Medicinal Chemistry and Pharmaceutics Commons^™

Ping-Chong-Jiang-Ni Formula Effectively Inhibits Migration And Invasion Of Endometriosis 12z Cell Line Via Trip13, Jiahua Peng, Shuzhen Liu, Yunxiang Xie, Min Xiao, Chichiu Wang, Ruining Liang

Journal of Food and Drug Analysis

The Ping-Chong-Jiang-Ni Formula (PCJNF), a compound of Traditional Chinese Medicine (TCM), has demonstrated remarkable clinical effectiveness and is widely utilized in the treatment of endometriosis (EMs). Previous studies have shown that PCJNF inhibits the proliferation and induces the apoptosis of ectopic endometrial stromal cells (EESCs) by modulating the JNK signaling pathway. In our most recent study, published in January 2024, we found that PCJNF effectively alleviates EMs-associated pain by reducing inflammatory mediators, including tumor necrosis factor-alpha (TNF-α) and nerve growth factor (NGF). Furthermore, PCJNF down-

regulates the expression of transient receptor potential vanilloid 1 (TRPV1), phosphorylated TRPV1 (p-TRPV1), and protein …

In Vitro Metabolic Profiling Of Methylenedioxy-Substituted Synthetic Cathinones For Enhanced Detection In Urine Sample Analysis, Ya-Ling Yeh, Chin-Lin Hsieh, Yi-Jia Huang, Yu-Hsiang Chang, Sheng-Meng Wang

Journal of Food and Drug Analysis

Synthetic cathinones are a widely abused class of new psychoactive substances that pose significant challenges in forensic toxicology owing to their complex metabolic pathways and lack of verified reference standards. This study investigated the in vitro metabolism of nine methylenedioxy-substituted synthetic cathinones, including methylone and eight structural isomers, which were categorized into three groups: Group 1 (dimethylone, ethylone, and butylone), Group 2 (dibutylone, pentylone, and eutylone), and Group 3 (N-ethylpentylone and dipentylone). Pooled human liver microsomes, cytosol, and uridine diphosphate glucuronic acid were used to identify phase Ⅰ and Ⅱ metabolites by liquid chromatography–quadrupole time-of-flight mass spectrometry. Key pathways included …

Integrating Network Analysis And Experimental Validation To Reveal The Ferroptosis-Associated Mechanism Of Velvet Antler In The Treatment Of Chronic Atrophic Gastritis, Quan Liao, Zhenzhen Guo, Chenchun Ding, Renjie Zuo, Guoyan Liu

Journal of Food and Drug Analysis

Chronic atrophic gastritis (CAG) is precancerosis with limited treatment options. This study investigated the therapeutic effects of velvet antler (VA), a traditional natural medicine, on CAG, with a focus on ferroptosis. In vivo experiments demonstrated the efficacy of VA in alleviating CAG, and network pharmacology analysis revealed its involvement in related terms, including inflammation, oxidative stress, and cell proliferation. Analyses further confirmed the modulation of ferroptosis by VA, particularly via the Keap1-Nrf2/HO-1/GPX4 pathway. In vitro assays supported these findings, demonstrating the ability of VA to reduce methylnitronitrosoguanidine-induced inflammation, oxidative stress, and ferroptosis in GES-1. This study provides a basis for …

Jiao San Xian Granule Containing Prebiotic Alleviate Functional Dyspepsia By Regulating Intestinal Flora And The Secretion Of Inflammatory Response, Huimin Pei, Mengyuan Zhao, Hongyue Wang, Xindi Zhang, Caihong Shi, Xiangrong Zhang

Journal of Food and Drug Analysis

Jiao Sanxian (JSX) consists of three traditional Chinese medicine including charred hawthorn, malt and Liu Shen Qu, they are also from Chinese medicine homologous food. It is commonly used to relieve functional dyspepsia (FD). The present study aims to explore the mechanism of JSX (granule), with the addition of prebiotics for the treatment of FD using mice model. The network pharmacology and molecular docking were used to forecast therapeutic targets for JSX. Based on the protein-protein interaction (PPI) results, thirteen targets exhibited strong interactions with each other. The results of network pharmacology and molecular docking revealed therapeutic activity of JSX …

Regulatory Framework And Challenges For Live Biotherapeutic Products In Taiwan, Shirley Pan, Jia-Chuan Hsu, Kuo-Teng Hung, Ching-Jung Ho

Journal of Food and Drug Analysis

Products containing live microorganisms may be classified as food or drugs depending on their intended use; live biotherapeutic products (LBPs) with therapeutic claims are defined as medicinal products containing live bacteria or yeasts intended to prevent or treat disease. Based on their characteristics, LBPs are classified as biological drugs and must be registered as biological drugs before they can enter the Taiwanese market. As research into the microbiota and its role in health and disease continues to advance, LBPs are expected to play an increasingly important role in medicine and biotechnology. With the growing popularity of microbial applications in recent …

