Medicinal Chemistry and Pharmaceutics Commons^™

Preface, Chih-Ching Huang, Yang-Wei Lin, Amit Nain

Journal of Food and Drug Analysis

No abstract provided.

Perilous Consequences Of Chemotherapy Induced Alopecia In Afflicted Cancer Survivors: A Comprehensive State Of The Art Review, Salma A. Fereig, Mona Gamal Arafa, Ghada Mamdouh Elzaafarany, Mona Mohamed Ahmed Abdelmottaleb, John Youshia

Pharmacy

Due to researchers’ great efforts during previous and current centuries to cure cancer, a remarkable increase in the number of cancer survivors has been observed. However, side effects of chemotherapeutic agents greatly affect the quality of life of cancer cases, usually referred to as cancer stigma, the most psychologically traumatizing of which is chemotherapy-induced alopecia (anagen effluvium). Unfortunately, there is no preventive protocol for chemotherapy-induced alopecia to date. The only suggested technique is vasoconstriction by scalp cooling during and after chemotherapy sessions to minimize the absorption of cytotoxic agents within the hair follicle area; a technique that is not very …

Incorporating Solvation Thermodynamic Mapping In Computer-Aided Drug Design, Yeonji Ji

Dissertations, Theses, and Capstone Projects

Advancements in computational techniques have revolutionized structure-based drug design, substantially improving the efficiency and effectiveness of the drug discovery process by reducing time, costs, and labor requirements. These advancements include various methods, such as investigating small molecule ligands binding to proteins, exploring alternative protein conformations, and solvation mapping on the protein surfaces. Among these methods, understanding the correlation between protein-ligand binding and the role of solvation is important.

A fundamental concept in protein-ligand binding is shape and electrostatic complementarity, which is complicated by the inherent flexibility of proteins. In the absence of small molecule ligands, proteins are complementary to surface …

Fluorescent Carbon Nanodot-Based Rapid Cell Nucleus Staining And Application For Diagnosis, Daiming Zhong, Huamin Yuan, Qiuyan Tian, Gongping Deng, Yanhong Ouyang, Yi Chen, Yang Wang, Zhiqin Yuan

Journal of Food and Drug Analysis

Cell nucleus status decides the activities of corresponding cells, making its rapid and effective staining important for revealing the actual condition of biological environment in life science and related fields. In this study, fast staining of cell nucleus is realized by fluorescent carbon nanodots (CDs). The staining mechanism is due to the positively charged CD surface-induced cell membrane penetration, which facilitates the CD-nucleus binding via electrostatic attraction. The size of cell nucleus is easily measured with fluorescence imaging technique. In addition, the CD-based cell nucleus stain is applied for discriminating the normal and cancer cells by determining the cell-to-nucleus ratio …

Effects Of Ibuprofen In The Zdf Rat Model Of Type 2 Diabetes, Alexander Gosslau, Unsal Ozdogru, Emmanuel Zachariah, Shiming Li, Chi-Tang Ho

Journal of Food and Drug Analysis

We aimed to investigate the therapeutic potential of ibuprofen against type 2 diabetes (T2D) using obese Zucker diabetic fatty (ZDF) rats as type 2 diabetes model. ZDF rats were hyperglycemic, dyslipidemic and expressed pro-inflammatory markers in contrast to lean controls, thus reflecting the relationship between obesity and chronic inflammation promoting T2D. Chronic treatment with ibuprofen (2-(4-Isobutylphenyl)propanoic acid) was used to study the impact on pathological T2D conditions as compared to metformin (1,1-dimethylbiguanide) treated ZDF as well as lean controls. Ibuprofen decreased A1c but induced a high insulin release with improved glucose tolerance only after early time points (i.g., 15 and …

Citrus Depressa Peel Extract Act As A Prebiotic To Reduce Lipid Accumulation And Modulate Gut Microbiota In Obese Mice, Zheng-Yuan Su, Jie-An Liao, Ching-Ting Lin, Guor-Jien Wei, Yen-Chen Tung

