Clinical Studies on Bioavailability, Biotransformation, Biokinetics and Bioeffects of Phytochemicals

A special issue of Journal of Clinical Medicine (ISSN 2077-0383). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: closed (20 June 2022) | Viewed by 11455

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Department of Biomedical, Surgical and Dental Sciences, Università degli Studi di Milano, 20133 Milan, Italy
Interests: essential oils; bioactive phytochemicals; ethnopharmacology; antimicrobial resistance; one health; food security
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Special Issue Information

Dear Colleagues,

The health-promoting effects of phytochemicals strictly depend on their oral bioavailability, which, in turn, relies on i) the individual biotransformation systems; ii) the chemical structure and properties of each compound; and iii) the complexity of the plant matrix consisting of seeds, leaves, roots, stems, flowers, and other plant tissues and organs. After intake, bioactive compounds have to be absorbed, distributed, and metabolized before reaching the target tissues and cells; finally, the metabolites of native compounds are excreted in urine and feces, mainly as water-soluble conjugates (methyl, glucuronide, and sulfate derivatives). The gastrointestinal tract, the systemic circulation, and the urinary system are involved in these complex and coordinated biotransformation processes including enterohepatic circulation, and Phase I (oxidation, reduction and hydrolysis) and Phase II (conjugation) metabolisms in enterocytes and hepatocytes. Finally, phytochemicals not absorbed in the small intestine reach the large intestine where they are biotransformed by the colonic microbiota. Indeed, though phytochemicals are commonly considered “natural” products, i.e., safe and healthy, it is not actually always so: Plant metabolites are recognized as xenobiotics by the human organism, and therefore, they are extensively metabolized.

In this very wide context, we invite investigators to submit both original research and review articles that explore all these aspects.

Prof. Dr. Marcello Iriti
Guest Editor

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Keywords

  • nutraceuticals
  • functional foods
  • phytotherapeutics
  • gut microbiota
  • metabolomics

Published Papers (5 papers)

