The Chinese caterpillar fungus Ophiocordyceps sinensis has colonized the extreme high-elevation environment of the Qinghai-Tibet Plateau despite severe cold, hypoxia and intense UV radiation. We analysed 305 whole genomes, including 69 newly sequenced genomes, and resolved nine phylogenetic clades with a mosaic geographic distribution, with the Hengduan Mountains acting as both a diversity centre and a corridor for gene flow. These clades represent three evolutionary regimes: early lineages (Clades 1-4) primarily shaped by incomplete lineage sorting (ILS), intermediate lineages (Clades 5-8) shaped by the combined effects of ILS and introgression, and the most recent lineage (Clade 9) associated with candidate signatures of selection. Functional analyses revealed that ILS retained pathogenicity-related genes, introgression introduced adaptations in RNA processing, mitochondrial transport and lipid metabolism and candidate regions under selection targeted UV-damage repair and DNA replication. Together, these results demonstrate how ILS, introgression and selection-associated genomic changes acted sequentially to maintain parasitic lifestyle, enable environmental adaptation and drive rapid radiation under extreme alpine conditions.

Ophiocordyceps sinensis is a premier medicinal fungus with a unique slow-killing parasitic strategy, yet the molecular basis of its long-term persistence in host hemocoel remains elusive. This fungus coexists with Thitarodes xiaojinensis larvae for over six months, ultimately leading to host death at the last instar before pupation. To decode the fungal survival strategies masked by host resistance, this study integrated omics approach combining sublethal imidacloprid-induced transcriptomics with longitudinal metabolomic profiling. We investigated the transcriptomic response of O. sinensis within the larval hemocoel under exposure to a sublethal dose of imidacloprid, a stressor utilized here to suppress host immunity via neuro-immune crosstalk. This approach allowed us to infer the core molecular responses of O. sinensis across three critical infection stages (30, 90, and 150 days post-infection, dpi). Differential gene expression and functional enrichment analyses revealed that O. sinensis significantly responds to host immune disturbance induced by sublethal dose of imidacloprid. During the early infection stage (30 dpi), Imidacloprid exposure suppressed fungal cell proliferation genes while activating secondary metabolite pathways and immune defense genes. This suggests that during a conventional infection, O. sinensis secondary metabolism was suppressed under the host immunity to maintain a balanced blastospore proliferation. Beyond similar response in fungal secondary metabolites and host immunity, imidacloprid also suppressed protein biosynthesis during the mid-infection stage (90 dpi), indicating that the fungus undergoes metabolism suppression while continuing to maintain balance between blastospore proliferation and host immunogenicity for the conventional infection. During the late stage (150 dpi), genes associated with hydrolytic activity, transport and cell wall degradation were upregulated while fatty acid synthesis genes were downregulated by imidacloprid, suggested that the conventional infection of O. sinensis at this stage exhibits metabolic polarization to shift blastospore to hypha, tightly regulating hydrolysis to balance nutrient acquisition with host viability and increasing fatty acid biosynthesis. Metabolomic analysis showed that the accumulation of chitin precursors in the late stage, including D-glucosamine-6-phosphate, marks the critical blastospore-to-hyphae transition. Furthermore, the accumulation of compounds like chlorogenic acid, L-glutathione oxidized, and hesperidin indicates the dual responses of secreting antimicrobials and deploying antioxidants to protect and sanitize the nutrient base. This study provides insights into the dynamic, stage-specific gene expression profiles of O. sinensis that enable its long-term survival in the host hemocoel. Through coordinated regulation of proliferation, metabolism, secondary metabolite production, and immune evasion, the fungus sustains persistent infection and successfully completes its life cycle. These findings advance our understanding of the strategies employed by slow-killing fungal parasites.