Aspergillosis: A Comprehensive Review Of Pathogenesis, Drug Resistance, And Emerging Therapeutics, Amanpreet Singh, Jeewanjot Singh, Sandeep Kumar

Journal of Food and Drug Analysis

Aspergillosis stands as a primary opportunistic fungal infection which mainly results from Aspergillus fumigatus events that have gained more importance because of its multiple infection patterns and developing antifungal resistance. Healthcare providers identify two main ends of the aspergillosis spectrum which include allergic responses and invasive systemic infections that affect mainly immunocompromised subjects. This review presents a detailed summary for understanding the epidemiology of aspergillosis along with its risk factors as well as pathogenesis and host immune response and diagnostic difficulties. The analysis puts significant weight on increasing azole and echinocandin resistance that has become worse because of agricultural and …

Targeting Detoxifying Enzymes In The Lymphatic Filariasis Vector: An In Silico Study On Curcumin, Camphor, And Menthol, Rizal Subahar, Rawina Winita, Surya Dwira, Gulshan Fahmi El Bayani

Indonesian Journal of Medical Chemistry and Bioinformatics

Vector control remains a critical component in the prevention of lymphatic filariasis, a disease transmitted by insect vectors. Natural compounds such as curcumin, camphor, and menthol are being explored for their bio-insecticidal properties due to their potential to inhibit key detoxification and neurological enzymes in insects, including acetylcholinesterase (AChE), glutathione S-transferase (GST), and cytochrome P450 oxidases (CYP450). A molecular docking study using SwissDock was conducted to evaluate the interaction of curcumin, camphor, and menthol with AChE, GST, and CYP450 enzymes. Binding affinity (ΔG), hydrogen bonding, and active site interactions were analyzed to assess the inhibitory potential of each compound. Curcumin …

Evaluating The Protective Role Of Epo-R76e In Oxidative Stress-Induced Cell Death In Retinal Pigment Epithelium, Jemima Alam

USF Tampa Graduate Theses and Dissertations

Age-Related Macular Degeneration (AMD) causes dysfunction and loss of Retinal pigment epithelium (RPE). The degeneration and death of RPE cells causes irreversible visual impairment. Oxidative stress is a widely accepted triggering factor for RPE dysfunction. A hormone called Erythropoietin (EPO) is responsible to facilitate the erythropoiesis process, prevents progenitor cells from apoptosis and protects photoreceptors downregulating retinal degeneration. In this study, we aim to elucidate the role of EPO in downregulating oxidative stress in RPE. It is hypothesized that EPO will have a positive impact on suppressing oxidative stress and ferroptosis-mediated RPE degeneration due to its vital role in apoptosis …

Dabigatran Reduced Acute Microgliosis In A Mouse Model With Tbi, Nicholas R. Eltman, Rashmeena Abbasi, Mary C. Kosciuk, Syed Ahmed, Jose L. Pascual, Randel L. Swanson, Nimish K. Acharya

Rowan-Virtua Research Day

Objective:

The study objective was to investigate the acute anti-inflammatory effects of dabigatran in a preclinical mouse controlled cortical impact (CCI) model of severe traumatic brain injury (TBI).

Design

Mice were separated into three groups: controlled cortical impact (CCI) with dabigatran (drug treatment, n=5), CCI with saline (positive control, n=5), and sham CCI without saline or dabigatran (negative control, n=3). Dabigatran (80mg/kg) or saline was administered orally at 2, 10, 18, 26, 34, and 42 hours following experimental CCI in the drug treatment or positive control groups, respectively. Animals in the negative control group received sham CCI only. 48h following …

Direct Synthesis Of Cerium Oxide Nanoparticles In Reducing Sugars: Enhanced Ce3+ Surface Density For Biological Application, Balaashwin Babu, Elayaraja Kolanthai, Craig J. Neal, Samarah V. Harb, Udit Kumar, Yifei Fu, Sudipta Seal

Rowan-Virtua Research Day

Cerium oxide nanoparticles (CNPs) are recognized for their ability to scavenge reactive oxygen species (ROS), making them promising candidates for mitigating oxidative damage in biomedical applications. However, many conventional synthesis methods limit the formation of Ce³⁺ states, which are critical for this antioxidant function. Building upon previous findings that glucose can promote Ce³⁺ formation, this study investigates the broader impact of both reducing (glucose, fructose, galactose) and non-reducing (dextran, sucrose, cyclodextrin) natural sugars on CNP synthesis. CNPs were synthesized in the presence of these sugars, and the surface densities of Ce³⁺ were measured. Results showed that reducing sugars significantly increased …

Assessing The Behavioral Impact Of Pyridostigmine Bromide In Rats, Noah A. Martin

