LIFE SCIENCES
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2020
·
IF 3.647
Jing Yang,Yiwen Zhou,Jinsong Shi
Acute pancreatitis (AP) is a noninfectious inflammatory disease with high morbidity and mortality, which is characterized by severe inflammation and tissue necrosis. Cordycepin (CRD), derived from Cordyceps militaris , possesses anti-inflammatory effects and immunomodulation properties. Here, we investigated the protective effects of CRD on pancreatic injury and clarified potential mechanisms in AP model. There were established caerulein-induced AP and CRD pretreatment models in vivo and in vitro, as showed by serum enzymes, histopathological alterations and pro-inflammatory cytokines. Pretreatment with CRD notably downregulated the serum amylase and lipase levels and apparently reduced pancreatic histopathological alterations in AP mice. Meanwhile, the MPO staining confirmed that CRD pretreatment modulated the infiltration of neutrophils in AP mice. Furthermore, CRD markedly decreased the levels of pro-inflammatory factors (IL-6, IL-1β, and TNF-α) though inhibiting the activation of nuclear factor-κB (NF-κB) and NLR family pyrin domain-containing protein 3 (NLRP3) inflammasome in AP mice. In pancreatic acinar cancer cell 266-6, CRD pretreatment decreased cholecystokinin(CCK)-induced inflammatory response was consistent with those in vivo. Mechanistically, CRD was also revealed to activate activated protein kinase (AMPK) and attenuated inflammation both in vivo and in vitro. On the whole, this study indicated that CRD protects mice from pancreatic inflammatory process and damage by suppressed NF-κB and NLRP3 inflammasome activation via AMPK, which probably contributed to the potential therapy for AP.
研究领域:
药理学
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免疫学
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分子生物学
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DOI
PubMed
高影响因子
Foods
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2025
·Vol. 14
·期 15
·2711
·
IF 5.1
Wanying Song,Xinyue Zhang,Huiyi Yang,Hanyu Liu,Baodong Wei
This study presents the development and optimization of a functional soy sauce fermented withCordyceps militaris(C. militaris), a medicinal fungus known for its high cordycepin and polysaccharide content. UsingC. militarisas the sole starter culture, the process aimed to improve both nutritional and functional properties. Response surface methodology was employed to optimize the entire fermentation process. During the koji stage, temperature, aeration, and inoculum concentration were adjusted to maximize protease activity and cordycepin production. In the fermentation stage, temperature, brine concentration, and water-to-material ratio were optimized to increase amino acid nitrogen and bioactive compound levels. Under optimal conditions (24 °C, 679.60 LPM aeration, 9.6% inoculum for koji; 32 °C, 12% brine, 1.53:1 water-to-material ratio for fermentation), the resulting soy sauce contained 1.14 ± 0.05 g/100 mL amino acid nitrogen and 16.88 ± 0.47 mg/100 mL cordycepin. Compared with traditionally fermented soy sauce, theC. militarisproduct exhibited a darker color, enhanced umami taste, and a distinct volatile profile featuring linoleic acid, methyl palmitate, and niacinamide. These results demonstrate the feasibility of usingC. militarisin soy sauce fermentation and its potential as a novel functional condiment with improved bioactivity and sensory quality.