Ophiocordyceps (Ophiocordyceps sinensis) is a precious medicinal and edible fungus widely utilized in nutraceuticals and functional foods. However, the structural intricacies and biological potential of its high-molecular-weight polysaccharides remain largely unknown. In the present study, a novel high-molecular-weight neutral polysaccharide, designated as CSP1b, was isolated and purified from cultured ophiocordyceps via water extraction, ethanol precipitation, and sequential column chromatography. Characterization revealed that CSP1b possesses an extraordinary molecular weight of 2.65 × 107 Da and consists predominantly of glucose (73.98%), mannose (13.35%), and galactose (12.67%). Structural elucidation identified CSP1b as a galactomannoglucan with a backbone of →4)-α-D-Glcp-(1 → 6)-α-D-Glcp-(1→, branched at the O-6 position by side chains containing →6)-α-D-Glcp-(1→, α-D-Manp-(1→, and various galactose residues, resulting in a branching degree of 32.06%. The polysaccharide exhibited a filamentous and ribbon-like intertwined surface morphology. In vitro immunomodulatory assays demonstrated that CSP1b significantly enhanced the proliferation and phagocytic capacity of RAW 264.7 (mouse macrophage cell line), as well as induced the secretion of nitric oxide (NO) and cytokines (TNF-α, IL-6) in a dose-dependent manner. In summary, a novel high-molecular-weight galactomannoglucan (CSP1b) was isolated for the first time from cultured ophiocordyceps and exhibited potent immunostimulatory activity. These findings enrich the polysaccharide library of ophiocordyceps and support its application in immunoregulatory products.

Capillary electrophoresis based on laser-induced fluorescence (CE-LIF) plays an important role in the analysis of nucleic acids. However, the commercial CE-LIF is not only quite expensive but also inflexible, thus hindering its widespread use in the lab. Herein, we proposed a compact, low-cost, and flexible CE-LIF system. We also investigated its stability by separating the DNA ladders. Experiments demonstrated that the relative standard error of the relative fluorescence intensity and migration time was lower than 6.2% and 1.1%, respectively. The aperture size of the light source illuminating the capillary can affect the separation performance. Smaller apertures offer higher resolution length for the adjacent DNA fragments but may reduce the number of theoretical plates. Various fluorescent dyes (e.g., SYBR Green I, Gel Green, EvaGreen) can be employed in the self-built system. The limit of detection of dsDNA was as low as 0.05 ng/μL. The working range for DNA was 0.05 ng/μL~10 ng/μL. Finally, we have successfully separated the PCR products of the target gene of Porphyromonas gingivalis and Candida albicans in the home-built CE system. Such a robust CE-LIF system is easy to assemble in the lab. The total cost of the assembled CE system did not exceed 1100 USD. We believe this work can advance the application of CE and hope it will facilitate the easy assembly of flexible CE instruments in labs.

The Asteraceae family, encompassing economically and aesthetically important genera such as chrysanthemum (Chrysanthemum x morifolium) and pyrethrum (Tanacetum cinerariifolium), holds substantial potential for ornamental, medicinal, and industrial applications. However, challenges in genetic transformation, primarily due to genotype-dependent regeneration barriers, significantly hinder advanced genetic research within this family. To overcome these obstacles, our study introduces a novel regeneration strategy that employing a chimeric transcriptional activation complex combining the potent VP64 transcriptional activator with Arabidopsis GROWTHREGULATING FACTOR 5 (AtGRF5) and GRF-INTERACTING FACTOR 1 (AtGIF1). This strategy markedly improved shoot induction and regeneration frequencies across various chrysanthemum and pyrethrum genotypes, achieving noTable 5-10-fold increases in these parameters in these parameters in genotypes traditionally challenging to regenerate. Additionally, this approach boosted the transformation efficiency, as demonstrated by a 7-fold increase in chrysanthemum '1581' following co-transformation with genetic vectors. Moreover, this approach enabled the successful transformation of the chrysanthemum genotypes 'LM28-4' and pyrethrum 'W99', which are relatively challenging to genetic modify. The broad applicability of this technique opens new avenues for the regeneration and genetic modification of a wide range of plant species, offering a fresh perspective on biotechnological interventions in horticulture.