Journal of Food and Drug Analysis

Citrus peels contain abundant polyphenols, particularly flavonoids, and have been shown to exert lipid accumulation decreasing ability. In this study, Citrus depressa peel applied to oven drying and extracted with ethanol extract as CDEE to analyze its flavonoids compositions and investigated its effects on a high-fat diet (HFD)-induced obese mice model. CDEE contained several flavonoids such as hesperidin, sinesentin, nobiletin, tangeretin, 5-demethylnobiletin, and 5-demethyltangeretin. The mice fed an HFD, and administration of 2% CDEE to could decrease weight gain, abdominal fat weight, inguinal fat weight, and the adipocyte size, and CDEE also reduced serum total cholesterol (TCHO), triacylglycerol (TG) compared …

Antityrosinase Activity And Lc-Ms/Ms Analysis Of Optimized Ultrasound-Assisted Condition Extracts And Fractions From Strawberry Tree (Arbutus Unedo L.), Serdar Demir, Halil Koyu, Mustafa Abdullah Yilmaz, Abbas Tarhan, Sura Baykan Ozturk

Journal of Food and Drug Analysis

Investigation of utilization possibilities of natural sources has been an important area for research. Tyrosinase inhibitory activity plays a key role in food and medicine industry. Strawberry tree (Arbutus unedo), a widely distributed plant among Mediterranean countries, possess fruits and leaves with rich bioactive phytochemicals, especially polyphenolic compounds. In this study, we aimed to investigate the antityrosinase activity of the fruit and leaf extracts of the plant, and to determine the phenolic compounds that contribute to the antityrosinase activity. In this regard, we evaluated the effect of solvent composition on the extraction of phenolic compounds from A. unedo …

Detection Of Aflatoxin B1 In Chili Powder Using Attenuated Total Reflectance–Fourier Transform Infrared Spectroscopy, Thin Thin Sein, Urairat Mongmonsin, Patutong Chatchawal, Molin Wongwattanakul, Oranee Srichaiyapol, Rungrueang Pattanakul, Patcharaporn Tippayawat

Journal of Food and Drug Analysis

Aflatoxin B₁, a major global food safety concern, is produced by toxigenic fungi during crop growing, drying, and storage, and shows increasing annual prevalence. This study aimed to detect aflatoxin B₁ in chili samples using ATR–FTIR coupled with machine learning algorithms. We found that 83.6% of the chili powder samples were contaminated with Aspergillus and Penicillium species, with aflatoxin B₁ levels ranging from 7.63 to 44.32 µg/kg. ATR–FTIR spectroscopy in the fingerprint region (1800−400 cm^-1) showed peak intensity variation in the bands at 1587, 1393, and 1038 cm^-1, which are mostly related …

Comparative Bioactivity Assessment Of Bixin Pigment And Associated Phytochemicals Extracted From Annatto Seeds Using Conventional And Green Solvents, Sonakshi Puri, Sumit Kumar Mandal, Harshit Jain, Pankaj Kumar Sharma, Perinkulam Ravi Deepa

Journal of Food and Drug Analysis

Nutraceuticals, that include food ingredients and bioactives from natural products, confer physiological health benefits and protection against chronic diseases. Annatto is a tropical shrub grown in Central and South America and parts of India. Its seeds are rich in the edible carotenoid-derived apocarotenoid pigment, bixin, which is used as a natural colorant in food, textiles, and cosmetics, and is now gaining attention for its potential health-promoting attributes. Here, we compared a green solvent (ethyl lactate) based extraction of bixin and associated metabolites in annatto seeds (crushed and seed coat) with two other conventional solvents (acetone and acid-base). Bixin was characterized …

Chemical Constituents From A Marine Medicinal Brown Alga-Derived Xylaria Acuta Sc1019, Hsiao-Yang Hsi, Shih-Wei Wang, George Hsiao, Li-Kwan Chang, Yuan-Chung Cheng, Shu-Jung Huang, Yi-Shan Lu, Tzong-Huei Lee

