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Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology最新文献

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Acetylcholinesterase Inhibitor-Based Nose‑to‑Brain Delivery of Donepezil‑Loaded Lipid Nanoemulsion for Alzheimer's Therapy. 基于乙酰胆碱酯酶抑制剂的多奈哌齐脂质纳米乳鼻脑递送治疗阿尔茨海默病
Chandan Mohanty, Mahendrakumar R Dubey, Saswati Panigrahi, Shubham Singh, Sanjesh Rathi, Junmoni Nath

Intranasal delivery offers a promising route for direct drug transport to the central nervous system, bypassing the blood-brain barrier and improving therapeutic outcomes in neurodegenerative diseases like Alzheimer's disease. Donepezil, a widely prescribed drug for Alzheimer's, suffers from poor oral bioavailability, delayed onset, and limited nootropic activity due to extensive systemic metabolism. To address these limitations, this study aimed to develop and optimize a Donepezil-loaded lipid-based nanoemulsion for enhanced nose-to-brain delivery. A Box-Behnken Design (BBD) was employed to optimize three formulation variables: drug-to-lipid ratio (1:2 to 1:6), surfactant concentration (1-2% w/v), and stirring speed (1500-2500 rpm), with their effects assessed on particle size, drug entrapment efficiency, and drug loading. Based on solubility and hydrophilic-lipophilic balance, Glyceryl Monostearate and Tween 80 were selected as excipients. Seventeen formulations were prepared and analyzed using Response Surface Methodology. The optimized formulation (Batch 18) exhibited a particle size of 160.12 nm, entrapment efficiency of 80.75%, and drug loading of 19.98%, with a desirability score of 0.977. Predicted and observed values were within ±5% variation, confirming model reliability with high Adjusted R² (>0.95), Predicted R² (>0.90), and a non-significant lack of fit (p > 0.05) by ANOVA. The optimized nanoemulsion showed enhanced brain-targeting efficiency and improved nootropic potential of Donepezil via the intranasal route, presenting a promising strategy for Alzheimer's therapy. However, the study was limited to in vitro assessments, and further in vivo pharmacokinetic, pharmacodynamic, and long-term safety evaluations are warranted to comprehensively establish its therapeutic potential.

鼻内给药是一种很有前途的途径,可以绕过血脑屏障,直接将药物输送到中枢神经系统,改善阿尔茨海默病等神经退行性疾病的治疗效果。多奈哌齐是一种广泛用于治疗阿尔茨海默病的处方药,由于广泛的全身代谢,口服生物利用度差、起效延迟和促智活性有限。为了解决这些限制,本研究旨在开发和优化一种装载多奈哌齐的脂质纳米乳,以增强鼻到脑的递送。采用Box-Behnken设计(BBD)对药脂比(1:2 ~ 1:6)、表面活性剂浓度(1 ~ 2% w/v)和搅拌速度(1500 ~ 2500 rpm) 3个配方变量进行优化,考察其对粒径、包载效率和载药量的影响。根据溶解度和亲水亲脂平衡,选择单硬脂酸甘油酯和Tween 80作为辅料。采用响应面法对17种配方进行了分析。优化后的配方(第18批)粒径为160.12 nm,包封效率为80.75%,载药量为19.98%,理想评分为0.977。预测值和实测值的差异在±5%以内,通过方差分析证实了模型的可靠性,校正R²(>0.95)、预测R²(>0.90)和非显著性拟合缺失(p > 0.05)。优化后的纳米乳具有更强的脑靶向效率,并能通过鼻内途径改善多奈哌齐的促智潜能,为阿尔茨海默病的治疗提供了一种有前景的策略。然而,该研究仅限于体外评估,需要进一步进行体内药代动力学、药效学和长期安全性评估,以全面确定其治疗潜力。
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引用次数: 0
CD3-Bispecific Monoclonal Antibodies: A Novel Therapeutic Approach for Complex and Multifactorial Diseases. cd3双特异性单克隆抗体:一种治疗复杂和多因素疾病的新方法。
Shubham Singh, Sanjesh Rathi, Sakshi Singh, Bhawna Sharma, Vivek Dwivedi

