ARCHIVES OF PHARMACAL RESEARCH 是韩国药学会的官方期刊，自 1976 年开始出版。ARCHIVES OF PHARMACAL RESEARCH 是一本跨学科期刊，致力于发表药物发现、药物开发、和药物行动，以提供关于药物和候选药物的基本和新颖的信息。

The Archives of Pharmacal Research is the official journal of the Korean Pharmaceutical Society, published since 1976. This interdisciplinary journal focuses on research in drug discovery, drug development, and drug action, aiming to provide fundamental and novel information about drugs and drug candidates.

《Archives of Pharmacal Research》是韩国药学会的官方期刊，自1976年开始出版。该期刊是一份跨学科的学术刊物，专注于药物发现、药物开发和药物作用的研究，旨在提供关于药物及其候选药物的基础和新颖的信息。

Archives of Pharmacal Research

In previous studies, several isoindolin-1-one analogs that exhibited significant anti-tobacco mosaic virus (anti-TMV) activities were isolated from Nicotiana tabacum. Since gene-editing mutants provide a new sample for the discovery of active metabolites, we focused on the stems of YN-18-23 (a mutant N. tabacum for gene editing with the alkaloid metabolic pathway cultivated by Yunnan Tobacco Company), which led to the isolation of four new (1-4) and four known (5-8) isoindolin-1-ones. To the best of our knowledge, nicindole C (3) is the first subclass of isoindolin-1-one bearing a pentacyclic ketone, while nicindole D (4) is the first example of isoindolin-1-one bearing a methyl-pyridin-2-(1H)-one moiety. Compounds 1-4 were tested for their anti-TMV activities, and the results revealed that compounds 1, 3, and 4 exhibited high anti-TMV activities at concentrations of 20 μM with inhibition rates of 48.6, 42.8, and 71.5%, respectively. These rates are higher than the inhibition rate of the positive control (33.2%). The mechanistic study of compound 4, which had the highest anti-TMV activity revealed that increased potentiation of defense-related enzyme activities and downregulation of expression of the NtHsp70 protein may induce resistance in tobacco against the viral pathogen TMV. Molecular docking studies also revealed that the isoindolin-1-one substructure is fundamental for anti-TMV activity. The methyl-pyridin-2-(1H)-one moiety in compound 4 and the 2-oxopropyl groups in compounds 1 and 3 at the N-2 position may increase inhibitory activities. This study of the structure-activity relationship is helpful for finding new anti-TMV activity inhibitors. To study whether the isoindolin-1-ones have broader antiviral activities, compounds 1-4 were also tested for their anti-rotavirus activities. Compound 4 exhibited high anti-rotavirus activity with a therapeutic index (TI) value of 20.7. This TI value is close to that of the positive control (20.2).

Guang-Yu Yang

Jia-Meng Dai

Zhen-Jie Li

Jin Wang

Feng-Xian Yang

Xin Liu

Jing Li

Qian Gao

Xue-Mei Li

Yin-Ke Li

Wei-Guang Wang

Min Zhou

Qiu-Fen Hu

Archives of pharmacal research

Arch Pharm Res

Isoindolin-1-ones from the stems of Nicotiana tabacum and their antiviral activities.

烟草茎中的异吲哚啉-1-酮及其抗病毒活性。

A series of flavonoids (1-14) was isolated from the roots of Sophora flavescens. We evaluated their ability to inhibit both microbial growth and sortase A, an enzyme that plays a key role in cell wall protein anchoring and virulence in Staphylococcus aureus. Most prenylated flavonoids (7-13) displayed potent inhibitory activity against gram-positive and gram-negative bacteria except E. coli, with minimum inhibitory concentrations values ranging from 4.40 to 27.7 μM, and weak or no activity against fungal strains tested. Kurarinol (6) was a potent inhibitor of sortase A, with an IC(50) value of 107.7 ± 6.6 μM. A preliminary structure-activity relationship, including essential structural requirements, is described.

