Medicinal Chemistry and Pharmaceutics Commons^™

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), …

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 …

Determination And Evaluation Of Epa And Dha Ethyl Esters In Fish Oils Using The Tmah Transesterification Method, Pai-Wen Wu, Ching-Hsuan Tsai, Ching-Yu Hsu, Shu-Han Chang, Ya-Min Kao, Su-Hsiang Tseng, Der-Yuan Wang

Journal of Food and Drug Analysis

A simple and dependable technique, known as THAM method, has been developed to detect and measure ethyl eicosapentaenoate (EE-EPA) and ethyl docosahexaenoate (EE-DHA) in encapsulated fish oils. This technique involves using tetramethylammonium hydroxide (TMAH) as a catalyst, followed by analysis using gas chromatography equipped with a flame ionization detector. Recoveries of EE-EPA and EE-DHA spiked between 5 mg/g and 20 mg/g were found to be between 90.8% and 95.2%, with coefficients of variation ranging from 0.2% to 2.5%, demonstrating the accuracy and precision of the technique. Additionally, its limitation of quantitation of EE-EPA and EE-DHA in fish oil samples was …

Cannabis Sativa L.: A Comprehensive Review On Legislation, Decriminalization, Phytochemistry, Antimicrobial Activity, And Safety, Mohammed Dalli, Salah-Eddine Azizi, Ali Azghar, Abderrazak Saddari, Elmostapha Benaissa, Yassine Ben Lahlou, Mostafa Elouennass, Adil Maleb

Journal of Food and Drug Analysis

Throughout history, medicinal and aromatic plants have been used extensively to cure a variety of ailments. This article provides a comprehensive overview of Cannabis sativa, specifically focusing on its legislative status, decriminalization, phytochemistry, antimicrobial activity, and safety. The study begins by briefly outlining the plant's history, including its cultivation, harvesting, and storage methods. The review analyzes extensively the antimicrobial properties of Cannabis sativaand its derivatives, specifically examining their reported antiviral, antibacterial, antifungal, and antiparasitic capabilities, which have been documented in databases such as Scopus, ScienceDirect, PubMed, and Web of Science. The paper also discusses trends in studies about the …

How To Deal With Frenemy Nrf2: Targeting Nrf2 For Chemoprevention And Cancer Therapy, Ya-Chu Tang, Yung-Jen Chuang, Hsin-Huei Chang, Shin-Hun Juang, Gow-Chin Yen, Jang-Yang Chang, Ching-Chuan Kuo

Journal of Food and Drug Analysis

Induction of antioxidant proteins and phase 2 detoxifying enzymes that neutralize reactive electrophiles are important mechanisms for protection against carcinogenesis. Normal cells provide multifaceted pathways to tightly control NF-E2- related factor 2 (NRF2)-mediated gene expression in response to an assault by a range of endogenous and exogenous oncogenic molecules. Transient activation of NRF2 by its activators is able to induce ARE-mediated cytoprotective proteins which are essential for protection against various toxic and oxidative damages, and NRF2 activators thereby have efficacy in cancer chemoprevention. Because NRF2 has a cytoprotective function, it can protect normal cells from carcinogens like an angel, but …

Effects Of Green Tea–Derived Natural Products On Resistance Exercise Training In Sarcopenia: A Retrospective Narrative Mini-Review, Hung-Wen Liu, Sue-Joan Chang

Journal of Food and Drug Analysis

Skeletal muscle function deficits result in metabolic disease development and physical dysfunction in older adults. Sarcopenia is characterized by a decrease in muscle mass and strength with advancing age, and it increases the risks of mobility impairments, disease development, and mortality. Lifestyle interventions involving a combination of diet and exercise to prevent and attenuate sarcopenia warrant substantial research attention. Resistance exercise training under supervision is a safe and the most effective approach to reducing age-related muscle loss and improving multiple aspects of overall health in the older population. The beneficial effects of resistance exercise training on skeletal muscle mass may …

Modeling Biphasic, Non-Sigmoidal Dose-Response Relationships: Comparison Of Brain- Cousens And Cedergreen Models For A Biochemical Dataset, Venkat D. Abbaraju, Tamaraty L. Robinson, Brian P. Weiser

Rowan-Virtua School of Osteopathic Medicine Faculty Scholarship

Biphasic, non-sigmoidal dose-response relationships are frequently observed in biochemistry and pharmacology, but they are not always analyzed with appropriate statistical methods. Here, we examine curve fitting methods for “hormetic” dose-response relationships where low and high doses of an effector produce opposite responses. We provide the full dataset used for modeling, and we provide the code for analyzing the dataset in SAS using two established mathematical models of hormesis, the Brain-Cousens model and the Cedergreen model. We show how to obtain and interpret curve parameters such as the ED50 that arise from modeling, and we discuss how curve parameters might change …

Using Lanthanide Ions As Magnetic And Sensing Probes For The Detection Of Tetracycline From Complex Samples, Yan-Cen Zhan, Chin-Poa Chiu, Yu-Chie Chen

Journal of Food and Drug Analysis

Tetracycline (TC) is a broad-spectrum antibiotic and has been added to animal feeds to grow livestock under healthy conditions, making it important to have effective methods for rapidly detecting TC in complex samples. In this study, a novel method that uses lanthanide ions (i.e. Eu³⁺ and Gd³⁺) as magnetic and sensing probes for the detection of TC from aqueous samples is explored. When dissolving Gd³⁺ in tris(hydroxymethyl)aminomethane (Tris) buffer at pH 9, magnetic Gd³⁺-Tris conjugates can be readily generated. The magnetic Gd³⁺-Tris conjugates possess trapping capacity toward TC from sample solutions via …