Cultivated Chinese cordyceps (CCC), different from the cultivated Cordyceps sinensis mycelia, is regarded as the ideal substitution for wild Chinese cordyceps. As the main active component in Chinese cordyceps, polysaccharide quantification is important for its quality assessment. In this study, a major polysaccharide (CSWP-40) of CCC, characterized as a glucan with immune enhancing activities, was purified as the standard reference. A high-performance size exclusion chromatography method was developed and validated for the polysaccharide quantification. The results of different grade CCC tests revealed that CSWP-40 content in each strand of the big CCC (0.45-0.55 g/strand) was 6 times higher than that in small CCC (0.18-0.22 g/strand). Through meticulous source tracing, it was discovered that CSWP-40 was predominantly derived from the host caterpillar. Additionally, CSWP-40 can distinguish Chinese cordyceps from four common adulterants (Cordyceps hawkesii, Cordyceps liangshanensis, Cordyceps gunnii, and Cordyceps taii), which lack detectable CSWP-40. It is worth mentioning that CSWP-40 was also detected in Cordyceps gracilis and Cordyceps militaris, which implies that it is not exclusive to Chinese cordyceps. In summary, this study demonstrates that CSWP-40, a host caterpillarderived immunoactive polysaccharide, can be established as a central biomarker for quality assessment of CCC. Quantitative analysis of CSWP-40 not only facilitates accurate authentication and product-grade optimization but also provides critical quality control parameters for standardized manufacturing of high-value-added Cordyceps-derived products (e.g., pharmaceuticals and nutraceuticals), thereby enhancing industrial standardization and market credibility.

Chinese cordyceps (Cordyceps sinensis) is a rare medicinal fungus with significant therapeutic value, and its cultivated variants have garnered increasing attention in recent years. However, detailed structural and functional insights into cultivated Chinese cordyceps (CCC) polysaccharides remain limited. In this study, a novel galactoglucomannan (CSWP-80) with a molecular weight (Mw) of 26.2 kDa was extracted and purified from CCC. Structure characterization revealed that CSWP-80 possessed a backbone composed of →2)-α-D-Manp-(1 → and →6)-α-D-Glcp-(1→, substituted at the C-3 position by side chains containing Galf, Manp, and minor Glcp residues. The Galf side chains are predominantly composed of →5)-β-D-Galf-(1→, →6)-β-D-Galf-(1→, and terminal β-D-Galf-(1 → units. The Manp and Glcp side chains primarily consists of →4)-β-D-Manp-(1→, →2)-α-D-Manp-(1→, →4)-α-D-Glcp-(1 → linkages, along with terminal α-D-Manp-(1→ units. Tripartite antioxidant assessment systems (DPPH, SOD, FRAP) demonstrated that CSWP-80 possessed excellent antioxidant capacity. Furthermore, immune tests revealed that CSWP-80 not only enhanced macrophage proliferation and phagocytic activities but also stimulated the secretion of nitric oxide and cytokines (e.g., TNF-α, IL-10 and IL-6), indicating superior immunomodulatory properties. Mechanistic studies suggested that CSWP-80 likely activated macrophages via the TLR4-mediated NF-κB (p65) and MAPK (p38) signaling pathways. These findings provide a chemical-biological foundation for the potential application of CSWP-80 as a natural antioxidant and immunostimulant.

Adenosine is a key quality marker for the valuable fungus Cordyceps sinensis (C. sinensis). This study presents the first HPLC-based method for quantifying the activities and kinetic parameters of two adenosine-metabolizing enzymes-nucleotidase and adenosine deaminase-in C. sinensis. The enzyme extraction protocols, reaction systems, and assay procedures were optimized. Water was selected as the extraction solvent to preserve native enzymatic activity. Nucleotidase exhibited optimal activity at pH 6 and 35 degrees C, while adenosine deaminase showed optimal activity at pH 8 and 45 degrees C, revealing distinct catalytic profiles. Adenosine deaminase exhibited superior thermostability compared to nucleotidase. Kinetic analysis revealed that nucleotidase had a Michaelis constant of 0.24 mu mol center dot mL-1 and a maximum reaction rate of 7.92 mu mol center dot L-1 center dot min-1, while adenosine deaminase showed corresponding values of 0.14 mu mol center dot mL-1 and 0.61 mu mol center dot L-1 center dot min-1 . Method validation confirmed the reliability of the analytical system. Source-tracing analysis revealed that nucleotidase originated primarily from the fungal component, whereas adenosine deaminase was exclusively derived from the host larva and detected only in insect tissues. Therefore, adenosine deaminase activity serves as a reliable marker for distinguishing insect-free fungus from fungus-insect complex. These findings provide a scientific basis for optimizing adenosine accumulation and improving the quality control and management of C. sinensis.

