Medicinal Chemistry and Pharmaceutics Commons^™

Analysis And Identification Of Phenolic Compounds With Antiproliferative Activity From Chinese Olive (Canarium Album L.) Fruit Extract By Hplc-Dad-Spe-Tt-Nmr, Yu-Te Yeh, Chien-Kuang Chen, Yi-Chun Liao, Shoei-Sheng Lee, Shu-Chen Hsieh

Journal of Food and Drug Analysis

Chinese olives (Canarium album L.) are rich in phenolic compounds, exhibiting a broad spectrum of potential clinical applications. This study is the first report on the isolation and elucidation of bioactive compounds with high antiproliferative activity from the ethyl acetate fraction of a Chinese olive fruit methanolic extract (CO-EtOAc). We used the WST-1 assay to determine which subfractions of CO-EtOAc had significant antiproliferative activity using the murine colon cancer cell line CT26. Subsequently, the functional compounds were characterized by the hyphenated technique and high-performance liquid chromatography-diode array detector-solid phase extraction-transfer tube-nuclear magnetic resonance (HPLC-DAD-SPE-TT-NMR). Thirteen phenolic constituents were identified …

Glycine-Rich Peptides From Fermented Chenopodium Formosanum Sprout As An Antioxidant To Modulate The Oxidative Stress, Chen-Che Hsieh, Shu-Han Yu, Hsing-Chun Kuo, Darin Khumsupan, Hsiao-Chu Huang, Yu-Wei Liou, Chen-Yu Kao, Szu-Chuan Shen, Kuan-Chen Cheng

Journal of Food and Drug Analysis

Rhizopus oligosporus was utilized in the solid-state fermentation of Chenopodium formosanum sprouts (FCS) in a bioreactor. Subsequently, the antioxidant activity of food proteins derived from FCS was investigated. Results showed that glycine-rich peptide (GGGGGKP, G-rich peptide), identified from the < 2 kDa FCS proteins, had antioxidant values. According to SwissADME, AllerTOP, ToxinPred, and BIOPEP-UWM analyses, G-rich peptide was identified as safe, non-toxic, and non-allergenic. Afterward, the peptide was examined using in silico and in vitro studies to evaluate its potential alleviating oxidative stress caused by particulate matter. This study proposed plausible mechanisms that involve the binding of G-rich peptide which inhibited phosphorylation of the v-rel avian reticuloendotheliosis viral oncogene homolog A (RELA) subunit on NF-κB pathway. The inhibition then resulted in down regulation of NF-κB transcription and genetic expression of inflammatory …

Investigation Of Microwave Extraction Of Red Cabbage And Its Neurotherapeutic Potential, Halil Koyu, Serdar Demir, Mehmet Zeki Haznedaroglu

Journal of Food and Drug Analysis

In the pursuit of bioactive compounds with health benefits from food and medicinal plants, optimization of process to reduce solvent, raw material, energy and time consumption has been a valuable research objective. Sustainable management and efficient use of natural resources are of critical importance for sustainability goals. In this manner, microwave extraction of red cabbage which has been a mass cultivated plant for food purposes, was optimized for maximizing acetylcholinesterase, butyrylcholinesterase, tyrosinase inhibitory activity and bioactive content. Quantitative analysis of total phenol, flavonoid and anthocyanin content were performed using spectrophotometry and UPLC-DAD-ESI-MS/MS. Optimum conditions were determined as 600 W, 100% …

Abundance Of Prevotella Copri In Gut Microbiota Is Inversely Related To A Healthy Diet In Patients With Type 2 Diabetes, Chih-Yiu Tsai, Po-Yu Liu, Meng-Chuan Huang, Chiao-I Chang, Hsin-Yun Chen, Yu-Hsien Chou, Chi-Neu Tsai, Chia-Hung Lin