Urolithin A Exhibits A Neuroprotective Effect Against Alzheimer’S Disease By Inhibiting Dyrk1a Activity, Huang-Ju Tu, Chih-Jou Su, Chao-Shiang Peng, Tony Eight Lin, Wei-Chun Huang Fu, Kai-Cheng Hsu, Tsong-Long Hwang, Shiow-Lin Pan

Journal of Food and Drug Analysis

Alzheimer’s disease (AD) is a devastating neurodegenerative disease with more than 50 million people suffer from it. Unfortunately, none of the currently available drugs is able to improve cognitive impairment in AD patients. Urolithin A (UA) is a metabolite obtained from ellagic acid and ellagitannin through the intestinal flora, and it has antioxidant and anti-inflammatory properties. Previous reports found that UA had neuroprotective effects in an AD animal model, but the detailed mechanism still needs to be elucidated. In this study, we performed kinase-profiling to show that dual-specific tyrosine phosphorylation-regulated kinase 1A (DYRK1A) is the main target of UA. Studies …

Chemometrics-Assisted Spectroscopic Methods For Rapid Analysis Of Combined Anti-Malarial Tablets, Panawan Pruksapha, Putthiporn Khongkaew, Chaweewan Suwanvecho, Nantana Nuchtavorn, Chutima Phechkrajang, Leena Suntornsuk

Journal of Food and Drug Analysis

Combination of piperaquine (PQ) (320 mg) and dihydroartemisinin (DHA) (40 mg) is an anti-malarial formulation, which is recommended by World Health Organization (WHO). Simultaneous analysis of PQ and DHA can be problematic due to the lack of chromophores or fluorophores in DHA molecule. Whereas PQ possesses strong UV absorption and it presents in 8 times of DHA contents in the formulation. In this study, two spectroscopic methods, Fourier transform infrared (FTIR) and Raman spectroscopy, were developed for the determination of both drugs in combined tablets. The FTIR and Raman spectra were recorded in the attenuate total reflectance (ATR) and scattering …

Three-Dimensional Strategies In The Quantitative Resolution Of Kinetic Uv Absorbance Measurements For Monitoring The Oxidation Of Quercetin By Oxidant Agents And Analyzing Dietary Supplement Product, Erdal Di̇nç, Asiye Üçer, Nazangül Ünal

Journal of Food and Drug Analysis

Three-dimensional strategies involving the application of parallel factor analysis (PARAFAC) to the kinetic UV absorbance measurements were elaborated to monitor the oxidation of quercetin with oxidant agents (K₂Cr₂O₇ and KIO₃) and to quantify analyte in a dietary supplement product. Loadings (spectral, kinetic and concentration profiles) were obtained by the PARAFAC deconvolution. Spectral identification, kinetics and quantification of the relevant analyte in the presence of interferent(s) were performed. The elaborated chemometric strategies were carefully validated to demonstrate the capability of the method. Assay results of the PARAFAC strategies were statistically compared to that of …

Resveratrol Stimulates Star Expression And Progesterone Production By Gper-Mediated Downregulation Of Snail Expression In Human Granulosa Cells, Tinglin Song, Jiaye Chen, Sizhu Yang, Boqun Liu, Lingling Zhang, Qian Zhang, Jung-Chien Cheng, Lanlan Fang

Journal of Food and Drug Analysis

Steroidogenic acute regulatory protein (StAR) plays a critical role in the regulation of progesterone (P4) production. Resveratrol (RSV), a natural polyphenol, has beneficial effects on reproductive function. However, its effects on StAR expression and P4 production in human granulosa cells remain undetermined. In this study, we showed the treatment of RSV upregulated StAR expression in human granulosa cells. G protein-coupled estrogen receptor (GPER) and ERK1/2 signaling were involved in RSV-stimulated StAR expression and P4 production. In addition, the expression of a transcriptional repressor, Snail, was downregulated by RSV, which contributed to the RSV-induced induction of StAR expression and P4 production.

Selective Detection Of Tricyclazole By Optical Technique Using Thiomalic Acid–Modified Au And Ag Nanoparticle Mixtures, Yu-Shu Pan, Tsunghsueh Wu, Cho-Chun Hu, Tai-Chia Chiu, Chen-Hao Yeh, Yang-Wei Lin

Journal of Food and Drug Analysis

This study proposes the use of thiomalic acid–modified Au and Ag nanoparticle mixtures (TMA-Au/AgNP mixes) for the selective detection of tricyclazole. Upon the addition of tricyclazole, the color of TMA-Au/AgNP mixes solution changes from orange-red to lavender (red-shift). According to the density-functional theory calculations, tricyclazole-induced aggregation of TMA-Au/AgNP mixes through electron donor–acceptor interactions was proved. The sensitivity and selectivity of the proposed method are affected by the amount of TMA, volume ratio of TMA-AuNPs to TMA-AgNPs, pH value, and buffer concentration. The ratio of absorbance (A₆₅₄/A₅₂₀) of TMA-Au/AgNP mixes solution is proportional to the concentration of …