BackgroundGlucagon-like peptide-1 (GLP-1)/glucagon (GCG) dual receptor agonists with different receptor selectivity are under investigation and have shown significant improvement in both weight loss and glycemic control, but the optimal potency ratio between the two receptors to balance efficacy and safety remains unclear.Experimental approachWe designed and constructed several dual receptor agonists with different receptor potency ratios using Fc fusion protein technology. The long-term effects of the candidates on body weight and metabolic dysfunction-associated steatotic liver disease (MASLD) were evaluated in diet-induced obese (DIO) model mice, high-fat diet (HFD)-ob/ob mice and AMLN diet-induced MASLD mice. Repeat dose toxicity assays were performed to investigate the safety profile of the candidate (HEC-C070) in Sprague Dawley (SD) rats.Key resultsThe high GCG receptor (GCGR) selectivity of HEC-C046 makes it more prominent than other compounds for weight loss and most MASLD parameters but may lead to safety concerns. The weight change of HEC-C052 with the lowest GCG agonism was inferior to that of selective GLP-1 receptor agonist (GLP-1RA) semaglutide in DIO model mice. The GLP-1R selectivity of HEC-C070 with moderate GCG agonism has a significant effect on weight loss and liver function in obese mice, and its lowest observed adverse effect level (LOAEL) was 30 nmol/kg in the repeat dose toxicity study.ConclusionWe compared the potential of the Fc fusion protein GLP-1/GCG dual receptor agonists with different receptor selectivity to provide the setting for future GLP-1/GCG dual receptor agonists to treat obesity and MASLD.

The high toxicity of arsenic (As) can cause irreversible harm to the environment and human health. In this study, the chlorin e6 (Ce6), which emits fluorescence in the infrared region, was introduced as the luminescence center, and the addition of copper ion (Cu2+) and As(V) provoked a regular change in fluorescence at 652 nm, whereas that of As(III) was 665 nm, which was used to optionally detect Cu2+, arsenic (As(III), and As(V)). The limit of detection (LOD) values were 0.212 μM, 0.089 ppm, and 1.375 ppb for Cu2+, As(III), and As(V), respectively. The developed method can be used to determine Cu2+ and arsenic in water and soil with good sensitivity and selectivity. The 1:1 stoichiometry of Ce6 with Cu2+ was obtained from the Job plot that was developed from UV–visible spectra. The binding constants for Cu2+ and As(V) were established to be 1.248 × 105 M−1 and 2.35 × 1012 M−2, respectively, using B–H (Benesi–Hildebrand) plots. Fluorescence lifetimes, B–H plots, FT–IR, and 1H-NMR were used to postulate the mechanism of Cu2+ fluorescence quenching and As(V) fluorescence restoration and the interactions of the two ions with the Ce6 molecule.