Journal of Food and Drug Analysis

While the gut microbiota is known to be influenced by habitual food intake, this relationship is seldom explored in type 2 diabetes patients. This study aims to investigate the relationship between dietary patterns and gut microbial species abundance in 113 type 2 diabetes patients (mean age, 58 years; body mass index, 29.1; glycohemoglobin [HbA1c], 8.1%). We analyzed the gut microbiota using 16S amplicon sequencing, and all patients were catogorized into either the Bacteroides enterotype (57.5%, n = 65) or the Prevotella enterotype (42.5%, n = 48) using the partitioning around medoids clustering algorithm, based on the most representative genera. Patients …

Therapeutic Effects Of Orally Administration Of Viable And Inactivated Probiotic Strains Against Murine Urinary Tract Infection, Vo Thi Hong Van, Zhen-Shu Liu, Yueh Jen Hsieh, Wei-Chen Shiu, Bo-Yuan Chen, Yu-We Ku, Po-Wen Chen

Journal of Food and Drug Analysis

Urinary tract infections (UTIs) are highly prevalent bacterial infections that pose significant health risks. Specific probiotic strains have been recommended for UTI control and management of antibiotic resistance. Otherwise, paraprobiotics, defined as inactivated probiotic cells, offer potential advantages by minimizing risks associated with live microorganisms. However, the effectiveness of heat-killed probiotic strains against UTIs remains uncertain. Additionally, lactoferrin (LF), an iron-binding glycoprotein, exhibits immunomodulatory, antimicrobial, and anti-inflammatory properties. Recently, we had developed recombinant LF-expression probiotics, which can display considerate antibacterial activities against select food-borne pathogens in vitro. Thus, the present study aimed to evaluate the antibacterial activities of heat-killed natural …

Recent Advances In Combined Avant-Garde Technologies (Thermal-Thermal, Non-Thermal-Non-Thermal, And Thermal-Non-Thermal Matrix) To Extract Polyphenols From Agro Byproducts, Isaac Duah Boateng

Journal of Food and Drug Analysis

Because food byproducts (waste) are rich in phytoconstituents, valorizing them is crucial for global food security. However, conventional extraction (CE), including decoction, maceration, Soxhlet, etc., for agro byproducts’ polyphenol extraction are time-consuming and rely significantly on vast volumes of potentially aggressive solvents. Hence, Avant-garde extraction technologies, including non-thermal (high hydrostatic pressure (HHPE), pulsed-electric field (PEF), high voltage electrical discharges (HVED), etc.) and thermal extraction (supercritical fluid (SCF), subcritical water extraction (SWE), microwave-assisted extraction (MAE), etc.), as well as their thermal combinations (SCF-PLE, SCCO2-SWE, SCCO2-MAE, etc.), non-thermal combinations (HHPE+UAE, PEF+UAE, HVED+UAE, etc.) and combined thermal-non-thermal (MAE-UAE, etc.) are increasingly replacing CE. …

Delta-9-Tetrahydrocannabinol And Cannabidiol Effect On Dopamine Transporter Expression And Function, Delia M. Guzman

Student Theses

Drug addiction is a major endemic crisis in the United States with a higher prevalence than any other country. Marijuana and hallucinogens make up a great percentage of the drugs of abuse in Americans ranging from 15 to 64 years old. Marijuana contains over 500 active compounds that contribute to its effects, the major components being delta-9-tetrahydrocannabinol (Δ-9-THC) and cannabidiol (CBD). Understanding the pharmacological mechanism as well as the effects that they elicit through the dopaminergic reward system is a key factor in being able to understand why addiction is so prevalent in our society. This research was aimed to …

Elucidation Of Molecular Mechanisms Underlying Novel Multi-Targeted Therapy Strategies For, Qianqian Hu

USF Tampa Graduate Theses and Dissertations

EML4-ALK fusion non-small cell lung cancer (NSCLC) represents a distinct subset of lung cancers that possesses unique molecular and clinical features, paving the way for targeted therapeutic interventions. Despite the promise of ALK-directed therapies, challenges such as metastasis at the time of diagnosis and treatment resistance persist, necessitating deeper research into the underlying mechanisms and potential solutions. In the context of these challenges, our study embarked on two specific objectives. The first goal, elucidated in Chapter 2, revolved around brain metastasis, an event critically facilitated by cell migration. Here, we assessed the anti-migratory activities of several clinical ALK inhibitors in …