研究领域:
食品科学
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微生物学
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生物技术
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营养学
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发酵工程
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PubMed
高影响因子
BIOMEDICAL CHROMATOGRAPHY
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2025
·Vol. 39
·期 4
·e70038
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IF 1.7
Mengjiao Li,Fuqiang Liu,Lulu Guo,Wu Fan,Jiazhong Wang,Binbin Lu,Guangfeng Hong,Wenjuan Zhang,Shu Tian,Jian Mao,Jianping Xie
Cordycepin, a natural adenosine derivative, exhibits multiple pharmacological effects on organisms. However, its distribution and metabolic characteristics have not been fully elucidated in vivo. In this study, ultra-high liquid chromatography tandem high-resolution mass spectrometry (UHPLC-HRMS/MS) was used to investigate the pharmacokinetic characteristics and effects of cordycepin on endogenous adenosine and inosine. Microdialysis was used for real-time monitoring of unbound drug in brain and blood, whereas conventional tissue homogenate methods assessed distribution in various tissues. Results showed that the distribution pattern of cordycepin was as follows: kidney > liver > heart > lung > spleen > brain. Cordycepin administration significantly altered the levels of adenosine and inosine in heart and liver. Synchronous microdialysis sampling for the pharmacokinetic profile indicated that cordycepin was rapidly consumed and 3′-deoxyinosine was generated as the main metabolite. The C max values of cordycepin in the rat blood and brain after exposure (10 mg/kg, i.p.) were 7.8 and 5.4 ng/mL, respectively. Mean residence time in blood and brain was 102.2 and 137.0 min, respectively. Inhibition of adenosine deaminase by racemic 9-(2-hydroxy-3-nonyl) adenine hydrochloride (EHNA) enhanced cordycepin levels in the blood. This work provides a solid basis for understanding the metabolism of cordycepin and its pharmacological effects.
研究领域:
药理学
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分析化学
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生物化学
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DOI
PubMed
高影响因子
Journal of Cosmetic Dermatology
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2019
·Vol. 18
·期 6
·1899-1906
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IF 1.311
Jie Tang,Lidan Xiong,Xiaohong Shu,Wei Chen,Wenjia Li,Jing Li,Lianzheng Ma,Ying Xiao,Li Li
Summary Background Excessive free radicals, generated from the metabolic reaction in organisms, have been implicated in many human diseases as well as aging process. Nowadays, many synthetic substances have been developed as anti-oxidation cosmetic ingredients. However, man-made antioxidants often have certain toxicity and side effects, which make their application under strict control. Therefore, more and more researchers focus on natural antioxidants because of their advantages. Aims In this study, CE obtained from natural Chinese medicine was used to investigate whether it had antioxidant effect in vitro and repair effect on HaCaT cell damage caused by UVB. Methods UV-Vis and HPLC were adopted for qualitative and quantitative analysis of CE. We investigated the antioxidant potential of CE by assessing its ABTS + , DPPH•, hydroxyl (OH•), and superoxide anions ( ) free-radical quenching ability. The safety of CE was studied by CCK-8 assay. To evaluate the anti-oxidation effect of CE on UVB-induced damage on HaCaT cells, superoxide dismutase (SOD) activity, and malondialdehyde (MDA) content were tested. Results Experiment data showed that the CE displayed high scavenging ability: ABTS + , DPPH•, OH•, and quenching rates were 88%, 64%, 94%, and 58%, respectively. Furthermore, after UVB radiation (30 mJ/cm 2 ), adding CE (50-500 μg/mL) could increase the SOD activity in HaCaT cells and reduce the MDA contents. Conclusions All results illustrate that the CE shows significant antioxidant effect on scavenging free radicals in vitro. Besides, the CE can repair UVB-induced oxidant damage by improving SOD activity and reducing MDA content.
研究领域:
药理学
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皮肤生物学
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天然产物化学
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DOI
PubMed
高影响因子
Developmental Neurobiology
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2025
·Vol. 85
·期 2
·e22961
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IF 2.3
Yongzhi San,Minghua Wang
Background Mitophagy is important for normal neural activity. Epilepsy is intimately linked to neurotoxicity due to mitochondrial dysfunction. Cordycepin (Cor) has been shown to exert neuroprotective effects. This study aims to investigate whether Cor could mitigate neurotoxicity in epilepsy by modulating mitophagy. Methods In vitro, kainic acid (KA) was utilized to induce cytotoxicity in HT22 cell. Cell viability was assessed using the CCK-8 assay, while cell damage was evaluated through an LDH kit. Flow cytometry was used to assess apoptosis. The expressions of G protein-coupled receptor 120 (GPR120), apoptosis, and mitophagy-related proteins were analyzed by western blot. Inflammatory factors and oxidative stress levels were examined by kits. DCFH-DA staining was applied to observe cellular reactive oxygen species (ROS) levels. The three-dimensional coordinates of GPR120 were retrieved from the PDB database, and molecular docking was performed using AutoDock. Immunofluorescence staining was used to observe mitophagy level. Results Cor significantly attenuated KA-induced HT22 cell viability injury and inflammation, while suppressing ROS and oxidative stress levels. Notably, Cor ameliorated the decrease of mitophagy level observed in HT22 cells treated with KA. GPR120 expression was upregulated following KA treatment and further elevated after adding Cor. Cor could bind to GPR120. Interference with GPR120 reversed the ameliorative effects of Cor on KA-induced mitophagy and cytotoxicity in HT22 cells. Conclusion Overall, Cor significantly alleviated KA-induced HT22 cell neurotoxic damage and oxidative stress. This protective effect may be mediated through GPR120-regulated mitophagy.