Journal of Food and Drug Analysis

In this study, a marine medicinal brown alga Sargassum cristaefolium-derived fungal strain Xylaria acuta SC1019 was isolated and identified. Column chromatography of the extracts from liquid- and solid-fermented products of the fungal strain was carried out, and led to the isolation of twenty-one compounds. Their structures were characterized by spectroscopic analysis, and the absolute configurations were further established by single X-ray diffraction analysis or modified Mosher’s method as nine previously undescribed compounds, namely xylarilactones A–C (1–3), ent-gedebic acid 8-O-α-D-glucopyranoside (4), 5R-hydroxylmethylmellein 11-O-α-D-glucopyranoside (5), ent …

The Role And Mechanism Of Cinnamaldehyde In Cancer, Jiahua Peng, Xin Song, Wenbin Yu, Yuhan Pan, Yufei Zhang, Hui Jian, Bin He

Journal of Food and Drug Analysis

As cancer continues to rise globally, there is growing interest in discovering novel methods for prevention and treatment. Due to the limitations of traditional cancer therapies, there has been a growing emphasis on investigating herbal remedies and exploring their potential synergistic effects when combined with chemotherapy drugs. Cinnamaldehyde, derived from cinnamon, has gained significant attention for its potential role in cancer prevention and treatment. Extensive research has demonstrated that cinnamaldehyde exhibits promising anticancer properties by modulating various cellular processes involved in tumor growth and progression. However, challenges and unanswered questions remain regarding the precise mechanisms for its effective use as …

Trends And Current Food Safety Regulations And Policies For Functional Foods And Beverages Containing Botanicals, Jarunee Intrasook, Takuji W. Tsusaka, Anil Kumar Anal

Journal of Food and Drug Analysis

Globally, the demand for functional foods and beverages has significantly increased due to socioeconomic changes, particularly in health consciousness to enhance their functionality. Functional ingredients derived from botanicals are widely used because of their phytochemical properties with health benefits. This study aims to (1) review the capabilities and challenges of botanical addition in functional foods, (2) review current policies and regulations for functional foods containing botanicals in the European Union (EU), Canada, Japan, the Republic of Korea, and Thailand, and (3) provide recommendations on effective food safety control measures for better consumer trust and trade facilitation. This critical review was …

A Randomized Double Blind Placebo Controlled Trial To Assess The Safety And Efficacy Of A Patented Fenugreek (Trigonella Foenum-Graecum) Seed Extract In Type 2 Diabetics, Rajinder Singh Gupta, Amarjit Singh Grover, Pawan Kumar, Apurva Goel, Samudra P. Banik, Sanjoy Chakraborty, Mehul Rungta, Manashi Bagchi, Partha Pal, Debasis Bagchi

Publications and Research

Background: Fenugreek plant (Trigonella foenum-graecum) constitutes a traditionally acclaimed herbal remedy for many human ailments including diabetes, obesity, neurodegenerative diseases, and reproductive disorders. It is also used as an effective anti-oxidative, anti-inflammatory, antibacterial, and anti-fungal agent. The seed of the plant is especially enriched in several bioactive molecules including polyphenols, saponins, alkaloids, and flavonoids and has demonstrated potential to act as an antidiabetic phytotherapeutic. A novel patented formulation (Fenfuro^®) was developed in our laboratory from the fenugreek seeds which contained >45% furostanolic saponins (HPLC).