An Insight Into The Physicochemical, Drug-Likeness, Pharmacokinetics And Toxicity Profile Of Kigelia Africana (Lam) Bioactive Compounds, Sulyman Olalekan Ibrahim, Halimat Yusuf Lukman, Marili Funmilayo Zubair, Oluwagbemiga Tayo Amusan, Fatimah Ronke Abdulkadri, Bashir Lawal, Lateefat Bello Abdulfatah, Olubunmi Atolani

Al-Bahir

Kigelia africana plant is multipurpose plant whose therapeutic potential has been thoroughly investigated. The physicochemical, solubilities, ADMET, pharmacological, and drug-like properties of this plant have not been reported in details. This study makes use of the information that is currently known on the chemical make-up of the plant to forecast its overall toxicity as well as the potential for the phytochemicals it contains to be employed in medication discovery. The study also employed free web servers for the lipophilicity, water solubility, drug-likness, bioavailability score, medicinal chemistry and toxicological profiling of the compounds of K. africana. Artemether, a known antimalaria …

Developing A Point-Of-Care Detection Kit For Parkinson’S Disease Using Gold Nanoparticle-Based Lateral Flow Assay, Ali Aljassabi

USF Tampa Graduate Theses and Dissertations

Parkinson’s disease (PD) is the second most common neurodegenerative disease after Alzheimer’s disease and the fastest-growing neurodegenerative disorder in the world. The major issue with PD is that it takes several years of biological changes until the patient starts to experience physiological symptoms that could affect their daily lives. The major hallmark of PD is the appearance of Lewy body inclusions in the neuron’s cytoplasm, which is rich in a protein called α-Synuclein (α-Syn). Several studies have shown that the levels of α-Syn in blood increase because the excess α-Syn is released from neurons into the bloodstream through extracellular vesicles. …

Piperine Encourages Apoptosis In Human Cervical Adenocarcinoma Cells Through Ros Generation, Dna Fragmentation, Caspase-3 Activation And Cell Cycle Arrest, Asif Jafri, Juhi Rais, Sudhir Kumar, Md Arshad

Research Symposium

Background: Cancer is one of the most common destructive diseases and the second leading cause of death in humans. Among cancer, cervical cancer is the second most common malignancy among women globally. Thus, there is a continuous need to search for chemotherapeutic chemicals or naturally occurring drugs to resolve this global health problem. Piperine (1-piperoylpeperdine) is present in the fruits of black pepper (Piper nigrum Linn.) and long pepper (Piper longum Linn.). It possesses several pharmacological properties and in the present study we have evaluated its anti-cancer potential on human cervical adenocarcinoma (HeLa) cells.

Methods: The anti-proliferative effect …

Cell-Based Experimental Evidence To The Anti-Covid-19 Potential Of Ashwagandha And Honeybee Propolis Ingredients, Renu Wadhwa, Durai Sundar, Yoshiyuki Ishida, Keiji Terao, Sunil C. Kaul

Research Symposium

Background: The COVID-19 pandemic emerged in December 2019 by a novel strain of SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2) has led to new endeavours in repurposing of existing drugs, anti-COVID-19 vaccine and drug development. Natural products, due to their general safety and wider availability, have attracted research and public attention. In this study, we report anti-COVID potential of compounds from honeybee propolis and Ayurvedic herb, Ashwagandha. Effect of active ingredients was studied on human cell surface receptors (ACE-2:Angiotensin Converting Enzyme-2/Spike protein and TMPRSS2:Transmembrane Protease Serine 2), critical for virus infection and virus main protease (Mpro, essential for virus replication), …

Adipocyte-Derived Pxr Signaling Is Dispensable For Diet-Induced Obesity And Metabolic Disorders In Mices, Fang Wang, Jinwei Liu, Rebecca Hernandez, Se-Hyung Park, Ying-Jing Lai, Shuxia Wang, Bruce Blumberg, Changcheng Zhou