A simple, rapid, sensitive and eco-friendly liquid chromatography tandem mass spectrometry (LC-MS/MS) method was developed for simultaneous determination of free cordycepin (3 '-deoxyadenosine) and isocordycepin (2 '-deoxyadenosine) in 10 kinds of Cordyceps samples. The samples were prepared by ultrasonic extraction at 75 degrees C for 30 min with boiling water as the extraction solvent. The LC separation was performed on an Agilent poroshell 120 SB-Aq C18 column (3.0 x 50 mm, 2.7 mu m) in isocratic mode with an eco-friendly mobile phase (2% ethanol containing 0.2% acetic acid) at a flow rate of 0.6 mL min(-1), and detected by MS/MS in positive mode with multiple reaction monitoring (MRM). The developed method showed good linearity (r > 0.9990), sensitivity (LODs = 0.04 pg, LOQ = 0.1 pg), precision (RSD <= 3.8%) and stability (RSD <= 3.6%). The recoveries of developed method were 94.4-109.5% (RSD <= 5.5%). Compared with reported methods, the current method was rapid (less than 35% analytical time), sensitive (more than 5 folds), and eco-friendly (less than 10 mu L harmful organic solvent). 10 different kinds of Cordyceps samples (40 batches) were tested by the developed method. Codycepin was only found in Cordyceps millitaris and C. millitaris fruiting body, and isocordycepin was detected in Cordyceps sinensis and other 6 Cordyceps samples. The developed method would be an improved method for the quality evaluation of Cordyceps samples.

In this study, 3,4-diaminobenzoic acid (DABA) was introduced into the porphyrin metal–organic framework (PCN-224) for the first time to prepare a ratiometric fluorescent probe (PCN-224-DABA) to quantitatively detect ferric iron (Fe(III)) and selenium (IV) (Se(IV)). The fluorescence attributed to the DABA of PCN-224-DABA at 345 nm can be selectively quenched by Fe(III) and Se(IV), but the fluorescence emission peak attributed to tetrakis (4-carboxyphenyl) porphyrin (TCPP) at 475 nm will not be disturbed. Therefore, the ratio of I345nm/I475nm with an excitation wavelength of 270 nm can be designed to determine Fe(III) and Se(IV). After the experimental parameters were systematically optimized, the developed method shows good selectivity and interference resistance for Fe(III) and Se(IV) detection, and has good linearity in the ranges of 0.01–4 μM and 0.01–15 μM for Fe(III) and Se(IV) with a limit of detection of 0.045 μM and 0.804 μM, respectively. Furthermore, the quenching pattern was investigated through the Stern–Volmer equation, and the results suggest that both Se(IV) and Fe(III) quenched on PCN-224-DABA can be attributed to the dynamic quenching. Finally, the constructed ratiometric fluorescent probe was applied in the spiked detection of lake water samples, which shows good applicability in real sample analysis. Moreover, the Fe(III) and Se(IV) contents in spinach and selenium-enriched rice were determined, respectively.

目的:对冬虫夏草繁育品干品和鲜品中重金属及有害元素分布特征进行研究,以期为无公害冬虫夏草的繁育提供技术支持.方法:采用微波消解法对干品和鲜品样品进行有机破坏处理,以ICP-MS法为检测方法,对干品和鲜品共30批次的样品中铅(Pb)、镉(Cd)、砷(As)、汞(Hg)、铜(Cu)5种重金属及有害元素进行测定,结合化学计量学对测定结果的含量特征进行分析;结合课题组前期建立的风险评估方法(HI或MOE法)从食用及药用两方面对分析结果进行风险评估.结果:分析过程中各元素在线性范围内线性关系良好,进样精密度RSD在0.34％～0.79％之间,各元素的回收率在93.0％～103.0％之间.30批次样品中,Cu、Cd全部检出,含量范围分别是2.1～8.98 mg·kg-1和0.02～0.25 mg·kg-1;As有26批检出,含量范围是0.10～0.48 mg·kg-1;Pb有16批检出,含量范围是0.10～0.50 mg·kg-1;Hg仅有4批检出,含量范围是0.02～0.05 mg·kg-1.主成分分析及聚类分析结果表明,干品和鲜品重金属及有害元素含量特征具有明显的区别;风险评估结果表明,Cu、Cd、Hg元素的HI＜1,Pb、As元素的MOE>1,干品和鲜品中重金属及有害元素潜在的健康风险均较低.结论:本研究为繁育无公害且低含量重金属及有害元素的冬虫夏草和其质量标准的完善具有一定的指导作用.

