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Arch Pharm Res 2022 Apr 27. Epub 2022 Apr 27.

School of Biological Science and Technology, University of Jinan, Jinan, 250022, China.

One new clerodane-type furanoditerpenoid tinosinoid A (1) and nine new nor-clerodane analogs tinosinoids B-J (2-10) have been isolated from the stems of Tinospora sinensis. The structures of the new compounds with absolute configurations have been elucidated by spectroscopic means, including MS, NMR and ECD techniques, as well as chemical correlation. Compound 1 is a rare sulfur-containing clerodane diterpenoid incorporating a 2-mercaptoethanol unit via a thioether bond, while compounds 4/5 and 9 represent two pairs of unusual equilibrium regioisomers through an interesting intramolecular transesterification. Read More

Arch Pharm Res 2022 Apr 21;45(4):263-279. Epub 2022 Apr 21.

Department of Internal Medicine, School of Medicine, Kyungpook National University, Daegu, 41944, Korea.

Although anti-angiogenic agents have been of limited use in the treatment of non-small cell lung cancer (NSCLC) until recently, further roles for the use of angiogenesis inhibition have emerged in the era of targeted therapy and immune checkpoint blockade. Given the shared common downstream signals of epidermal growth factor receptor (EGFR) and vascular endothelial growth factor (VEGF) with their complementary roles in tumorigenesis and tumor angiogenesis, the dual inhibition of EGFR and VEGF pathways represents a rational strategy to maximize clinical efficacy and overcome resistance in the treatment of EGFR-mutant NSCLC. VEGF-driven angiogenesis is a potent driver of immunosuppressive tumor microenvironment (TME), with the recruited immunosuppressive cells driving angiogenesis, highlighting the interplay between the tumor vasculature and the anticancer immunity. Read More

Arch Pharm Res 2022 Apr 20;45(4):280-293. Epub 2022 Apr 20.

Department of Infectious Diseases and Public Health, Jockey Club College of Veterinary Medicine, City University of Hong Kong, Hong Kong SAR, China.

Zika virus (ZIKV), an arbovirus of the Flaviviridae family, has emerged as a significant public health concern owing to its association with congenital abnormalities and severe neurological sequelae. Thus, there is an urgent need to develop effective therapeutic approaches to efficiently treat ZIKV infections. This study used phenotypic screening to identify a series of 1,2,4-oxadiazole derivatives that possess antiviral activity against ZIKV infection. Read More

Arch Pharm Res 2022 Apr 15;45(4):245-262. Epub 2022 Apr 15.

College of Pharmacy, Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul, 03760, Republic of Korea.

Synthetic mRNA has been considered as an emerging biotherapeutic agent for the past decades. Recently, the SARS-CoV-2 pandemic has led to the first clinical use of synthetic mRNA. mRNA vaccines showed far surpassing influences on the public as compared to other vaccine platforms such as viral vector vaccines and recombinant protein vaccines. Read More

Arch Pharm Res 2022 Apr 7;45(4):229-244. Epub 2022 Apr 7.

Department of Manufacturing Pharmacy, College of Pharmacy and Research Institute for Drug Development, Pusan National University, Busan, 46241, Republic of Korea.

Nonalcoholic fatty liver disease (NAFLD) is the hepatic manifestation of metabolic syndrome and has become prevalent in the adult population worldwide, given the ongoing obesity pandemic. NAFLD comprises several hepatic disorders, ranging from fatty liver to nonalcoholic steatohepatitis (NASH), cirrhosis, and carcinoma. Excessive fat accumulation in the liver can induce the development of fatty liver, whereas the progression of fatty liver to NASH involves various complex factors. Read More

Arch Pharm Res 2022 Apr 7;45(4):205-228. Epub 2022 Apr 7.

Center of Excellence for Advanced Materials Research, King Abdulaziz University, Jeddah, 21589, Saudi Arabia.