UK CARES Faculty Publications

Pregnane X receptor (PXR) is a xenobiotic receptor that can be activated by numerous chemicals including endogenous hormones, dietary steroids, pharmaceutical agents, and environmental chemicals. PXR has been established to function as a xenobiotic sensor to coordinately regulate xenobiotic metabolism by regulating the expression of many enzymes and transporters required for xenobiotic metabolism. Recent studies have implicated a potentially important role for PXR in obesity and metabolic disease beyond xenobiotic metabolism, but how PXR action in different tissues or cell types contributes to obesity and metabolic disorders remains elusive. To investigate the role of adipocyte PXR in obesity, we generated …

Jinhua Qinggan Granule Uhplc-Q-Extractive-Orbitrap-Ms Assay: Putative Identification Of 45 Potential Anti-Covid-19 Constituents, Confidential Addition, And Pharmacopoeia Quality-Markers Recommendation, Jingyuan Zeng, Xican Li, Rongxin Cai, Chunhou Li, Shaoman Chen

Journal of Food and Drug Analysis

The study combined UHPLC-Q-Orbitrap-MS analysis with authentic standards, to create a novel strategy for isomers recognition and putative identification. Through the strategy, anti-Covid-19 Jinhua Qinggan Granule was found to comprise 28 isomers and 45 potential anti-Covid-19 constituents. The detection of three constituents (Danshensu, cryptotanshin, and tanshinone IIA) suggests Danshen as confidential additive. Based on this, 6 constituents are recommended as quality-marker candidates, including chlorogenic acid, acteoside, peimisine, baicalein, licoricesaponin H2, and tanshinone IIA. Obviously, the study can not only help the public to really understand the Granule's formula and chemistry, but also facilitate its Pharmacopoeia collection in future.

Autophagy-Urea Cycle Pathway Is Essential For The Statin-Mediated Nitric Oxide Bioavailability In Endothelial Cells, Wen-Hua Chen, Bei-Chia Guo, Chia-Hui Chen, Man-Chen Hsu, Chih-Hsien Wang, Tzong-Shyuan Lee

Journal of Food and Drug Analysis

Statins induce nitric oxide (NO) bioavailability by activating endothelial nitric oxide synthase via kinase- and calciumdependent pathways in endothelial cells (ECs). However, their effect on the metabolism of L-arginine, the precursor for NO biosynthesis, and regulatory mechanism have not yet been investigated. In this study, we investigated the role of the autophagy–urea cycle-L-arginine pathway in simvastatin-mediated NO bioavailability in ECs. Griess's assay was used to determine the NO bioavailability. Protein expression was assessed using Western blot analysis. Further, immunocytochemistry was performed to observe autophagosome formation, while conventional assay kits were used to quantify the levels of different intermediate substrates of …

Identification For Metabolism Profiles And Pharmacokinetic Studies Of Tradition Chinese Prescription Ji-Ming-San And Its Major Metabolites In Rats By Uhplc-Q-Tof-Ms/Ms And Uhplc-Ms/Ms, Cheng-Yang Hsieh, Ching-Chiung Wang, Lemmuel L. Tayo, Po-Wei Tsai, Chia-Jung Lee

Journal of Food and Drug Analysis

Ji-Ming-Shan (JMS) is a traditional prescription use for patients with rheumatism, tendons swelling, athlete's foot, diuresis and even gout. This study developed a rapid and sensitive method for the analysis of JMS chemical components in the Traditional Chinese medicine (TCM) prescription and in the serum samples of rats which were administered with the herbal extract. Two mass spectrometric approaches were used namely Ultra-performance liquid chromatographyquadrupole time-of-flight-mass spectrometry (UPLC-Q-TOF-MS) method for the major metabolites of the JMS extract while Ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) was employed for the detection of the JMS metabolites in the sera of rats. It was …