Monoclonal antibodies (mAbs) have witnessed significant advancements in recent years, offering promising therapeutic options for the management of complex and multifactorial diseases. Despite their success, conventional mAbs exhibit limitations such as restricted targeting capacity and suboptimal immune activation, which has driven the development of bispecific monoclonal antibodies (BsAbs) capable of engaging multiple antigens simultaneously. Among these, CD3-bispecific mAbs have emerged as a potent class of immunotherapeutics, capable of activating T cells and inducing T cell-mediated cytotoxicity against target cells, particularly in cancer immunotherapy. This review highlights several representative formats of BsAbs, elucidates their underlying mechanisms of action, and discusses current design strategies for CD3-bispecific mAbs. Emphasis is placed on optimizing their therapeutic efficacy while minimizing adverse effects, supported by recent drug development examples and clinical applications.

单克隆抗体(mab)近年来取得了重大进展,为复杂和多因素疾病的治疗提供了有希望的治疗选择。尽管取得了成功,但传统的单克隆抗体仍存在局限性,如靶向能力有限和免疫激活不理想,这推动了双特异性单克隆抗体(BsAbs)的发展,能够同时参与多种抗原。其中,cd3双特异性单克隆抗体已成为一类有效的免疫治疗药物,能够激活T细胞并诱导T细胞介导的细胞毒性对抗靶细胞,特别是在癌症免疫治疗中。本文重点介绍了几种具有代表性的单克隆抗体,阐明了它们的潜在作用机制,并讨论了目前cd3双特异性单克隆抗体的设计策略。重点放在优化其治疗效果,同时尽量减少不良反应,支持最近的药物开发实例和临床应用。
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引用次数: 0
Cancer Research in the 21st Century: Recent Advances and Future Perspectives. 21世纪的癌症研究:最新进展和未来展望。
Vrushali P Patole, Nirmala V Shinde, Siddhi M Chandak, Ashwini T Satalkar

Introduction: Cancer remains a major global health concern, accounting for nearly 10 million deaths annually. Despite its complexity and heterogeneity, significant advancements in cancer research over the past two decades have transformed the landscape of cancer diagnosis, treatment, and prevention. Notably, the integration of personalized medicine and technological innovations has led to more precise, effective, and individualized care strategies.

Materials: This review utilized peer-reviewed articles, clinical trial data, and recent meta-analyses published between 2015 and 2025. Major databases including PubMed, Scopus, and Web of Science were searched using keywords such as "cancer therapy," "personalized medicine," "cancer diagnostics," "immunotherapy," and "cancer prevention.

Methods: A systematic review approach was applied, focusing on studies that reported significant advancements in cancer treatment modalities (e.g., targeted therapy, immunotherapy), diagnostic technologies (e.g., liquid biopsy, AI-based imaging), and preventive strategies (e.g., vaccination, genetic screening). Articles were selected based on relevance, impact, and recency, with a preference for clinical studies and high-impact reviews.

Results: Emerging therapies such as immune checkpoint inhibitors, CAR-T cell therapy, and molecularly targeted agents have shown improved survival and response rates in several cancer types. Diagnostic innovations, including next-generation sequencing and non-invasive liquid biopsies, have enhanced early detection and monitoring of treatment response. Preventive measures, such as HPV and HBV vaccination and genetic risk profiling, have reduced the incidence of several preventable cancers. Personalized medicine approaches have enabled treatment decisions based on individual genetic and molecular profiles, leading to improved therapeutic outcomes and reduced adverse effects.

Discussion: The integration of genomics, artificial intelligence, and immunotherapy into oncology practice marks a shift toward precision medicine. While these advances have significantly improved patient care, challenges such as treatment resistance, access disparities, and the high cost of novel therapies remain. Continued interdisciplinary research, equitable healthcare policies, and investment in emerging technologies are essential to fully realize the benefits of modern cancer care.