Honors Theses

Pyridostigmine bromide (PB) is an organophosphate (OP) nerve agent prophylactic used to protect warfighters against chemical warfare agents. OPs inhibit the neural enzyme acetylcholinesterase (AChE) in the brain. This leads to the buildup of acetylcholine, causing respiratory failure, seizures, and death. PB functions by inhibiting ~30% of peripheral AChE temporarily, protecting the enzymes so that the body is able to restore sufficient cholinergic function post-exposure. PB does not cross the blood-brain barrier, though it may still indirectly affect toxicity in the brain due to repeated AChE inhibition throughout treatment, or by inhibition of non-target ChE’s in the blood. The aim …

Phytochemistry, Antioxidant And Cytotoxic Activities Of Hibiscus (Hibiscus Rosa-Sinensis) Extract On Mcf-7 Breast Cancer Cells, Ade Arsianti, Isma Zahira Suhaima, Steven Gill, Ajeng Megawati Fajrin, Lince Dameria Nadapdap, Norma Nur Azizah, Hiroki Tanimoto, Shun Hirota

Indonesian Journal of Medical Chemistry and Bioinformatics

Background: Breast cancer is the most common type of cancer in women with a very high mortality rate. This cancer is caused by uncontrolled growth of breast cells. Treatments for this malignancy are surgery, chemotherapy, and radiotherapy, however those methods can cause adverse effects and quite expensive. Complementary and alternative medicines (CAMs) are also used to support those main treatments, one of them is herbal medicine. Hibiscus rosa-sinensis is known to have various phytochemical components with antioxidant, antibacterial, anticancer, and analgesic activities. This study is aimed to determine the phytochemical composition, antioxidant activity and cytotoxicity of Hibiscus rosa-sinensis extract towards …

Investigation Of The Effects Of The Peptidylarginine Deiminase Inhibitor Cl-Amidine On Apoptosis And Gene Expression In Ovarian Cancer, Victoria Walden

Longwood Senior Thesis Proposal

Peptidylarginine deiminases (PADs) are a family of enzymatic proteins responsible for the conversion of arginine and methylarginine residues to citrulline. This conversion is important for several key cellular processes including transcriptional gene regulation. Recently, a link has been established between overexpression of a particular PAD, PAD4, and the accelerated progression of both autoimmune diseases and cancers. Ovarian cancer exhibits heightened levels of PAD4 in affected cells. High levels of PAD4 are associated with the formation of neutrophil extracellular traps (NETs) that promote cancer metastasis, and downregulation of the p53 apoptotic pathway. Thus, it is important to explore inhibitors of PAD4. …

Preparation And Evaluation Of Mesoporous Celecoxib For Improved Antiarthritic Activity In Rodents, Reena I. Fernandaes, Sayani Bhattacharyya

The Thai Journal of Pharmaceutical Sciences

Background: Celecoxib, a model anti-inflammatory drug, used in the management of arthritis exhibits limited oral bioavailability and slow onset of action due to its poor solubility. Objective: The present study explores a mesoporous drug delivery of celecoxib to investigate the efficacy of its antiarthritic activity in animal models, and develops a low-oral dose therapy. Materials and Methods: The solvent evaporation method was employed for the preparation of mesoporous delivery of celecoxib, using Syloid^®, and Neusilin^®, at a molar ratio of silica/ drug 1:2.5. The formulations were characterized for drug loading, in vitro drug release, and material …

Bacillus Coagulans 198 And L-Glutamine In Combination Attenuated Intestinal Mucositis In A 5-Fu-Induced Balb/C Mouse Model Via Modulation Of Gut Microbial Community Structure And Diversity, Wei-Jen Chen, Siou-Ru Shen, Wei-Hsuan Hsu, Bao-Hong Lee, Yu-Shan Wei, Hui-Fang Chu, Ming-Chung Tseng, Tang-Long Shen

Journal of Food and Drug Analysis

5-Fluorouracil (5-FU) disrupts intestinal cells and causes dysbiosis in the gut microbiota. This study explores the potential of Bacillus coagulans-198 (BC198) to mitigate gut microbiota imbalance and mucositis caused by 5-fluorouracil. L-glutamine is used to alleviate mucositis, and this study found that BC198 exhibits protective effects on the gut, including maintaining a healthy microbiota and reducing intestinal inflammation, regardless of whether L-glutamine is used in combination. Therefore, it can help reduce the deterioration of the gut environment caused by 5-fluorouracil. BC198 can be provided to cancer patients to prevent severe side effects, thereby improving their treatment outcomes and nutritional …

Protective Role Of Hsian-Tsao Ethanol Extract Against Body Fat, Serum Lipid Profiles, And Hepatic Lipid Profiles In High-Fat Diet-Fed Rats, Ching-Chang Cho, Gow-Chin Yen, Hsin-Yi Lee, Chun-Tse Tsai, Wei-Tang Chang, Chin-Lin Hsu