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Research

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11 pages, 1212 KiB  
Article
Efficacy and Safety of the Cudrania tricuspidata Extract on Functional Dyspepsia: A Randomized Double-Blind Placebo-Controlled Multicenter Study
by Jinyoung Shin, Tae-Hoon Oh, Joo-Yun Kim, Jae-Jung Shim and Jung-Lyoul Lee
J. Clin. Med. 2021, 10(22), 5323; https://doi.org/10.3390/jcm10225323 - 16 Nov 2021
Cited by 2 | Viewed by 1737
Abstract
Cudrania tricuspidata is a folk remedy used to treat inflammation in patients with tumors or liver damage. This study investigated the efficacy of Cudrania tricuspidata extract (CTE) for relieving the symptoms of functional dyspepsia. In an 8-week, randomized, double-blind, placebo-controlled study, 100 adults [...] Read more.
Cudrania tricuspidata is a folk remedy used to treat inflammation in patients with tumors or liver damage. This study investigated the efficacy of Cudrania tricuspidata extract (CTE) for relieving the symptoms of functional dyspepsia. In an 8-week, randomized, double-blind, placebo-controlled study, 100 adults with any condition featured in the Rome IV criteria and a Gastrointestinal Symptoms Scale (GIS) score ≥4 were randomly allocated to take either a placebo (maltodextrin) or a 50 mg CTE tablet, which equally included celluloses, magnesium stearate, and silicon dioxide, twice daily, 20 January 2020, and 3 August 2020. Among the 83 participants finally analyzed, the CTE group was associated with a significant reduction in the gastrointestinal symptom rating scale (day 0: 8.0 ± 5.2, day 28: 4.7 ± 3.9, and day 56: 2.3 ± 2.4, p < 0.001, respectively) in comparison with the control group (day 0: 8.1 ± 4.7, day 28: 7.8 ± 5.7, and day 56: 7.5 ± 6.6, p > 0.05) after adjusting for smoking, drinking, eating habits, stress levels, and caffeine intake. The CTE group resulted in significant improvements of GIS, Nepean Dyspepsia Index (Korean version), and functional dyspepsia-related quality of life over time. There were no different adverse events (p = 0.523). These findings suggest that CTE is safe and efficacious for alleviating gastrointestinal symptoms in patients with functional dyspepsia. Full article
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11 pages, 793 KiB  
Article
Development of p-Coumaric Acid Analysis in Human Plasma and Its Clinical Application to PK/PD Study
by Hohyun Kim, Yunkyoung Choi, Yongwun An, Young-Rim Jung, Jin-Yong Lee, Hong-Jin Lee, Jihoon Jeong, Zisoo Kim and Kyeongsoon Kim
J. Clin. Med. 2021, 10(1), 108; https://doi.org/10.3390/jcm10010108 - 30 Dec 2020
Cited by 6 | Viewed by 2353
Abstract
It has been recognized that p-Coumaric acid (p-CA) has protective effects as an antioxidant, anti-inflammatory agent. A sensitive and efficient Liquid Chromatography-Mass Spectrometry (LC-MS) method for maximum determination of p-CA in human plasma has been established using Ultra-performance liquid [...] Read more.
It has been recognized that p-Coumaric acid (p-CA) has protective effects as an antioxidant, anti-inflammatory agent. A sensitive and efficient Liquid Chromatography-Mass Spectrometry (LC-MS) method for maximum determination of p-CA in human plasma has been established using Ultra-performance liquid Chromatography-tandem mass Spectrometry (UPLC-MS/MS). This study provides the developed analysis of p-CA extracted from Bambusae Caulis in Taeniam (BC) to examine the improvement of the treatment p-CA, IGF-1 and Osteocalcin level in human children which are important factors on the growth of children’s height through Pharmacokinetics/Pharmacodynamics (PK/PD) model. p-CA and internal standard in a plasma sample were detected by the Multiple Reaction Monitoring (MRM) scan mode with positive ion detection. The sample participating in the study was made of 34 subjects (placebo = 18, treatment = 16). The subjects were enrolled to be randomized to the control group and BC group. Randomized subjects took tested treatment twice a day, three capsules with oral administration (258 mg/capsule) each time after a meal. Standard calibration curves (reproducibility) were constructed and the lower limit of quantitation (LLOQ) for p-CA was found to be 0.2 ng/mL on injection of the sample into the UPLC-MS/MS system. Accuracy and precision were evaluated and the intra-accuracy was 99.2–103.8% with precision of 1.0–5.6% and inter-accuracy was 99.6–108.4% and precision of 1.3–6.4% for p-CA. The method has been successfully applied to PK/PD studies of p-CA in human plasma. The p-CA, BC in Taeniam extract increased the level of IGF-1 and Osteocalcin, and changed the height from baseline, which suggested that the p-CA could play an important role in longitudinal bone growth. Therefore, the p-CA extracted from BC in Taeniam might be a good alternative medicine to growth hormone (GH) therapy. Full article
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13 pages, 775 KiB  
Article
Efficacy and Safety of Combined Extracts of Cornus officinalis and Ribes fasciculatum for Body Fat Reduction in Overweight Women
by Eunkuk Park, Chang Gun Lee, Jeonghyun Kim, Jae-Heon Kang, Young Gyu Cho and Seon-Yong Jeong
J. Clin. Med. 2020, 9(11), 3629; https://doi.org/10.3390/jcm9113629 - 11 Nov 2020
Cited by 6 | Viewed by 1995
Abstract
Obesity is a medical condition that presents excessive fat accumulation with high risk of serious chronic diseases. The aim of this clinical trial is to investigate the anti-obesity effects of Cornus officinalis (CO) and Ribes fasciculatum (RF) on body fat reduction in Korean [...] Read more.