Ikhoon Oh

Woo-Young Yang

Soon-Chun Chung

Tae-Yoon Kim

Ki-Bong Oh

Jongheon Shin

In vitro sortase A inhibitory and antimicrobial activity of flavonoids isolated from the roots of Sophora flavescens.

槐角根中分离的黄酮类化合物的体外Sortase A抑制及抗菌活性研究。

Obesity is one of the worldwide prevalent disease caused by the imbalance between food intake and energy expenditure. Over a 100 years of research demonstrate that hypothalamus is the critical brain region regulating energy homeostasis, and evidences suggest the participation of non-neuronal populations such as astrocytes and microglia in the regulation of energy homeostasis. Recently, fat-rich diet induced hypothalamic inflammation has been found to deregulate the energy homeostasis, leading to the insulin resistance, glucose intolerance, and obesity. Several underlying mechanisms have been proposed, yet compelling evidences require further elucidations. This review discusses the up to date proposed mechanisms by which fat-rich diet induces hypothalamic inflammation and obesity.

Jichang Seong

Jung Yun Kang

Ji Su Sun

Ki Woo Kim

Hypothalamic inflammation and obesity: a mechanistic review.

下丘脑炎症与肥胖：机制综述。

Drug discovery utilizes chemical biology and computational drug design approaches for the efficient identification and optimization of lead compounds. Chemical biology is mostly involved in the elucidation of the biological function of a target and the mechanism of action of a chemical modulator. On the other hand, computer-aided drug design makes use of the structural knowledge of either the target (structure-based) or known ligands with bioactivity (ligand-based) to facilitate the determination of promising candidate drugs. Various virtual screening techniques are now being used by both pharmaceutical companies and academic research groups to reduce the cost and time required for the discovery of a potent drug. Despite the rapid advances in these methods, continuous improvements are critical for future drug discovery tools. Advantages presented by structure-based and ligand-based drug design suggest that their complementary use, as well as their integration with experimental routines, has a powerful impact on rational drug design. In this article, we give an overview of the current computational drug design and their application in integrated rational drug development to aid in the progress of drug discovery research.

Stephani Joy Y Macalino

Vijayakumar Gosu

Sunhye Hong

Sun Choi

Role of computer-aided drug design in modern drug discovery.

计算机辅助药物设计在现代药物发现中的作用。

Gastrodia elata Blume is a well-known traditional Chinese medicine that is mainly used to treat diseases related to the nervous system, such as stroke, epilepsy, and headache. Gastrodin is the main bioactive component of Gastrodia elata Blume, and studies have shown that it has extensive pharmacological activity. This narrative review aims to systematically review relevant studies on the pharmacological effects of gastrodin to provide researchers with the latest and most useful information. Studies have shown that gastrodin has prominent neuroprotective effects and can treat or improve epilepsy, Tourette syndrome, Alzheimer's disease, Parkinson's disease, emotional disorders, cerebral ischemia-reperfusion injury, cognitive impairment, and neuropathic pain. Gastrodin can also improve myocardial hypertrophy, hypertension, and myocardial ischemia-reperfusion injury. In addition, gastrodin can mitigate liver, kidney, and bone tissue damage caused by oxidative stress and inflammation. In short, gastrodin is expected to treat many diseases, and it is worth investing more effort in research on this compound.

Guirong Xiao

Rong Tang

Nan Yang

Yanhua Chen

Review on pharmacological effects of gastrodin.