导言:癌症仍然是一个主要的全球健康问题,每年造成近1000万人死亡。尽管癌症具有复杂性和异质性,但在过去二十年中,癌症研究取得了重大进展,改变了癌症诊断、治疗和预防的格局。值得注意的是,个性化医疗和技术创新的结合导致了更精确、有效和个性化的护理策略。材料:本综述利用了同行评议的文章、临床试验数据和2015年至2025年间发表的近期荟萃分析。主要数据库包括PubMed、Scopus和Web of Science,搜索关键词包括“癌症治疗”、“个性化医疗”、“癌症诊断”、“免疫治疗”和“癌症预防”。方法:采用系统综述方法,重点关注在癌症治疗方式(如靶向治疗、免疫治疗)、诊断技术(如液体活检、基于人工智能的成像)和预防策略(如疫苗接种、基因筛查)方面取得重大进展的研究。文章的选择基于相关性、影响和近时性,优先考虑临床研究和高影响的综述。结果:免疫检查点抑制剂、CAR-T细胞疗法和分子靶向药物等新兴疗法已经显示出在几种癌症类型中提高了生存率和应答率。诊断创新,包括下一代测序和非侵入性液体活检,加强了早期发现和监测治疗反应。预防措施,如人乳头瘤病毒和乙型肝炎病毒疫苗接种和遗传风险分析,减少了几种可预防癌症的发病率。个性化医疗方法使得基于个体遗传和分子谱的治疗决策成为可能,从而改善了治疗效果,减少了不良反应。讨论:将基因组学、人工智能和免疫疗法整合到肿瘤实践中,标志着精准医学的转变。虽然这些进展显著改善了患者护理,但诸如治疗耐药性、可及性差异和新疗法的高成本等挑战仍然存在。持续的跨学科研究、公平的医疗政策和对新兴技术的投资对于充分实现现代癌症治疗的好处至关重要。
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引用次数: 0
Golden Flaxseed (Linum Usitatissimum): Unveiling Its Botanical Marvels, Therapeutic Potentials, and Nanoscale Applications. 金亚麻籽(Linum Usitatissimum):揭示其植物奇迹,治疗潜力和纳米级应用。
Nirmala V Shinde, Nikita S Sahane, Sachin K Bhosale, Vrushali P Patole, Ashwini T Satalkar

Flax seeds, scientifically known as Linum usitatissimum, are nutrient-rich seeds with omega-3 fatty acids, lignans, and fiber. They offer diverse health benefits including cholesterol reduction, cardiovascular support, anti-inflammatory properties, and potential in combating chronic diseases like diabetes and cancer. Additionally, their anti-arrhythmic and anti-atherogenic properties benefit vascular health. Studying their botanical features, phytochemical composition, and pharmacological activities could lead to innovative medical treatments. Flax seeds, with their nutritional versatility, present a valuable addition to a balanced diet, potentially contributing to improved well-being and disease prevention. studies have demonstrated its effectiveness in the production of nanoparticles with enhanced pharmacological effects and potential applications in various biomedical fields. Therefore, the main purpose of this review is to explore the importantrole of L. usitatissimum as an important medicinal weed and to study its various pharmacological activities as well as the required chemical components.

亚麻籽,科学上被称为亚麻籽,是富含omega-3脂肪酸、木脂素和纤维的营养丰富的种子。它们提供多种健康益处,包括降低胆固醇、支持心血管、抗炎特性,以及对抗糖尿病和癌症等慢性疾病的潜力。此外,它们的抗心律失常和抗动脉粥样硬化特性有益于血管健康。研究它们的植物特征、植物化学成分和药理活性可以带来创新的医学治疗。亚麻籽营养丰富,是均衡饮食的宝贵补充,可能有助于改善健康和预防疾病。研究已经证明其在生产纳米颗粒方面的有效性,具有增强的药理作用和在各种生物医学领域的潜在应用。因此,本综述的主要目的是探讨白屈草作为一种重要的药用杂草的重要作用,并研究其各种药理活性和所需的化学成分。
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引用次数: 0
A Pharmacological Study of Shirisharishta and Its Antihistaminic Effects in Guinea Pigs with Reference to Urticaria. 白瑞香对豚鼠抗组胺作用的药理研究及对荨麻疹的参考。
Monarani Chaurasia, Praveena P Nair, Aparna Saxena