For decades, the use of secondary metabolites of various herbs has been an attractive strategy in combating human diseases. Rosmarinic acid (RA) is a bioactive phenolic compound commonly found in plants of Lamiaceae and Boraginaceae families. RA is biosynthesized using amino acids tyrosine and phenylalanine via enzyme-catalyzed reactions. Read More

Arch Pharm Res 2022 Mar 25;45(3):159-173. Epub 2022 Mar 25.

College of Pharmacy, Pusan National University, 2, Busandaehak-ro 63beon-gil, Geumjeong-gu, Busan, 48434, Republic of Korea.

Renal fibrosis is defined by excessive extracellular matrix (ECM) accumulation and is associated with a decreased kidney function. Increased inflammation and infiltration of inflammatory cells are the key features of renal fibrosis development; however, the mechanism of how inflammation starts is still un-known. Here, we show that the activation of epithelial Protease-activating receptor 2 (PAR2) signaling plays an important role in the initiation of inflammation via increased chemokine expression and inflammatory cell induction. Read More

Arch Pharm Res 2022 Mar 24;45(3):174-184. Epub 2022 Mar 24.

College of Pharmacy, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon, South Korea.

Ginsenoside-Rh1 (Rh1) is a ginseng-derived compound that has been reported to exert anticancer effects by regulating cell cycle arrest and apoptosis according to reactive oxygen species (ROS) production. However, the effects of Rh1 on mitochondrial dysfunction are involved in triple negative breast cancer (TNBC) cell apoptosis, and the related molecular mechanisms remain unknown. Rh1 treatment induced cell toxicity less than 50% at 50 μM. Read More

Arch Pharm Res 2022 Mar 21;45(3):123-141. Epub 2022 Mar 21.

College of Pharmacy, Chung-Ang University, Seoul, 06974, Republic of Korea.

The gene amplification of human epidermal growth factor receptor 2 (HER2) plays an essential role in the proliferation and progression of several cancers. However, HER2 inhibitors such as lapatinib strongly suppress wild-type EGFR, resulting in severe adverse effects. Therefore, there is an unmet need for highly selective HER2 inhibitors. Read More

Arch Pharm Res 2022 Mar 18;45(3):185-204. Epub 2022 Mar 18.

Evidence-Based and Clinical Research Laboratory, Department of Health, Social and Clinical Pharmacy, College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea.

This systematic review and meta-analysis assessed the antidiabetic effect of pharmaconutrients as an add-on in type 2 diabetes mellitus patients by pooling data from currently available randomized controlled trials (RCTs). Data sources included the PubMed and EMBASE, Cochrane Central Register of Controlled Trials. RCTs reporting changes in glycosylated hemoglobin (HbA1c), fasting blood glucose (FBG), or homeostasis model assessment of insulin resistance (HOMA-IR) levels following add-on pharmaconutritional therapies for T2DM patients consuming antidiabetic drugs were targeted. Read More

Arch Pharm Res 2022 Mar 4;45(3):142-158. Epub 2022 Mar 4.

Pharmacology and Toxicology Department, Faculty of Pharmacy, Mansoura University, El Gomhoria Street, Eldakahlia, 35516, Egypt.

The current study aims at repurposing the anti-arthritic drug diacerein (DCN) for the treatment of acetaminophen hepatotoxicity and investigating the potential underlying mechanisms. Mice were randomly divided into six groups receiving either no treatment (control group), 20 mg/kg DCN i.p, 400 mg/kg acetaminophen i. Read More

Arch Pharm Res 2022 Feb 24;45(2):105-113. Epub 2022 Feb 24.

School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.