Journal of Food and Drug Analysis

This study investigated the preventive effects of a 40% ethanol extract of Hsian-tsao (40EEHT) on obesity in high-fat diet (HFD)-induced obese rats. Male Wistar rats were administered 0, 100, 200, or 500 mg/kg of 40EEHT, resulting in reduced body weight, total body fat, and hepatic tissue weight after 8 weeks. 40EEHT also decreased adipocyte size, improved lipid profiles, alleviated oxidative stress, and enhanced hepatic antioxidant enzyme activities. Additionally, it regulated fatty acid metabolism by reducing lipogenesis and increasing lipolysis and β-oxidation, suggesting its potential as an anti-obesity dietary supplement.

Xanthohumol As A Potential Therapeutic Strategy For Acute Myeloid Leukemia: Targeting The Flt3/Srpk1 Signaling Axis, Duan-Na Zhang, Wen-Ya Yang, Xiao-Xue Hu, Xiao-Min-Ting Song, Chuan-Jie Guo, Fu Peng, Yu-Zhi Li, Zhi-Xing Cao

Journal of Food and Drug Analysis

Xanthohumol (XN) is an isoprene chalcone found in hops (Humulus lupulus L.), a food ingredient with a wide range of pharmacological activities. The aim of this study was to reveal the therapeutic effect of XN on acute myeloid leukemia (AML) and the potential underlying molecular mechanism. Through network pharmacology analysis, molecular docking, and HTRF determination, XN was shown to inhibit the kinase activities of FLT3 and SRPK1 by targeting their ATP-binding domains, with IC₅₀ values of 1.51 ± 0.44 μM and 0.37 ± 0.15 μM, respectively. By inhibiting AML cell proliferation, promoting apoptosis, regulating autophagy, and inhibiting …

Within-Trial Cost-Effectiveness Of Novel Macrophage-Regulating Treatment On Wound Healing In Patients With Diabetic Foot Ulcers, Hsuan-Yu Su, Chen-Yi Yang, Yi-Hsin Chang, Shyi-Gen Chen, Jui-Ching Chen, Hui-Ju Ho, Huang-Tz Ou, Shihchen Kuo

Journal of Food and Drug Analysis

An M1/M2 macrophage-regulating treatment, ON101 cream, has shown its superior healing efficacy for diabetic foot ulcers (DFUs) versus standard absorbent dressing, according to a phase Ⅲ trial. Given its high cost, corroborating the economic value of ON101 treatment can facilitate clinical and policy decision-makings. This study sought to evaluate the cost-effectiveness of ON101 versus an absorbent dressing for patients with DFUs from Taiwan's healthcare sector perspective. This economic evaluation utilized effectiveness and cost data (in 2022 USD) from a randomized controlled trial of ON101, published literature, and Taiwan’s National Health Insurance program. Incremental cost-effectiveness ratio (ICER) against willingness-to-pay (WTP) threshold …

Method Development For The Determination Of Phosphine Residues In Foods, Shu-Wei Lin, Yu-Ting Liu, Ya-Chun Chou, Yu-Ching Hung, Shu-Han Chang, Ya-Min Kao, Su-Hsiang Tseng, Der-Yuan Wang

Journal of Food and Drug Analysis

Phosphine (PH₃) is a fumigant used for pest control of stored products and foods. In Taiwan, PH₃ has the maximum residue level (MRL) in 14 foods, including dried fruits, vegetables, spices, nuts, crops, roots, and tuber vegetables. In this study, gas chromatography/mass spectrometry coupled with a headspace sampler (HS-GC/MS) was used to determine the PH₃ content in foods. The stability of the PH₃ standard was evaluated either directly using the gas standard or indirectly using zinc phosphide (Zn₃P₂) with an acid. The optimal conditions for the headspace agitator were determined to …

A Deep Dive Into The Orchard Of Health: Exploring The Anti-Cancer And Anti-Aging Potential Of Apple Polyphenols, Li-Ching Chen, Han-Sheng Chang, Yuan-Soon Ho

Journal of Food and Drug Analysis

Apples, a ubiquitous and beloved fruit, harbor a treasure trove of bioactive compounds, with apple polyphenols (APs) taking center stage. This review delves into the latest scientific advancements illuminating the anti-cancer and anti-aging properties of APs. We dissect the intricate mechanisms by which APs combat cancer initiation, progression, and metastasis, highlighting their prowess in inducing apoptosis, inhibiting angiogenesis, and modulating cell signaling pathways. Furthermore, we explore the multifaceted ways APs combat aging, including their potent antioxidant and anti-inflammatory actions, DNA protective effects, and ability to modulate cellular processes like autophagy and metabolism. This comprehensive review underscores the therapeutic promise of …