Cordyceps sinensis is a precious medicinal food which has been successfully cultivated indoors. It remains to be investigated for a simultaneous comparison on aqueous components of natural and cultivated samples. Herein, an approach of quantitative nuclear magnetic resonance (qNMR) analysis combined with global spectral deconvolution (GSD) was established for simultaneous quantification of 26 aqueous components in C. sinensis. Processed by GSD, the distorted baselines of 1H NMR spectra were greatly improved, and overlapped signals were also well separated so as to achieve accurate identification and quantitation of components in C. sinensis. Method validation by UHPLC-QTOF-MS and TOF-SIMS analysis revealed that qNMR combined with GSD is a reliable approach for simultaneous quantification of multiple components including characteristic markers of glutamine, GABA and trehalose in authentic and fake C. sinensis. The well-established qNMR approach can be used for quality assessment of natural and cultivated C. sinensis as well as differentiation from fake ones.

Aims To verify whether the oral insulin N11005 is administered as a prandial insulin by assessing the pharmacokinetics (PK), pharmacodynamics (PD), and safety profiles of N11005 with a short-acting biosynthetic human insulin (Novolin R) as reference. Methods This was a randomized, open-label, single-dose, crossover hyperinsulinemic-euglycemic clamp study in healthy Chinese male subjects. A total of 12 subjects were enrolled in the test (T) group (N11005, 300 IU, p.o.) and the reference (R) group (Novolin R, 0.1 IU/Kg, i.h.) with a washout period of 14 days. All subjects were administered on the same day of the clamp study. Glucose Infusion Rates (GIR), serum insulin, and C-peptide concentration were determined during every 8-hour clamp cycle. Trial registration: Clinicaltrials.gov identifier NCT04975022. Results After administration, the ratios of mean serum C-peptide concentration to baseline concentration in both T and R groups were lower than 50%, which confirmed the stability of the clamp platform. T group (N11005) showed a more rapid onset of action (tGIR 10%max ≈11 min) and a comparable duration of action to the R group, which was basically in line with the characteristics of prandial insulins. No adverse events (AEs) occurred throughout the study, which demonstrated that N11005 and Novolin R are safe and well-tolerated. Conclusions The PD profiles of the single-dose N11005 in the human body are similar to those of prandial insulins, with an excellent safety profile. Clinical trial registration Clinicaltrials.gov , identifier NCT04975022.

A high-performance liquid chromatography (HPLC) method for the determination of 4 nucleosides by one reference compound in Chinese cordyceps was developed. The sample of Chinese cordyceps was prepared by ultrasonic extraction with a 0.5% phosphoric acid aqueous solution. The separation of the sample was performed on a CORTECS T3 column (100 mm × 4.6 mm, 2.7 μm) by gradient elution with acetonitrile and water at a flow rate of 1.0 mL/min. The wavelengths were set as 258 nm (0-5 min), 252 nm (5-9.1 min), 258 nm (9.1-10.5 min), 249 nm (10.5-20 min) at which 4 nucleosides exhibited identical ultraviolet absorption. The accuracy, precision, reproducibility, and stability tests of the HPLC method were carried out, and the results indicated that the established HPLC method was suitable for the quantitative analysis of 4 nucleosides in Chinese cordyceps. This approach was compared to the traditional external standard method with 4 nucleoside reference compounds and the relative standard errors of the content determination results by the 2 methods were less than 3.5%. The HPLC method developed for quantitative measurement of 4 nucleosides in Chinese cordyceps is simple, lower cost, and time-saving, which provides a methodology alternative for quality control of Chinese cordyceps.