Phenalenone derivatives sourced from fungi are polyketides that have attracted significant interest because of their diverse chemical structures and potential bioactivities. As part of our ongoing quest to discover novel natural products with biological properties from diverse natural resources, three unreported phenalenone derivatives (1-3), named ent-12-methoxyisoherqueinone (1), (-)-scleroamide (2), and (+)-scleroamide (3), together with four known phenalenone derivatives, ent-atrovenetinone (4), isoherqueinone (5), herqueinone (6), and ent-peniciherquinone (7) were isolated from the Hawaiian soil fungus Penicillium herquei FT729, collected on the Big Island, Hawaii. Compounds 2 and 3 were enantiomers, which were separated using a chiral-phase HPLC column, which provided optically pure compounds 2 and 3. Read More

Arch Pharm Res 2022 Jan 7;45(1):29-37. Epub 2022 Feb 7.

College of Pharmacy, Keimyung University, 1095 Dalgubeol-daero, Dalseo-gu, Daegu, 42601, Republic of Korea.

Improving the aqueous solubility of poorly soluble compounds have been a major issue in the pharmaceutical industry. In the present study, binary amorphous solid dispersions (SDs) of Coenzyme Q10 (CoQ), a biopharmaceutics classification system (BCS) II compound and Soluplus were prepared to enhance the solubility and pharmacokinetic properties compared to crystalline CoQ. SDs were prepared with different ratios of CoQ and Soluplus (1:3, 1:5, and 1:7) using spray drying technology, and the physicochemical properties of the SDs were evaluated. Read More

Arch Pharm Res 2022 Feb 31;45(2):63-89. Epub 2022 Jan 31.

Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Padjadjaran, Jatinangor, 45363, Sumedang, West Java, Indonesia.

This study aims to analyze the ethnobotanical, chemical, and biological activities of triterpenoid compounds isolated from the Dysoxylum genus of the Meliaceae family between 1974 and 2021. The species are mainly distributed in Africa, Asia, and Australia, and used as a traditional medicine to treat various diseases. Triterpenoid was first isolated in 1976 and as tetranortriterpenoid or limonoid, it was named dysobinin. Read More

Arch Pharm Res 2022 Feb 30;45(2):90-104. Epub 2022 Jan 30.

Institute of Pharmaceutical Research and Development, College of Pharmacy, Wonkwang University, Iksan, 54538, Republic of Korea.

Penicillium is a rich source of bioactive compounds. Among all Penicillium species, Penicillium oxalicum has been reported to produce various types of secondary metabolites, including alkaloids, phenolics, and tetrahydroxanthone dimeric compounds, exhibiting many pharmacological effects, such as antiviral, antibacterial, and cytotoxic activities. Three secondary metabolites were isolated from a fermented culture of the sponge-associated fungal strain P. Read More

Arch Pharm Res 2022 Jan 20;45(1):11-28. Epub 2022 Jan 20.

Department of Pharmacology, Research Institute for Basic Medical Science, School of Medicine, CHA University, Cha Bio Complex, 335 Pangyo, Bundang-gu, Seongnam-si, Gyeonggi-do, 13488, Republic of Korea.

Atopic dermatitis (AD) and mood disorder comorbidities are typical, but the exact mechanism underlying their interplay has not been clarified. In this study, we aimed to identify the possible mechanisms of anxiety/depressive-like behaviors observed in AD, focusing on microglia. AD was induced by Dermatophagoides farinae body extract (Dfb) in NC/Nga mice and anxiety/depressive-like behaviors were analyzed by behavioral assessments such as open field test (OFT), tail suspension test (TST), sucrose preference test (SPT), and social interaction. Read More

Arch Pharm Res 2022 Jan 4;45(1):51-62. Epub 2022 Jan 4.

College of Pharmacy, Chung-Ang University, Seoul, 06974, Republic of Korea.

Asian sand dust (ASD), which mainly originates in China and Mongolia in the spring and blows into Korea, can exacerbate respiratory and immunological diseases. This study aims to observe effects of co-exposure to ASD on ovalbumin (OVA)-induced asthmatic lung inflammation and of treatment with a phosphodiesterase 7 (PDE7) inhibitor in a mouse model. The challenge with OVA increased airway hyperresponsiveness (AHR) and inflammatory cell infiltration into the lung tissue. Read More

Arch Pharm Res 2022 Feb 24;45(2):114-121. Epub 2021 Dec 24.