Objective: A placebo-controlled clinical compliance study was designed to assess …

Nanoparticles As Antioxidant Agents: A Comprehensive Review, Sulyman Olalekan Ibrahim, Halimat Yusuf Lukman, Fatimat Ronke Abdulkadir, Monsurat Yemisi Bello, Yusuf Oloruntoyin Ayipo, Halimah Funmilayo Babamale, Marili Funmilayo Zubair, Olubunmi Atolani

Al-Bahir

This study seeks to provide a comprehensive overview of the latest progress in the antioxidant properties of nanoparticles. Nanoparticles (NPs) have emerged as a promising tool in several domains of science and industry, including their application as antioxidant agents. The main knowledge gaps seem to be in correctly identifying the make-up of the naturally occurring phytochemicals that give these nano-antioxidants their extraordinary pharmacology and drug-like properties. In many instances, that characterization is done using spectroscopy instrumentation such as fourier-transform Infrared (FT-IR), scanning electron microscope (SEM), and X-ray diffraction analysis (XRD). From literature appraisals, it was discovered that a lot of …

Development Of Long-Acting Antiviral And Antimicrobial Prodrug Nanoformulations, Srijanee Das

Theses & Dissertations

Over the past decade, the global burden of infectious diseases has increased substantively, underscoring the need for more effective treatment strategies. However, the discovery and development of new drugs with desirable safety, pharmacokinetics, and efficacy is a time consuming and costly process with great uncertainty around success rate. As an alternative to new drug development, prodrugs and novel drug delivery systems have increasingly been explored. Both serve to overcome the drug development challenges. Such drug formulations that permit extended dosing intervals of potent native drugs serve multiple purposes by promoting patient adherence to in improving treatment outcomes. This is especially …

Pharmacodynamic Effects Of Zsj-0228 On Complement Protein Deposition In The Kidneys Of Focal Segmental Glomerulosclerosis-Afflicted Mice., Braeden Pinkerton

Theses & Dissertations

Chronic inflammation, when left untreated, may result in significant morbidity and in severe cases, mortality. While glucocorticoids (GCs) are still being extensively used clinically as a class of very potent anti-inflammatory agents, they are also notorious for diverse adverse side effects. To mitigate these side effects, we have developed a polyethylene glycol (PEG)-based prodrug (ZSJ-0228) of dexamethasone (Dex). When tested on rodent models of Lupus Nephritis and Focal Segmental Glomerulosclerosis (FSGS), ZSJ-0228 was found to provide potent and sustained therapeutic efficacy without any detectable typical GC-associated side effects. Given ZSJ-0228’s transient renal exposure after systemic administration, it is yet to …

An Ultra Long-Acting Bictegravir Prodrug Nanocrystal With A Shape-Shifting Pharmacokinetic Tail, Mohammad Ullah Nayan

Theses & Dissertations

While antiretroviral therapy (ART) has significantly reduced human immunodeficiency virus type one (HIV-1) co-morbidities and mortality, adherence to daily oral therapy remains a key barrier to all therapeutic and preventative outcomes. Over the past years, the emergence of long-acting (LA) ART has gained considerable enthusiasm amongst people living with HIV (PLWH) and could potentially simplify dosing regimens and improve treatment outcomes. LA ART could also improve drug adherence, reduce viral transmission, and limit viral drug resistance and systemic toxicities. In response to these needs, a combination of two LA injectable nanocrystalline drugs (CABENUVA) was recently approved for bimonthly administration in …

Efficacy Of Mcl-1 Inhibitors In Multiple Myeloma Cells Resistant To Bortezomib, Emily Nelson, Omar S. Al-Odat, Sabrina M. Paparo, Daniel A. Guirguis, Gabriella Yao, Manoj Pandey, Subash Jonnalagadda, Tulin Budak-Alpdogan

Rowan-Virtua Research Day

Multiple myeloma (MM) is a type of cancer that affects plasma B cells. Patients with MM often experience frequent relapses and can develop resistance to drugs. As a medical researcher, it is important to understand the role of Mcl-1 in preventing intrinsic apoptosis and drug resistance. Mcl-1 belongs to the anti-apoptotic subgroup of Bcl-2 family proteins and plays a crucial role in these processes. Mcl-1 plays a crucial role in driving disease progression and contributing to drug resistance in MM. It has been observed that there is an increased expression of Mcl-1 in 52% of patients with MM during diagnosis, …