Aim To develop and investigate an imbalanced dual gastric inhibitory polypeptide receptor (GIPR)/glucagon-like peptide-1 receptor (GLP-1 R) agonist with Fc fusion protein structure.Methods We designed and constructed an Fc fusion protein that is a dual agonist (HEC-CG115) with an empirically optimized potency ratio for GLP-1R and GIPR. The long-term effects of HEC-CG115 on body weight and glycaemic control were evaluated in diet-induced obese mice and diabetic db/db mice. Repeat dose toxicity assays were performed to investigate the safety profile of HEC-CG115 in Sprague-Dawley rats.Results HEC-CG115 displayed high potency for GIPR and relatively low potency for GLP-1R, and we labelled it 'imbalanced'. In animal models, HEC-CG115 (3 nmol/kg) led to more weight loss than semaglutide at a higher dose (10 nmol/kg) in diet-induced obese model mice. HEC-CG115 (one dose every 3 days) reduced fasting blood glucose and glycated haemoglobin levels similar to those after semaglutide (once daily) at the same dose. In a 4-week subcutaneous toxicity study conducted to assess the biosafety of HEC-CG115, the no observed adverse effect level was determined to be 3 mg/kg.Conclusion HEC-CG115 is a novel Fc fusion protein with imbalanced dual agonism that shows superior weight loss, glycaemic control and metabolic improvement in animal models, and has an optimal safety profile according to a repeat-dose toxicity study. Therefore, the use of HEC-CG115 appears to be safe and effective for the treatment of obesity and type 2 diabetes.

The development of pharmacological antiangiogenic agents to disrupt the vascular supply and starve tumours of nutrients and oxygen is a novel strategy for tumour therapy. Chinese cordyceps, a traditional Chinese herb, has been widely reported to exhibit antitumor effects. In the present study, we tested the suppression of tumour angiogenesis by Chinese cordyceps extract (CCE) via a tube formation assay using human umbilical vascular endothelial cells (HUVECs) in vitro and Lewis lung carcinoma xenografts in mice. In addition, CCE was investigated in an ex vivo angiogenesis assay using rat aortic rings. CCE showed a dose-dependent suppression of capillary tube formation in HUVECs as well as in rat aortic rings. The antiangiogenic activity of CCE was further verified in Lewis lung carcinoma xenograft models in mice, where the tumour volume was significantly decreased after treatment with CCE at 100 mg/kg. The mean vascular density (MVD) in the tumours, as measured by immunohistochemical staining of platelet endothelial cell adhesion molecule-1 (CD31), was also markedly reduced by treatment with CCE at 100 mg/kg. These results indicated that Chinese cordyceps may exhibit antitumor effects through antiangiogenic activity and could be used in the prevention and/or therapy of angiogenesis-related cancers.

目的:评价冬虫夏草提取物及其核苷酸类成分对碱性磷酸酶(ALP)的抑制活性.方法:采用紫外分光光度法测定27个冬虫夏草水提物和5个核苷酸成分的ALP抑制活性,采用分子对接研究5个核苷酸成分在ALP上的结合模式和位点.结果:测定结果表明冬虫夏草对ALP具有较好的抑制活性,不同来源和加工方式样品的ALP抑制活性存在差异.5个核苷酸小分子化合物的ALP抑制活性研究发现,AMP-2Na和CMP-2Na具有相对较好的酶抑制活性.分子对接结果表明氢键和金属—受体相互作用是核苷酸类小分子化合物与ALP结合的重要作用力.结论:研究结果可为虫草类药材治疗疾病及加工提供参考.

The material basis of Cordyceps sinensis (Berk.) Sacc has not yet been well understood and natural C. sinensis resources are very rare. The present study aimed to clarify the substance basis and compare the protective effect of natural and artificially-cultivated C. sinensis against cyclophosphamide (CTX)-induced myelosuppression. Both natural and artificially-cultivated C. sinensis effectively improved CTX-induced decrease of peripheral blood counts and hemopoietic growth factors, pathological changes, and apoptosis of bone marrow. Importantly, artificially-cultivated C. sinensis showed similar capacity compared with natural C. sinensis. Uridine (1), adenosine (2), L-pyroglutamic acid (3), lysinonorleucine (4), 1,3,5-trimethoxybenzene (5), D-mannitol (6), L-pyroglutamic acid methyl ester (7), tryptophan (8), and phenylalanine (9) were isolated from bioactivity-guided fraction and identified to attenuate CTX-induced myelosuppression in mice. In conclusions, nucleosides and amino acids represented the effective chemical components in C. sinensis. Artificial cultivation can be used as an effective substitute for natural C. sinensis.