The effect of Shirisharishta on histamine-induced bronchospasm in guinea pigs was evaluated in this study. Guinea pigs were placed in a histamine chamber, and an aerosol of 0.5% histamine was introduced using a compressor and nebulizer. The antihistaminic activity of the compound formulation of Albizzia lebbeck bark, i.e., Shirisharishta, as well as the extracts of its individual Prakshepa Dravyas, was assessed against histamine aerosol-induced bronchospasm in guinea pigs. Additionally, a clinical trial of Shirisharishta was conducted on a group of patients suffering from urticaria, wherein its antiallergic effects were observed and compared to a standard treatment group. The study demonstrated promising antiallergic and bronchodilator activity of Shirisharishta, supporting its therapeutic potential in allergic and respiratory disorders.

本研究评价了百毒泻对豚鼠组胺性支气管痉挛的影响。将豚鼠置于组胺室中,使用压缩机和雾化器注入0.5%组胺的气雾剂。在豚鼠组胺气雾剂诱导的支气管痉挛中,评估了合合花小檗树皮(即Shirisharishta)的复方制剂及其单个Prakshepa Dravyas提取物的抗组胺活性。此外,对一组荨麻疹患者进行了Shirisharishta的临床试验,观察了其抗过敏效果,并与标准治疗组进行了比较。该研究表明,湿婆灵有良好的抗过敏和支气管扩张活性,支持其治疗过敏性和呼吸系统疾病的潜力。
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引用次数: 0
A Comprehensive Overview of Traditional Chinese Medicine (TCM). 《中医药综合概览》。
Roshan Kumar Dubey, Bablu Kumar

Traditional Chinese Medicine (TCM) represents a holistic approach to health and wellness that integrates ancient philosophies with diverse therapeutic modalities. Rooted in concepts of Yin-Yang balance, Qi (vital energy), and the Five Elements theory, TCM aims to harmonize the body, mind, and spirit to achieve optimal health outcomes. This review explores the historical development, philosophical foundations, diagnostic methods, and common practices within TCM. It highlights the integration of acupuncture, herbal medicine, dietary therapy, and mind-body practices as key components of TCM's therapeutic arsenal. Scientific perspectives on TCM emphasize ongoing research efforts to validate its efficacy, mechanisms of action, and integration into modern healthcare systems. Criticisms surrounding TCM include challenges related to scientific validation, safety concerns regarding herbal products, and cultural differences in healthcare practices. Despite these challenges, TCM continues to evolve with advancements in research methodologies, digital health technologies, and integrative medicine approaches. The future of TCM holds promise in personalized and preventive medicine, global standardization, and ethical practices, positioning it as a valuable contributor to comprehensive healthcare models worldwide.

传统中医(TCM)代表了一种全面的健康和保健方法,将古代哲学与多种治疗方式相结合。中医植根于阴阳平衡、气(生命能量)和五行理论的概念,旨在协调身体、思想和精神,以达到最佳的健康结果。本文综述了中医的历史发展、哲学基础、诊断方法和常见做法。它强调了针灸、草药、饮食疗法和身心实践的整合,作为中医治疗武器库的关键组成部分。中医的科学观点强调正在进行的研究工作,以验证其疗效、作用机制和与现代医疗保健系统的整合。对中医的批评包括与科学验证相关的挑战、草药产品的安全问题以及医疗保健实践中的文化差异。尽管存在这些挑战,但随着研究方法、数字健康技术和中西医结合方法的进步,中医仍在继续发展。中医的未来在个性化和预防医学、全球标准化和道德实践方面前景光明,将其定位为全球综合医疗模式的重要贡献者。
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引用次数: 0
Perspectives on Fecal Microbiota Transplantation: Uses and Modes of Administration. 粪便微生物群移植的前景:用途和给药方式。
Ruchi Tiwari, Anjali Paswan, Gaurav Tiwari, V Jaya Sankar Reddy, Mahesh Kumar Posa