Intra-Accumbens Microinfusion Of The Dopamine D3 Receptor Partial Agonist (±)Vk4-40 Does Not Affect Basal Locomotion In Mice, Yeonwoo Sim, Nicole M. Hinds, Amy Hauck Newman, Daniel F. Manvich

Rowan-Virtua Research Day

The opioid epidemic remains a pressing public health crisis, prompting the search for alternative pharmacotherapies for Opioid Use Disorder (OUD). This study explores the potential of the dopamine D3 receptor (D3R) partial agonist, (±)VK4-40, as a novel treatment option. We investigated the impact of intra-nucleus accumbens (NAc) microinfusion of VK4-40 on basal locomotion in mice. Results indicate that VK4-40 did not significantly alter basal locomotion, suggesting that its therapeutic effects may not be mediated through disruptions in generalized motor function. Future research will focus on elucidating the neuropharmacological mechanisms underlying VK4-40's therapeutic actions and exploring its effects on psychostimulant-induced hyperlocomotion. …

The Revolutionary St. Louis Insane Asylum, Julia Talbert

Undergraduate Research Symposium

Even with its grand structure on Arsenal Street towering over the city below, few residents of St. Louis and surrounding areas are aware of the grand history or even existence of the St. Louis Insane Asylum. The building is over 150 years old and was a place of hope, failure, strife, and empathy. The asylum had a large impact on St. Louis and provided revolutionary outlooks, unique perspectives, and curious therapies.

Advancing Text Summarization And Classification: Deep Insights From Transformer-Based Statistical Learning, Kun Bu

USF Tampa Graduate Theses and Dissertations

Artificial Intelligence (AI) is a part of human's daily life nowadays. Machine Learning (ML) as one aspect from AI has been rapidly developing during the past two decades, especially from the statistical learning approaches, which emphasized the use of probability and statistics to model data, such as Support Vector Machines (SVMs) for classification and regression tasks to the ensemble learning techniques, such as Random Forest, Gradient Boosting Machine (GBM), and stacking. Ensemble learning has evolved into a pivotal concept in contemporary machine learning, empowering practitioners to amalgamate multiple models to enhance generalization, accuracy, and robustness. As the field of machine …

An Acute Herb-Drug Interaction Of Magnoliae Officinalis Cortex With Methotrexate Via Inhibiting Multidrug Resistance-Associated Protein 2, Chung-Ping Yu, Pei-Ying Li, Szu-Yu Chen, Shiuan-Pey Lin, Ying-Chen Chen, Lu-Ching Ho, Yow-Wen Hsieh, Yu-Chi Hou

Journal of Food and Drug Analysis

Magnoliae Officinalis Cortex (MOC), an herbal drug, contains polyphenolic lignans mainly magnolol (MN) and honokiol (HK). Methotrexate (MTX), a critical drug for cancers and autoimmune deseases, is a substrate of multidrug resistance-associated protein 2 (MRP2) and breast cancer resistance protein (BCRP). This study investigated the effect of coadministration of MOC on the pharmacokinetics of MTX and relevant mechanisms. Sprague-Dawley rats were orally administered MTX alone and with single dose (2.0 and 4.0 g/kg) and repeated seven doses of MOC (2.0 g/kg thrice daily for 2 days, the 7th dose given at 0.5 h before MTX). The serum concentrations of MTX …

An Auxiliary Strategy Of Partial Least Squares Regression In Pharmacokinetic/Pharmacodynamic Studies: A Case Of Application Of Guhong Injection In Myocardial Ischemia/Reperfusion Rats, Hai-Yang Chen, Chang Li, Chong-Yu Shao, Yu-Jia Wu, Hai-Tong Wan, Yu He