研究领域:
神经科学
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药理学
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DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF PHARMACOLOGY
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2025
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IF 4.7
Yang Sun,Mengling Zhong,Jingjie Wang,Mingmei Feng,Caihong Shen,Zhipeng Han,Xiaonian Cao,Qi Zhang
Aging can cause age-related diseases such as cancer, cardiovascular and neurodegenerative diseases. Cordycepin exerts anti-oxidation, anti-inflammatory and neuroprotective effects. However, the anti-aging effect of cordycepin is still unclear. This study aimed to investigate the anti-aging effect of cordycepin and unravel the underlying mechanism. Cordycepin prolonged the lifespan of C. elegans under normal and heat stress conditions, without effects on the normal growth and reproduction of C. elegans . Cordycepin also improved the locomotion ability, inhibited the deposition of aging pigment lipofuscin and alleviated the oxidative stress damage by decreasing the excessive accumulation of ROS and raising the antioxidant enzyme activities in C. elegans . The metabolomics study showed that cordycepin changed 19 metabolites including citric acid, linoleic acid, oleic acid, glutamic acid, pyruvic acid and so on. Transcriptomics study revealed that cordycepin up-regulated the gene expression of acox-1.2, acox-1.3, acox-1.4, acs-1, acs-15, acdh-1, acdh-4 and acdh-8 in C. elegans , suggesting that cordycepin prolonged its lifespan via regulating fatty acid degradation, fatty acid metabolism and so on. In summary, the current study demonstrated that cordycepin exerted the anti-aging effect on C. elegans by improving the antioxidant system and regulating the genes involved in fatty acid metabolism to inhibit the accumulation of linoleic acid and oleic acid. Therefore, cordycepin might be a promising agent for aging and age-related diseases.
研究领域:
生物化学
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分子生物学
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衰老研究
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DOI
PubMed
高影响因子
Crystals
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2025
·Vol. 15
·期 12
·1043
·
IF 2.4
Wenbo Li,Shushu Li,Qingshi Wen,Xiaohan Zhang,Ke Zhang,Chenglun Tang,Fengxia Zou,Keke Zhang,Pengfei Jiao,Pengpeng Yang
Cordycepin (3′-deoxyadenosine, 3′-dA), the flagship nucleoside antibiotic from Cordyceps militaris, exerts potent anti-inflammatory, antimicrobial, and antitumor activity but is rapidly inactivated by human adenosine deaminase (ADA). While prodrugs, ADA inhibitors, and nanocarriers have been pursued to prolong its half-life, the influence of solid form on delivery performance remains unexplored. Here, three polymorphs—anhydrate-I (flake-like), anhydrate-II (rod-like), and a previously unreported monohydrate (fibrillar)—were prepared, characterized (PXRD, TG-DSC, FTIR), and subjected to equilibrium solubility, slurry-conversion, and humidity-sorption mapping. The monohydrate dehydrates at 144 °C and sequentially transforms to anhydrate-I → anhydrate-II (ΔH = −127.5 J g−1), establishing a monotropic relationship between the two anhydrous forms. Solubility displays a bell-shaped profile versus water activity: the monohydrate is stable above aw 0.8, whereas anhydrate-II predominates below aw 0.2. In model immediate-release tablets, anhydrate-II achieves complete dissolution within 10 min, whereas the monohydrate sustains release for 30 min. Hygroscopicity tests show the monohydrate absorbs <6% water up to 75% RH without structural change, whereas anhydrate-I converts to the monohydrate above 63% RH. The quantitative humidity–crystal form–performance correlations provide a rational platform for crystal form selection and the design of stable, efficacious cordycepin solid dosage forms.