Fecal microbiota Transplantation (FMT), often referred to as stool transplantation, fecal transfusion, and fecal bacteria therapy, is considered one of the most medical innovations of the 20th century. Fecal microbiota Transplantation entails filtering and dilution of a healthy donor's feces before injecting it into the recipient's digestive system. In China, it was first administered orally in the fourth century for diarrhea and food poisoning under the name "Yellow Soup." It has recently been widely employed in a variety of clinical settings, including cases of Clostridium difficile infection that are recurring and resistant. By replacing the unhealthy intestinal microbiota with a healthy bacterial community, the FMT treatment aims to enhance the intestinal flora. It also looks at neurological conditions where alterations in gut microbiota are prevalent. We have discussed FMT in the context of its use in conditions affecting the nerve system, such as neurological and other conditions (multiple sclerosis, Parkinson's disease, Alzheimer's disease, stroke, epilepsy, Amyotrophic lateral sclerosis, Tourette syndrome, neuropathic pain, Huntington's diseases, etc.), as well as the role of gut microbiota in many neurological disorders.

粪便微生物群移植(FMT)通常被称为粪便移植、粪便输血和粪便细菌治疗,被认为是20世纪最重要的医学创新之一。粪便微生物群移植需要过滤和稀释健康捐赠者的粪便,然后将其注射到接受者的消化系统。在中国,黄汤最早是在公元4世纪用于治疗腹泻和食物中毒,当时被称为“黄汤”。它最近被广泛应用于各种临床环境,包括难辨梭状芽胞杆菌感染复发和耐药的病例。通过用健康的细菌群落取代不健康的肠道微生物群,FMT治疗旨在增强肠道菌群。它还研究了肠道微生物群普遍改变的神经系统疾病。我们讨论了FMT在影响神经系统的疾病中的应用,如神经系统和其他疾病(多发性硬化症、帕金森病、阿尔茨海默病、中风、癫痫、肌萎缩侧索硬化症、妥瑞特综合征、神经性疼痛、亨廷顿病等),以及肠道微生物群在许多神经系统疾病中的作用。
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引用次数: 0
Unlocking the Potential of Sotagliflozin in Diabetes Mellitus targeting SGLT 1 & SGLT 2: A Comprehensive Review. 释放Sotagliflozin治疗糖尿病sglt1和sglt2的潜力:一项全面的综述。
Manoj Kumbhare, Siddhi Chandak, Arshad Shaikh, Sakshi Velhal, Aishwarya Dukare, Harshali Gode, Nishant Pagere, Bhagwan Ide

Sotagliflozin, a novel dual inhibitor of sodium-glucose cotransporters 1 and 2 (SGLT1/2), represents a promising therapeutic advancement for managing diabetes mellitus. By inhibiting SGLT1 in the small intestine and SGLT2 in the kidneys, sotagliflozin uniquely improves glycemic control through reduced postprandial glucose absorption and enhanced urinary glucose excretion. This dual mechanism has shown significant benefits for both type 1 and type 2 diabetes, including reduced insulin requirements, better glycemic control, weight loss, and improved cardiovascular and renal outcomes. Clinical trials have highlighted its potential to mitigate the risks of diabetic complications such as heart failure and chronic kidney disease. However, its use is associated with some side effects, including gastrointestinal disturbances, urinary tract infections, and an elevated risk of diabetic ketoacidosis. This review explores the chemistry, pharmacology, and therapeutic implications of sotagliflozin, emphasizing its unique dual-target approach and potential to address unmet needs in diabetes management.

Sotagliflozin是一种新型的钠-葡萄糖共转运蛋白1和2 (SGLT1/2)双重抑制剂,代表了治疗糖尿病的一个有希望的进展。通过抑制小肠中的SGLT1和肾脏中的SGLT2,索他列净通过减少餐后葡萄糖吸收和增强尿糖排泄来独特地改善血糖控制。这种双重机制对1型和2型糖尿病都有显著的益处,包括降低胰岛素需求、更好的血糖控制、体重减轻、改善心血管和肾脏预后。临床试验强调了其降低糖尿病并发症(如心力衰竭和慢性肾脏疾病)风险的潜力。然而,它的使用与一些副作用有关,包括胃肠道紊乱、尿路感染和糖尿病酮症酸中毒的风险增加。这篇综述探讨了sotagliflozin的化学、药理学和治疗意义,强调其独特的双靶点方法和解决糖尿病管理中未满足需求的潜力。
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引用次数: 0
A Brief Review on Transdermal Patches. 透皮贴剂研究综述。
Shubham Singh, Dharmendra Singh Rajput, Naveen Gupta, Bhawna Sharma, Sanjesh Rathi, Arjun Singh