Journal of Food and Drug Analysis

Guhong injection (GHI) has been applied in the therapy of cardio-cerebrovascular disease in clinic, but there is no report about the pharmacokinetic/pharmacodynamic (PK/PD) research on GHI treating myocardial ischemia/reperfusion (MI/R) injury in rats. In this study, eight compounds of GHI in plasma, including N-acetyl-L-glutamine (NAG), chlorogenic acid (CGA), hydroxysafflor yellow A (HSYA), p-coumaric acid (pCA), rutin, hyperoside, kaempferol-3-O-rutinoside, and kaempferol-3-O-glucoside, were quantified by LC-MS/MS. We discovered that the values of t_1/2β, k₁₂, V₂, and CL₂ were larger than those of t_1/2α, k₂₁, V₁, and …

Ionizable Copolymer Functionalized Magnetic Nanocomposite As An Adsorbent For Boosting The Extraction Selectivity Of Aristolochic Acids, Qi-Yue Xie, Yang Chen, Chang-Jun Li, Jia-Bin Zhang, Xiu-Jun Cao, Jun Lu

Journal of Food and Drug Analysis

Aristolochic acid nephropathy (AAN) has drawn increasing public attention. Organic anion transporters (OATs) are considered to be responsible for mediating nephrotoxicity of aristolochic acids (AAs), as AAs are typical OAT1 substrates that exhibit anionic properties and contain one hydrophobic domain. Inspired by the OAT1 three-dimensional structure or substrate/protein interactions involved in transport, we designed a magnetic polymeric hybrid, mimicking the effect of basic and aromatic residues of OAT1, for efficient enriching aristolochic acid I (AA I) and aristolochic acid II (AA II) in Traditional Chinese patent medicines (TCPM). N, N-dimethylaminopropyl acrylamide (DMAPAm) was used as a cationic monomer and copolymerized …

Effect Of Indian Gooseberry Extract On Improving Methylglyoxal-Associated Leptin Resistance In Peripheral Tissues Of High-Fat Diet-Fed Rats, Sheng-Yi Chen, Yue-Ning Huang, Jer-An Lin, Gow-Chin Yen

Journal of Food and Drug Analysis

Increased leptin resistance and methylglyoxal (MG) levels are observed in obese patients. However, whether MG deposits contribute to leptin resistance, oxidative stress, and inflammation in peripheral tissues remains unclear. In addition, the edible fruit of Indian gooseberry (Phyllanthus emblica L.) contains abundant bioactive components such asvitamin C, β-glucogallin (β-glu), gallic acid (GA), and ellagic acid (EA). Water extract of Indian gooseberry fruit (WEIG) and GA has been shown to improve cognitive decline by suppressing brain MG-induced insulin resistance in rats administered a high-fat diet (HFD). Accordingly, this study investigated the functions of WEIG and GA in inhibiting MG-induced leptin …

Pomelo (Citrus Grandis (L.) Osbeck) Sponge Layers As A Potential Source Of Soluble Dietary Fiber: Evaluation Of Its Physicochemical, Structural And Functional Properties, Xiaowei Chen, Jiajia Chen, Jian Peng, Yuanshan Yu, Jijun Wu, Jing Wen, Zhiying Kang, Yanhui Wang, Yujuan Xu, Lu Li

Journal of Food and Drug Analysis

Pomelo sponge layer (PSL) had been considered as a potential source of soluble dietary fiber (SDF), while they were mostly disposed of as waste. To promote high-value utilization of pomelo wastes, this study extracted SDF from PSL of six varieties of pomelo, and their physicochemical, structural and functional properties were investigated. Results indicated that all PSL-SDFs showed good physicochemical and functional properties. Among them, PSL-SDF from grapefruit (GRSDF) showed better water holding capacity and swelling capacity, whereas Shatian pomelo PSL-SDF and Guanxi pomelo PSL-SDF had the highest thermal stability and oil holding capacity, respectively. Furthermore, compared with other PSL-SDFs, GRSDF …

Trans-2-Nonadecyl-4-(Hydroxymethyl)-1,3-Dioxolane (Tnhd) Purified From Freshwater Clams Markedly Alleviates Dimethylnitrosamine-Induced Hepatic Fibrosis, Ya-Ru Kuo, Chen-Yu Tsai, Wei-Sheng Lin, Chi-I Chang, Ching-Shu Lai, Min-Hsiung Pan