天麻素药理作用综述。

Neurological disorders, encompassing conditions such as Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), and amyotrophic lateral sclerosis (ALS), pose a significant global health challenge, affecting millions worldwide. With an aging population and increased life expectancy, the prevalence of these disorders is escalating rapidly, leading to substantial economic burdens exceeding trillions of dollars annually. Animal models play a crucial role in understanding the underlying mechanisms of these disorders and developing effective treatments. Various species, including rodents, non-human primates, and fruit flies, are utilized to replicate specific aspects of human neurological conditions. However, selecting the ideal animal model requires careful consideration of its proximity to human disease conditions and its ability to mimic disease pathobiology and pharmacological responses. An Animal Model Quality Assessment (AMQA) tool has been developed to facilitate this selection process, focusing on assessing models based on their similarity to human conditions and disease pathobiology. Therefore, integrating intrinsic and extrinsic factors linked to the disease into the study's objectives aids in constructing a biological information matrix for comparing disease progression between the animal model and human disease. Ultimately, selecting an ideal animal disease model depends on its predictive, face, and construct validity, ensuring relevance and reliability in translational research efforts.

Shrawani Lamichhane

Jo-Eun Seo

Ji Hoon Jeong

Sooyeun Lee

Sangkil Lee

Ideal animal models according to multifaceted mechanisms and peculiarities in neurological disorders: present and challenges

根据多方面机制和神经系统疾病特点的理想动物模型：现状与挑战

Hypericum beanii, a traditional folk medicine plant, has been employed in treating various inflammation-related diseases. In this study, three new prenylated xanthones, named beanigenin A (1), beanigenin B (2), and beanigenin C (3), along with twenty-five known compounds (4-28), were isolated from the aerial parts of H. beanii. The new xanthones were elucidated based on modern spectroscopic experiments, including nuclear magnetic resonance spectroscopy (NMR) techniques, high-resolution electrospray ionization mass spectroscopy (HR-ESI-MS), and electronic circular dichroism (ECD). All the compounds were evaluated for their anti-inflammatory effects by measuring their inhibitory effect on nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophages. Our findings showed that compounds 1-10, 12, 14, 21-23, 26, and 28 displayed significant anti-inflammatory effects, with IC50 values ranging from 0.82 to 9.71 μM. The MOE software was utilized to conduct an in silico evaluation of the potential inhibitory activity of the three new xanthones against inducible NO synthase (iNOS) and cyclooxygenase 2 (COX-2) proteins. The results indicated that the three new xanthones demonstrated a high binding affinity with both iNOS and COX-2 proteins.

Wei Ma

Fu-Cai Ren

Xue-Ru Wang

Ning Li

Three new xanthones and other anti-inflammatory components from the aerial parts of Hypericum beanii

三新黄酮类化合物及贯叶连翘地上部分的其它抗炎成分

The specific binding of a drug to the receptor is a prerequisite for its action. The equilibrium dissociation constant (KD) is an important parameter for measuring the strength of drug-receptor interactions. Cell membrane chromatography (CMC) is a powerful way to determine the KD value; however, the common disadvantage is that the attenuation of biological activity with the analysis process leads to corresponding errors in comparing KD values of a series of drugs. Therefore, it is of practical significance to analyze the relative KD values of drugs for the same membrane receptor under the same conditions. We developed a CMC relative competitive method to determine the relative KD values of drugs through simultaneous injection of the control compound and analyte in each analysis, circumventing the error in KD values of drugs due to the attenuation of the biological activity of the CMC column. The results showed that the KD values of CD147 antagonists and MRGPRX2 agonists determined using the CMC relative competitive method correlated well with the KD values obtained via frontal analysis and stepwise frontal method using the CD147h (MRGPRX2h)/CMC system. Critically, the biological activities of the CD147 antagonists and MRGPRX2 agonists were significantly correlated with KD values measured using the CMC relative competitive method. Therefore, the CMC relative competitive method can accurately and efficiently evaluate the relative KD values of drugs and effectively predict the differences in pharmacological activity between a series of drugs, which has important guiding significance in the development of targeted drugs.