Transdermal drug delivery system was presented to overcome the difficulties of drug delivery especially oral route. A transdermal patch is a medicated adhesive patch that is placed on the skin to deliver a specific dose of medication through the skin and into the bloodstream. It promotes healing to an injured area of the body. An advantage of a transdermal drug delivery route over other types of delivery system such as oral, topical, i.v., i.m., etc. is that the patch provides a controlled release of the medication into the patient, usually through either a porous membrane covering a reservoir of medication or through body heat melting thin layers of medication embedded in the adhesive. The main disadvantage to transdermal delivery systems stems from the fact that the skin is a very effective barrier, as a result, only medications whose molecules are small can easily penetrate the skin, so it can be delivered by this method. This review article describes the overall introduction of transdermal patches including type of transdermal patches, method of preparation of transdermal patches and factor affecting etc.

为了克服口服给药的困难,提出了经皮给药系统。透皮贴片是一种贴在皮肤上的药物贴片,通过皮肤将特定剂量的药物输送到血液中。它能促进身体受伤部位的愈合。透皮给药途径比其他类型的给药系统(如口服、局部、静脉注射、i.m.m等)的一个优点是,该贴片通常通过覆盖药物储存库的多孔膜或通过体热融化嵌入粘合剂中的薄层药物,将药物可控地释放到患者体内。透皮给药系统的主要缺点是皮肤是一个非常有效的屏障,因此,只有分子小的药物才能很容易地穿透皮肤,所以可以通过这种方法给药。本文对透皮贴剂的类型、制备方法、影响因素等进行了综述。
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引用次数: 0
Evaluation, Characterization of Antioxidant Activity for Novel Benzothiazole Derivatives. 新型苯并噻唑衍生物抗氧化活性的评价与表征。
Siddhi M Chandak, Manoj R Kumbhare

The present study focuses on the design, synthesis, in-silico studies, characterization, and evaluation of the antidiabetic activity of nitrogen and sulphur-containing heterocyclic compounds, specifically benzothiazole derivatives (2a-2e). The synthesized compounds were characterized using spectroscopic techniques such as IR, NMR, and mass spectrometry. Their biological activity was assessed through molecular docking studies, which revealed strong binding interactions with target proteins, with compound 2a exhibiting the highest docking score (-8.7). Swiss ADME analysis was performed to evaluate pharmacokinetic properties, indicating good drug-likeness and bioavailability. In vitro antidiabetic activity was assessed using the α-amylase inhibition method, where compounds 2a and 2e demonstrated significant inhibitory potential with IC₅₀ values of 22.95±2.50µg/mL and 27.80±3.00µg/mL, respectively. These findings suggest that benzothiazole derivatives, particularly compound 2a, hold promise as potential antioxidant agents, warranting further investigation for therapeutic applications.

本研究的重点是设计、合成、硅研究、表征和评价含氮和含硫杂环化合物的抗糖尿病活性,特别是苯并噻唑衍生物(2a-2e)。合成的化合物用红外光谱、核磁共振和质谱等光谱技术进行了表征。通过分子对接研究评估了它们的生物活性,发现它们与靶蛋白有很强的结合相互作用,其中化合物2a的对接评分最高(-8.7)。瑞士ADME分析评估药代动力学性质,表明良好的药物相似性和生物利用度。采用α-淀粉酶抑制法评估体外抗糖尿病活性,其中化合物2a和2e表现出显著的抑制潜力,IC₅₀值分别为22.95±2.50µg/mL和27.80±3.00µg/mL。这些发现表明,苯并噻唑衍生物,特别是化合物2a,有望成为潜在的抗氧化剂,值得进一步研究其治疗应用。
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引用次数: 0
期刊
Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology
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