC modified PAMMA, which entrapped pDNA could significantly improve the transfection efficiency. It was about 7.56-times higher than that of lipofectamine 2000. In addition, the expression level of hirudine fusion protein was the highest at N/P ratio of 0.5. The results of antithrombotic effect showed that the weight of thrombus was reduced in RGDyC modified group; compared with heparin group, there was no significant difference ( P > 0.05). Overall, we take the advantage of the unique advantages of hirudine, combining the genetic engineering, nanocarriers, and targeting technology, to achieve the targeted enrichment and activation the hirudine fusion protein in the thrombus site, to improve the concentration of drugs in the thrombus site, finally increasing the curative effect and reduce the risk of bleeding. The strategy of gene delivery system holds unique properties as a gene delivery system and has great promises in thrombus targeting therapy.

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.

Temporal trends of polybrominated diphenyl ethers in the sediment cores from different areas in China.

This paper presented the historical data on the temporal trends of polybrominated diphenyl ethers (PBDEs) in the sediment cores collected from the Huaihe River, Yellow River and Chaohu Lake, China. Among the 40 targeted PBDE congeners, only 10, 6, and 9 of them were detected respectively in the samples from the Huaihe River, Yellow River and Chaohu Lake. On average, the total PBDEs concentrations in sediments were highest in Chaohu Lake followed by the Huaihe River and the Yellow River. As compared to other PBDE congeners, BDE-209 had higher concentrations and detection rates. The similar down core variation between PBDEs and total organic carbon (TOC) suggests that TOC is an important factor influencing PBDEs distribution in the sediments. The total PBDEs concentrations showed an increasing trend from bottom to upper sediments before a decreasing trend in the topmost sediments. The rapid urbanization and industrialization of these regions in recent decades may cause the historically increasing concentrations of sedimentary PBDEs, especially BDE-209. The decreasing PBDEs concentrations in topmost sediments was probably related to the strict environmental policies at present.

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.

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.

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.

HPLC quantification of all five ginkgolic acid derivatives in Ginkgo biloba extracts using 13 : 0 ginkgolic acid as a single marker compound.

An HPLC quantification method for ginkgolic acid derivatives in Ginkgo biloba leaf extracts was developed. Using 13 : 0 ginkgolic acid as a marker compound, the relative correlation factors of the four other ginkgolic acid derivatives - namely, 15 : 0 ginkgolic acid, 15 : 1 ginkgolic acid, 17 : 1 ginkgolic acid, and 17 : 2 ginkgolic acid - to 13 : 0 ginkgolic acid were determined by HPLC and subsequently used for calculating their contents in ten hydro-ethanolic refined extract samples. In other words, the content of 13 : 0 ginkgolic acid in the extracts was determined using the isolated compound as an external standard. Subsequently the now known concentration of this compound functioned as an internal standard for the quantification of the other four ginkgolic acid derivatives via the described correlation factors. This HPLC method was validated by two independent control measurements, one with an external standard for every individual compound and one based on the present method with the single marker compound alone. The results did not differ significantly in any of the 10 tested extract samples. The protocol presented here thus not only uses the same reference substance for G. biloba extracts as the current Chinese Pharmacopoeia method but also incorporates the advantages of the current European Pharmacopoeia approach. It is simple, reproducible, and can be used to determine the total contents of ginkgolic acid derivatives in G. biloba leaf extracts.

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.

[Optimization of extraction technology of compatibility of couplet medicines Epimedium brevicornu and Ligusticum chuanxiong by orthogonal design].

The study was using the orthogonal test and making the extraction rates of icariin, ferulic acid, epimedin A, epimedin B, epimedin C, baohuoside I and ligustilide determinated by HPLC multiwavelength switch, gradient elution and multi-index comprehensive weighted scoring method (weight coefficient was 0.47: 0.16: 0.07: 0.07: 0.08: 0.06: 0.09) as evaluation index, combine with SPSS 16.0 software to optimizing the best extraction. It was Yinpian soak 1 h, 12 times more than the volumn of 50% ethanol solution, by heating reflux extraction for 60 min. The compliance test indicates that the optimized compatibility extraction technology is stable and practical, and it has provided an experimental basis for compound preparation technology research of Epimedium brevicornu and Ligusticum chuanxiong.