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高影响因子
Scientific Reports
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2025
·Vol. 15
·期 1
·1-12
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IF 3.9
Cheng Chunfang,Zhang Shasha,Chen Chong,Gong Yanchun,Ding Kaizhi,Li Guoyin,Jiang Wei,Zhang Zhenyu,He Bin,Hu Zhihong,Li Yuhua,Yao Lihua
Excessive exercise can lead to physical fatigue and disruption of the antioxidant system, resulting in neurological damage and cognitive decline. Cordycepin, the main component of Cordyceps militaris , has anti-inflammatory, antioxidant and neuroprotective effects. In this study, the anti-fatigue effect and potential mechanism of action of cordycepin were investigated using a forced exercise mouse model. The results showed that oral administration of cordycepin enhanced exercise endurance, increased liver and muscle glycogen content, and simultaneously decreased serum levels of lactic acid, lactate dehydrogenase, creatine kinase, and blood urea nitrogen ( p < 0.05). In addition, cordycepin had antioxidant effects, increasing superoxide dismutase activity and decreasing serum malondialdehyde (MDA) levels ( p < 0.01). In vitro experiments further demonstrated the antioxidant and anti-fatigue effects of cordycepin. Behavioral tests showed that the learning and memory ability of mice in the excessive exercise model group decreased to 40% compared with the control group. Cordycepin alleviated the learning and memory deficits in the over-exercised mice, significantly reduced the levels of fatigue metabolites and oxidative stress in vivo ( p < 0.05), and altered the levels of neurotransmitters levels ( p < 0.05). Furthermore, cordycepin modulated Keap1/Nrf2/HO-1-mediated oxidative stress and enhanced BDNF levels ( p < 0.05). These findings suggest that cordycepin can alleviate excessive exercise-induced fatigue by modulating the Keap1/Nrf2/HO-1 signaling pathway and BDNF expression, providing strong supporting evidence for the development of cordycepin-functional foods or anti-fatigue drugs.
研究领域:
运动生理学
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药理学
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神经科学
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DOI
PubMed
高影响因子
Cell Chemical Biology
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2017
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IF 0
Yongliang Xia,Feifei Luo,Yanfang Shang,Peilin Chen,Yuzhen Lu,Chengshu Wang
Summary Cordycepin (COR) and pentostatin (PTN) are adenosine analogs with related bioactivity profiles as both mimic adenosine and can inhibit some of the processes that are adenosine dependent. Both COR and PTN are also natural products and were originally isolated from the fungus Cordyceps militaris and the bacterium Streptomyces antibioticus , respectively. Here, we report that not only is PTN produced by C. militaris but that biosynthesis of COR is coupled with PTN production by a single gene cluster. We also demonstrate that this coupling is an important point of metabolic regulation where PTN safeguards COR from deamination by inhibiting adenosine deaminase (ADA) activity. ADA is not inhibited until COR reaches self-toxic levels, at which point ADA derepression occurs allowing for detoxification of COR to 3′-deoxyinosine. Finally, we show that using our biosynthetic insights, we can engineer C. militaris to produce higher levels of COR and PTN.
研究领域:
真菌学
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生物化学
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药物开发
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DOI
Frontiers in Microbiology
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2018
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IF 4.019
Yong Tianqiao,Chen Shaodan,Xie Yizhen,Chen Diling,Su Jiyan,Shuai Ou,Jiao Chunwei,Zuo Dan
Recently, we've reported the anti-hyperuricemic effects of Cordyceps militaris. As a characteristic compound of C. militaris, we hypothesized that cordycepin may play a role in preventing hyperurecimia. Remarkably, cordycepin produced important anti-hyperuricemic actions, decreasing SUA (serum uric acid) to 216, 210, and 203 μmol/L (P < 0.01) at 15, 30, and 60 mg/kg in comparison of hyperuricemic control (337 μmol/L), closing to normal control (202 μmol/L). Elisa, RT-PCR and western blot analysis demonstrated that the actions may be attributed to its downregulation of uric acid transporter 1 (URAT1) in kidney. Serum creatinine levels and blood urine nitrogen and liver, kidney, and spleen coefficients demonstrated that cordycepin may not impact liver, renal, and spleen functions. In addition, we used computational molecular simulation to investigate the binding mechanism of cordycepin. Of which, van der Waals interaction dominated the binding. Residues TRP290, ARG17, ALA408, GLY411, and MET147 contributed mainly on nonpolar energy. This provided the theoretical guidance to rationally design and synthesis novel URAT1 inhibitors.