Cordycepin Inhibits Erk Pathway To Suppress Fgf9-Induced Tumorigenesis With Ma-10 Mouse Leydig Tumor Cells, Li-Ching Chen, Chin-Ying Chen, Yi-Ping Lee, Bu-Miin Huang

Journal of Food and Drug Analysis

Fibroblast growth factor 9 (FGF9) is a member of FGF family, and abnormal expression of FGF9 can promote tumorigenesis. Cordycepin, a major bioactive component in fungus Cordyceps sinensis, could suppress various tumors. We have shown that cordycepin could inhibit FGF9-induced testicular tumor growth in vitro and in vivo with MA-10 mouse Leydig tumor cells. In the present study, the mechanisms related to apoptosis and autophagy were determined. Results show that cordycepin significantly suppressed cell viability and colony formation with correlatedly morphological change related to cell death in FGF9-treated MA-10 cells. Flow cytometry and western blotting results further demonstrate that …

An Integrative Approach For Compressive Quality Control Of Respireaidtm, A Traditional Chinese Medicine Formula Against Sars-Cov-2, Kun-Teng Wang, Chia-Jung Lee, Ming-Chung Lee, Chao-Yu Chen, Yun-Chen Tsai, Wu-Chang Chuang

Journal of Food and Drug Analysis

RespireAid™ (NRICM101) is an effective anti-SARS-CoV-2 traditional Chinese medicine formula and has been licensed as a drug or dietary supplement in Taiwan, Luxembourg, Australia, Singapore, Cambodia, Philippines, and Canada. In this study, we provided integrated quality control strategy to analyze the ingredient of RespireAid™. In addition, the lot-to-lot efficacy stabilities were also evaluated. We found that RespireAid™ comprised of monosaccharides and disaccharides (34.0%), maltodextrin (23.5%), inorganic elements and ash (12.2%), oligosaccharides and polysaccharides (11.4%), principal components (4.4%), moisture (4.0%), amino acids (3.5%), b-Cyclodextrin (0.25%), menthol (0.25%), and nucleotides (0.14%), while the remainder was unidentified (6.36%). This is the first time …

Attenuation Of Diabetes-Mediated Muscle Atrophy In Rats By Fish Oil Enriched Omega-3 Polyunsaturated Fatty Acids Supplementation, Shing-Hwa Liu, Wei-Hsuan Lin, Huei-Ping Tzeng, Meng-Tsan Chiang

Journal of Food and Drug Analysis

Diabetes is associated with an increased risk of muscle wasting/atrophy, which adversely affects quality of life. We hypothesized that long term supplementation of fish oil may have protective effects against sarcopenia or muscle atrophy in streptozotocin (STZ) and high-fat (HF) diet-induced diabetic rat model. Wistar rats at age of 7 weeks were injected with saline or STZ to induce hyperglycemia. After one week, they were fed on a normal control diet or HF diet with/without supplementation of fish oil for 18 weeks. Feeding diabetic rats with a fish oil-enriched diet alleviated body weight loss and the impaired glucose tolerance using …

Ssr-Based Molecular Diagnosis For Taiwan Tea Cultivars And Its Application In Identifying Cultivar Composition Of The Processed Tea, Chih-Yi Hu, Hsien-Tung Tsai, Chui-Feng Chiu, Tsung-Chen Su, Nguyen Hoang Khoi Le, Shu-Dan Yeh

Journal of Food and Drug Analysis

Taiwan specialty teas are produced with distinct manufacturing processes from specific cultivars of tea plants in Camellia. Due to the widespread transplantation of Taiwan tea cultivars and active international trading of tea materials, an accurate and reliable method to identify tea cultivars at the border is vital to protect the image of premium Taiwan specialty teas. In this study, we introduced the Taiwan Tea Variety Identification (TTVID) kit, a capillary electrophoresis-based multiplex PCR assay consisting of 12 simple sequence repeat (SSR) markers. A database composing these 12 SSR loci genotypes in 144 cultivars was established for marker assessment and …