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.

Construction of a methodology framework to characterize dynamic full-sector land-use carbon emissions embodied in trade.

The globally massive land-use changes associated with unprecedented urbanization rate are leading to prodigious quantities of carbon emissions. Nonetheless, the dynamics of land-use carbon emissions, particularly driven by supply-chain activities across all relevant industrial sectors, remain largely unexplored, especially in non-agricultural sectors. Here, we constructed a novel methodological framework to quantify full-sector land-use carbon emissions in Shenzhen, China, an international megacity grappling with acute land resource scarcity. Then, we integrated this framework with multiregional input-output analysis to uncover the multi-scale embodied land-use emissions propelled by Shenzhen's supply-chain activities. Our results indicate a marked increase in Shenzhen's embodied carbon emissions, approximately two orders of magnitude greater than its physical emissions, tripling during 2005-2018. Remarkably, non-agriculture sectors contributed 81.3-90.5 % of physical and 46.6-58.4 % of embodied land-use emissions. The land-use changes occurred outside Shenzhen accounted for 6.5-13.3 % of Shenzhen's total embodied land-use emissions. The sectoral analysis revealed a transition from traditional manufacturing (e.g., metallurgy, chemical products, textiles, wood products) in 2010-2015 to high-tech sectors (e.g., electronic equipment and other manufacture) in 2015-2018. This shift was primarily attributed to concurrent industry transfer actions, leading to aggressive changes in land-use emission intensity discrepancies within and outside Shenzhen. This study provides a scientific basis for designing effective strategies to mitigate land-use carbon emissions associated with supply-chain activities.

Optimizing the development of contaminated land in China: Exploring machine-learning to identify risk markers.

Often available for use, previously developed land, which includes residential and commercial/industrial areas, presents a significant challenge due to the risk to human health. China's 2018 release of health risk assessment standards for land reuse aimed to bridge this gap in soil quality standards. Despite this, the absence of representative indicators strains risk managers economically and operationally. We improved China's land redevelopment approach by leveraging a dataset of 297,275 soil samples from 352 contaminated sites, employing machine learning. Our method incorporating soil quality standards from seven countries to discern patterns for establishing a cost-effective evaluative framework. Our research findings demonstrated that detection costs could be curtailed by 60% while maintaining consistency with international soil standards (prediction accuracy = 90-98%). Our findings deepen insights into soil pollution, proposing a more efficient risk assessment system for land redevelopment, addressing the current dearth of expertise in evaluating land development in China.

Quality Evaluation of Shexiang Tongxin Dropping Pill Based on HPLC Fingerprints Combined with HPLC-Q-TOF-MS/MS Method.

Shexiang Tongxin Dropping Pill (STP) is a composite formula of traditional Chinese medicine that is widely used for the treatment of cardiovascular diseases. It consists of seven medicinal extracts thereof or materials, including Bufonis venenum, synthetic Moschus, Panax ginseng, Bovis calculus artifactus, Bear bile powder, Salvia miltiorrhiza Bge and synthetic borneol. However, it is considerably difficult to evaluate the quality of STP due to its complex chemical compositions. This paper was designed to explore a comprehensive and systematic method combining fingerprints and chemical identification for quality assessment of STP samples. Twenty batches of STP samples were analyzed by high-performance liquid chromatography (HPLC) and high-performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry. Ten common peaks were detected by HPLC fingerprint similarity evaluation system. Meanwhile, 100 compounds belonging to 4 structural characteristics, including 23 bufadienolides, 36 organic acids, 34 saponins and 7 other types, were systematically identified as the basic components in STP. This study could be used for clarifying the multiple bioactive substances and developing a comprehensive quality evaluation method of STP.

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.