School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.

Glipizide is a second-generation sulfonylurea antidiabetic drug. It is principally metabolized to inactive metabolites by genetically polymorphic CYP2C9 enzyme. In this study, we investigated the effects of CYP2C9*3 and *13 variant alleles on the pharmacokinetics and pharmacodynamics of glipizide. Read More

Arch Pharm Res 2021 Nov 15;44(11):903-986. Epub 2021 Dec 15.

Chemistry of Natural Compounds Department, National Research Centre, El-Bohouth Street, Giza-Dokki, 12622, Egypt.

Sophora is deemed as one of the most remarkable genera of Fabaceae, and the third largest family of flowering plants. The genus Sophora comprises approximately 52 species, 19 varieties, and 7 forms that are widely distributed in Asia and mildly in Africa. Sophora species are recognized to be substantial sources of broad spectrum biopertinent secondary metabolites namely flavonoids, isoflavonoids, chalcones, chromones, pterocarpans, coumarins, benzofuran derivatives, sterols, saponins (mainly triterpene glycosides), oligostilbenes, and mainly alkaloids. Read More

Arch Pharm Res 2022 Jan 14;45(1):1-10. Epub 2021 Dec 14.

College of Pharmacy, Chungbuk National University, 194-21, Osongsaengmyung-1, Heungdeok, Cheongju, Chungbuk, 28160, Republic of Korea.

The susceptibility of cancer cells to natural killer (NK) cell-mediated cytotoxicity depends on the balance of activating and inhibitory ligands expressed on their surface. Although many types of cancer cells are killed by NK cells, non-small-cell lung cancer (NSCLC) cells are relatively resistant to NK cell-mediated cytotoxicity. In this study, we showed that several NSCLC cell lines have differential sensitivity to NK cell-mediated cytotoxicity: NCI-H522 cells were highly sensitive, but A549, NCI-H23, NCI-H1915, and NCI-H1299 were resistant. Read More

Arch Pharm Res 2021 Dec 24;44(12):1109-1119. Epub 2021 Nov 24.

School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.

Candesartan cilexetil is an angiotensin II receptor blocker and it is widely used to treat hypertension and heart failure. This drug is a prodrug that rapidly converts to candesartan after oral administration. Candesartan is metabolized by cytochrome P450 2C9 (CYP2C9) enzyme or uridine diphosphate glucurinosyltransferase 1A3, or excreted in an unchanged form through urine, biliary tract and feces. Read More

Arch Pharm Res 2021 Dec 22;44(12):1076-1090. Epub 2021 Nov 22.

School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.

Meloxicam, a non-steroidal anti-inflammatory drug, is used for the treatment of rheumatoid arthritis and osteoarthritis. Cytochrome P450 (CYP) 2C9 and CYP3A4 are major and minor enzymes involved in the metabolism of meloxicam. Impaired enzyme activity of CYP2C9 variants increases the plasma exposures of meloxicam and the risk of adverse events. Read More

Arch Pharm Res 2022 Jan 19;45(1):38-50. Epub 2021 Nov 19.

College of Pharmacy, Yeungnam University, Gyeongsan, Republic of Korea.

Adiponectin, an adipose tissue-derived hormone, exhibits a modulatory effect on cell death/survival and possesses potent anti-inflammatory properties. However, the underlying molecular mechanisms remain elusive. Sestrin2, a stress-inducible metabolic protein, has shown cytoprotective and inflammation-modulatory effects under stressful conditions. Read More

Arch Pharm Res 2021 Nov 13;44(11):1024. Epub 2021 Nov 13.

School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.

Arch Pharm Res 2021 Dec 10;44(12):1062-1075. Epub 2021 Nov 10.