Journal of Food and Drug Analysis

Liver fibrosis occurs due to injury or inflammation, which results in the excessive production of collagen and the formation of fibrotic scar tissue that impairs liver function. Despite the limited treatment options available, freshwater clams may hold promise in the treatment of liver fibrosis. In this study, we demonstrated the effects of ethanol extract of freshwater clam (FCE), ethyl acetate extract of FCE (EA-FCE), and trans-2-nonadecyl-4-(hydroxymethyl)-1,3-dioxolane (TNHD) on liver fibrosis induced by dimethylnitrosamine (DMN). Administration of FCE and TNHD alleviated liver injury, including tissue damage, necrosis, inflammation scores, fibrosis scores, serum enzymes, and triglyceride levels. Furthermore, we analyzed the expression …

Facile One-Pot Synthesis And Anti-Microbial Activity Of Novel 1,4-Dihydropyridine Derivatives In Aqueous Micellar Solution Under Microwave Irradiation, Asmita Goswami, Navneet Kaur, Manvinder Kaur, Kishanpal Singh, Harvinder Singh Sohal, Haesook Han, Pradip K. Bhowmik

Chemistry and Biochemistry Faculty Research

The current study describes a novel and eco-conscious method to synthesize 1,4-dihydropyridine derivatives utilizing an aqueous micellar solution containing aluminum dodecyl sulfate, Al(DS)3, using readily available starting material. The final products were synthesized with excellent yields within remarkably quick reaction durations, promoting remarkable atom economy and minimizing environmental impacts. The present protocol has several advantages over other methodologies in terms of high yield (up to 97%) with excellent purity. Further, the synthesized 1,4-DHPs exhibit favorable to excellent resistance against examined bacterial and fungal species. Intriguingly, polar groups on the phenyl ring (5b, 5c, 5i and 5j) make the 1,4-DHPs equally …

Human Mitragynine And 7-Hydroxymitragynine Pharmacokinetics After Single And Multiple Daily Doses Of Oral Encapsulated Dried Kratom Leaf Powder, Marilyn A. Huestis, Martin A. Brett, John Bothmer, Ramsey Atallah

Institute of Emerging Health Professions Faculty Papers

Kratom leaves, consumed by millions worldwide as tea or ground leaf powder, contain multiple alkaloids, with mitragynine being the most abundant and responsible for most effects. Mitragynine is a partial µ-opioid receptor agonist and competitive antagonist at κ- and δ-opioid receptors; however, unlike morphine, it does not activate the β-arrestin-2 respiratory depression pathway. Due to few human mitragynine data, the largest randomized, between-subject, double-blind, placebo-controlled, dose-escalation study of 500–4000 mg dried kratom leaf powder (6.65–53.2 mg mitragynine) was conducted. LC-MS/MS mitragynine and 7-hydroxymitragynine plasma concentrations were obtained after single and 15 daily doses. Mitragynine and 7-hydroxymitragynine C_max increased dose …

Metabolic Stability And Metabolite Identification Of N-Ethyl Pentedrone Using Rat, Mouse And Human Liver Microsomes, Alexandre Barcia Godoi, Natalícia De Jesus Antunes, Kelly Francisco Cunha, Aline Franco Martins, Marilyn A. Huestis, Jose Luiz Costa

Institute of Emerging Health Professions Faculty Papers

New Psychoactive Substances (NPSs) are defined as a group of substances produced from molecular modifications of traditional drugs. These molecules represent a public health problem since information about their metabolites and toxicity is poorly understood. N-ethyl pentedrone (NEP) is an NPS that was identified in the illicit market for the first time in the mid-2010s, with four intoxication cases later described in the literature. This study aims to evaluate the metabolic stability of NEP as well as to identify its metabolites using three liver microsomes models. To investigate metabolic stability, NEP was incubated with rat (RLM), mouse (MLM) and human …