研究领域:
药理学
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生物化学
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分子生物学
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DOI
PubMed
高影响因子
JOURNAL OF FOOD PROCESSING AND PRESERVATION
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2015
·Vol. 40
·期 3
·447-452
·
IF 1.159
Jike Lu,Guofeng Gu,Limin Hao,Zenan Jin,Xu Wang
The characteristics and antioxidant activities of C ordyceps sobolifera polysaccharide (CSP) were investigated. Results from high-performance gel filtration chromatography showed that the average molecular weight of CSP was 1.53 × 10 4 kDa, while this polysaccharide was mainly composed of mannose, glucose and galactose in the molar ratio of 1.7:8.9:1 as determined by high-performance liquid chromatography after pre-column derivatization with 1-phenyl-3-methyl-5-pyrazolone. Fourier-transform infrared spectrum of CSP indicated the typical functional groups of polysaccharide. Antioxidant activity results showed that CSP had reducing power (OD700 was 0.87 at 1.5 mg/mL), and it also exhibited scavenging activities on hydroxyl (·OH scavenging rate was 47.6% at 5 mg/mL) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals (scavenging rate was 55.6% at 1 mg/mL) in a concentration-dependent manner. These results indicate that CSP has good in vitro antioxidant activity and can potentially be used for functional foods. Practical Applications C ordyceps sobolifera is a pricy traditional Chinese herb and it has been used in China for a long time. Polysaccharide extracted from C . sobolifera was characterized, and the antioxidant activities of this polysaccharide were investigated. The result may lay the foundation for the development of antioxidant functional foods from C . sobolifera .
研究领域:
食品科学
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生物化学
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高影响因子
MOLECULAR BIOTECHNOLOGY
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2024
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IF 2.4
Chen Ya,Zhu Congcong,Tai Zongguang,Lian Tianyan,Zhu Quangang,Chen Zhongjian
Apoptosis is a natural physiological process of programmed cell death. It is essential for maintaining the homeostasis of the body and the immune system. The dysfunction of apoptosis can lead to the development of autoimmune diseases. In psoriasis, the dysfunction of keratinocyte proliferation manifests as an impairment of apoptosis. Cordycepin is the major active component in cordyceps militaris and has pharmacological effects, including regulation of apoptosis. The pharmacological mechanism of Cordycepin in psoriasis remains unclear. In this study, bioinformatics analysis revealed that the mechanism may be associated with the p53 apoptotic pathway. Further, we confirmed in the experiments that cordycepin inhibited the interleukin (IL)-17A-induced proliferation of HaCaT cells and down-regulated the expression of proliferating cell nuclear antigen (PCNA) and Ki-67. Regulating the expression of apoptotic proteins BAX, Bcl-2, and p53 promote apoptosis. Further investigation of the upstream pathway of apoptosis revealed that cordycepin could normalize the abnormal p53-mouse double minute 2 (MDM2) feedback loop. In vivo results showed that the cordycepin gel could effectively improve imiquimod (IMQ)-induced psoriasis-like skin lesions in mice, and the p53-MDM2 pathway was verified at the protein level. In conclusion, the anti-psoriasis effect of Cordycepin and its potential mechanism have not been discussed in detail. However, our work supports the idea that Cordycepin can be further developed as an Active Pharmaceutical Ingredient (API) for the treatment of psoriasis.
研究领域:
药理学
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皮肤科
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分子生物学
·
免疫学
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产品关联
DOI
PubMed
高影响因子