College of Pharmacy, Keimyung University, 1095 Dalgubeil-daero, Daegu, 42601, South Korea.

Histone deacetylase 6 (HDAC6) is a promising target for cancer treatment because it regulates cell mobility, protein trafficking, cell growth, apoptosis, and metastasis. However, the mechanism of HDAC6-induced anticancer drug resistance is unclear. In this study, we evaluated the anticancer effect of ACY-241, an HDAC6-selective inhibitor, on erlotinib-resistant pancreatic cancer cells that overexpress HDAC6. Read More

Arch Pharm Res 2021 Nov 9;44(11):1025-1036. Epub 2021 Nov 9.

School of Pharmacy, Health Science Center, Xi'an Jiaotong University, No.76, Yanta West Street, #54, Xi'an, 710061, Shaanxi Province, People's Republic of China.

Hepatocellular carcinoma (HCC) is one of the most common tumor types globally. Despite the progress made in surgical procedures and therapeutic options, HCC remains a considerable cause of cancer-related mortality. In this study, we investigated the antitumor effects of sanguinarine (Sang) on HCC and its potential mechanisms. Read More

Arch Pharm Res 2021 Nov 9;44(11):1037-1049. Epub 2021 Nov 9.

School of Pharmacy, Sungkyunkwan University, Suwon, 16419, Republic of Korea.

Tamsulosin, a selective [Formula: see text]-adrenoceptor blocker, is commonly used for alleviation of lower urinary tract symptoms related to benign prostatic hyperplasia. Tamsulosin is predominantly metabolized by CYP3A4 and CYP2D6 enzymes, and several studies reported the effects of CYP2D6 genetic polymorphism on the pharmacokinetics of tamsulosin. This study aims to develop and validate the physiologically based pharmacokinetic (PBPK) model of tamsulosin in CYP2D6*wt/*wt, CYP2D6*wt/*10, and CYP2D6*10/*10 genotypes, using Simcyp® simulator. Read More

Arch Pharm Res 2021 Nov 9;44(11):987-1011. Epub 2021 Nov 9.

Fujian Provincial Key Laboratory of Tumor Biotherapy, Fujian Cancer Hospital, Fujian Medical University Cancer Hospital, Fuzhou, 350014, China.

In recent years, immunotherapy has emerged as a novel antitumor strategy in addition to traditional surgery, radiotherapy and chemotherapy. It uniquely focuses on immune cells and immunomodulators in the tumor microenvironment and helps eliminate tumors at the root by rebuilding the immune system. Despite remarkable breakthroughs, cancer immunotherapy still faces many challenges: lack of predictable and prognostic biomarkers, adverse side effects, acquired treatment resistance, high costs, etc. Read More

Arch Pharm Res 2021 Dec 9;44(12):1091-1108. Epub 2021 Nov 9.

BRL & BK-4th Team, College of Pharmacy, The Catholic University of Korea, 43, Jibong-ro, Wonmi-gu, Bucheon-si, Gyeonggi-do, 14662, Republic of Korea.

Resolution to chemoresistance is a major challenge in patients with advanced-stage malignancies. Thus, identification of action points and elucidation of molecular mechanisms for chemoresist human cancer are necessary to overcome this challenge. In this study, we provide important evidence that kaempferol targeting RSKs might be a strategy to reduce the oxaliplatin-resistant colon cancer cells. Read More

Arch Pharm Res 2021 Dec 7;44(12):1051-1061. Epub 2021 Nov 7.

College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon, South Korea.

Vascular smooth muscle cell (VSMC) proliferation and migration are critical events that contribute to the pathogenesis of vascular diseases such as atherosclerosis, restenosis, and hypertension. Recent findings have revealed that VSMC phenotype switching is associated with metabolic switch, which is related to the role of mitochondria. Mitochondrial dynamics are directly associated with mitochondrial function and cellular homeostasis. Read More