Panpan Lei

Weina Ma

Jiapan Gao

Bingxi Ren

Xiaoyu Ma

Yuxiu Zhang

Xinyue Su

Jinna Liang

Langchong He

Cell membrane chromatography relative competitive method for the accurate determination of relative KD values of drug-receptor interactions

细胞膜色谱相对竞争法用于药物-受体相互作用相对KD值的准确测定

Sleep deprivation or sleep loss, a prevalent issue in modern society, is linked to cognitive impairment, leading to heightened risks of errors and accidents. Chronic sleep deprivation affects various cognitive functions, including memory, attention, and decision-making, and is associated with an increased risk of neurodegenerative diseases, cardiovascular issues, and metabolic disorders. This review examines the potential of β-caryophyllene, a dietary non-psychotropic cannabinoid, and FDA-approved flavoring agent, as a therapeutic solution for sleep loss-induced cognitive impairment. It highlights β-caryophyllene's ability to mitigate key contributors to sleep loss-induced cognitive impairment, such as inflammation, oxidative stress, neuronal death, and reduced neuroplasticity, by modulating various signaling pathways, including TLR4/NF-κB/NLRP3, MAPK, Nrf2/HO-1, PI3K/Akt, and cAMP/PKA/CREB. As a naturally occurring, non-psychotropic compound with low toxicity, β-caryophyllene emerges as a promising candidate for further investigation. The review underscores the therapeutic potential of β-caryophyllene for sleep loss-induced cognitive impairment and provides mechanistic insights into its action on crucial pathways, suggesting that β-caryophyllene could be a valuable addition to strategies aimed at combating cognitive impairment and other health issues due to sleep loss.

Cher Ryn Lim

Satoshi Ogawa

Yatinesh Kumari

Exploring β-caryophyllene: a non-psychotropic cannabinoid's potential in mitigating cognitive impairment induced by sleep deprivation

探索β-石竹烯：一种非精神活性大麻素在缓解睡眠剥夺引起的认知障碍中的潜力

The recent resurgence of traditional medicines, driven by a renewed interest in the medicinal use of plant extracts, has garnered significant scientific attention for their therapeutic efficacy in treating a wide range of diseases. Glycyrrhiza species, commonly known as licorice, are widely recognized both as herbal remedies and as natural sweeteners. Among these, Glycyrrhiza uralensis stands out for its exceptional therapeutic potential, particularly in enhancing muscle regeneration, slowing muscle aging, and promoting skeletal muscle myogenesis. This review explores the traditional uses and biological effects of G. uralensis, highlighting the biological significance of its bioactive constituents, such as saponins and flavonoids. The hepatoprotective, antibacterial, antioxidant, anticancer, antidiabetic, antiobesity, anti-inflammatory, skeletal muscle-enhancing and cardiovascular effects of G. uralensis are reviewed, along with its toxicity and safety profile. Additionally, we propose directions for future clinical and scientific investigations, advocating for using G. uralensis as a natural therapeutic agent. The primary aim of this review is to contribute to the incorporation of this ancient medicine into modern clinical practice.

Sibhghatulla Shaikh

Khurshid Ahmad

Jeong Ho Lim

Syed Sayeed Ahmad

Eun Ju Lee

Inho Choi

Biological insights and therapeutic potential of Glycyrrhiza uralensis and its bioactive compounds: an updated review

甘草（Glycyrrhiza uralensis）及其生物活性化合物的生物学见解与治疗潜力：最新综述

Abbreviation	Arch. Pharm. Res.
Journal Impact	6.86
Quartiles(Global)	PHARMACOLOGY & PHARMACY(Q1)

ISSN	0253-6269, 1976-3786
h-index	105

Publication Information	Publisher: Pharmaceutical Society of Korea，Publishing cycle: Monthly，Journal Type: journal，Open Access Journals: No
Basic data	Year of publication: 1978，Proportion of original research papers: 55.00%，Self Citation Rate:7.20%， Gold OA Rate: 9.24%
Average review cycle	网友分享经验：平均4.0个月
Average recruitment ratio	网友分享经验：约50%

Archives of Pharmacal Research

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