Obesity is a medical condition that presents excessive fat accumulation with high risk of serious chronic diseases. The aim of this clinical trial is to investigate the anti-obesity effects of Cornus officinalis (CO) and Ribes fasciculatum (RF) on body fat reduction in Korean overweight women. A total of 147 overweight female participants enrolled in double-blinded clinical trial for 12 weeks and 76 participants completed the clinical study. Participants were treated with four CO and RF mixture (COEC; 400 mg per tablet) or four placebo tablets once a day. Obesity associated parameters (body weight, body mass index (BMI), waist circumference, waist-to-hip ratio, body fat percentage and body fat mass) and safety assessment were analyzed. After 12 weeks of COEC treatment, primary outcomes such as body fat percentage (0.76% vs. 0.01%; p = 0.022) and mass (1.1 kg vs. 0.5 kg; p = 0.049) were significantly decreased. In addition, the results were statistically significant between the COEC and placebo groups, strongly indicated that COEC had anti-obesity effects on overweight women. Secondary outcomes—including body weight, waist and hip circumference, waist-to-hip ratio, body mass index and computed tomography measurement of visceral fat area, subcutaneous fat area, total abdominal fat area and visceral-to-subcutaneous fat ratio—were reduced in COEC-treated group, but no statistical differences were found between the COEC and placebo groups. The safety assessment did not differ between the two groups. These results suggest that treatment of COEC extract reduces body fat percentage and mass in Korean overweight women, indicating it as a protective functional agent for obesity. Full article
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10 pages, 1125 KiB  
Article
Polyphenol Bioavailability and Plasma Antiradical Capacity in Healthy Subjects after Acute Intake of Pigmented Rice: A Crossover Randomized Controlled Clinical Trial
by Sara Vitalini, Andrea Sardella, Daniela Fracassetti, Rita Secli, Antonio Tirelli, Giovanni Lodi, Antonio Carrassi, Elena Maria Varoni and Marcello Iriti
J. Clin. Med. 2020, 9(10), 3209; https://doi.org/10.3390/jcm9103209 - 5 Oct 2020
Cited by 7 | Viewed by 2169
Abstract
Health-promoting effects of plant foods have been emphasized in the last few decades and ascribed to the bioactive phytochemicals present therein—in particular, phenylpropanoids. The latter have been investigated for a number of preclinical biological activities, including their antioxidant power. Due to the paucity [...] Read more.
Health-promoting effects of plant foods have been emphasized in the last few decades and ascribed to the bioactive phytochemicals present therein—in particular, phenylpropanoids. The latter have been investigated for a number of preclinical biological activities, including their antioxidant power. Due to the paucity of human studies, in this randomized intervention trial, we investigated whether the acute intake of pigmented rice could increase the plasma bioactive levels and antiradical power in twenty healthy subjects. A crossover randomized controlled clinical trial was conducted on 19 volunteers. Artemide and Venere black rice cultivars were tested, while brown rice Carnaroli was used as a control. Each patient received randomly one serving (100 g) of rice on three different experimental days, separated by a 7-day washout period. After baseline blood withdrawal, time-course changes of plasma polyphenols, flavonoids and radical-scavenging capacity were determined at 30, 60, 120 and 180 min post rice intake. Compared to Carnaroli rice, the two black rice cultivars significantly increased the plasma levels of polyphenols and flavonoids at 60 and 120 min and, correspondingly, the plasma antiradical power at 60 min after consumption. Pigmented rice consumption can contribute to diet-related health benefits in humans. Full article
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14 pages, 15413 KiB  
Protocol
Pharmacokinetics and Metabolomic Profiling of Metformin and Andrographis paniculata: A Protocol for a Crossover Randomised Controlled Trial
by Khim Boon Tee, Luqman Ibrahim, Najihah Mohd Hashim, Mohd Zuwairi Saiman, Zaril Harza Zakaria and Hasniza Zaman Huri
J. Clin. Med. 2022, 11(14), 3931; https://doi.org/10.3390/jcm11143931 - 6 Jul 2022
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Abstract
This protocol aims to profile the pharmacokinetics of metformin and Andrographis paniculata (AP) and continue with untargeted pharmacometabolomics analysis on pre-dose and post-dose samples to characterise the metabolomics profiling associated with the human metabolic pathways. This is a single-centre, open-labelled, three periods, crossover, [...] Read more.
This protocol aims to profile the pharmacokinetics of metformin and Andrographis paniculata (AP) and continue with untargeted pharmacometabolomics analysis on pre-dose and post-dose samples to characterise the metabolomics profiling associated with the human metabolic pathways. This is a single-centre, open-labelled, three periods, crossover, randomised-controlled, single-dose oral administration pharmacokinetics and metabolomics trial of metformin 1000 mg (n = 18), AP 1000 mg (n = 18), or AP 2000 mg (n = 18) in healthy volunteers under the fasting condition. Subjects will be screened according to a list of inclusion and exclusion criteria. Investigational products will be administered according to the scheduled timeline. Vital signs and adverse events will be monitor periodically, and standardized meals will be provided to the subjects. Fifteen blood samples will be collected over 24 h, and four urine samples will be collected within a 12 h period. Onsite safety monitoring throughout the study and seven-day phone call safety follow-up will be compiled after the last dose of administration. The plasma samples will be analysed for the pharmacokinetics parameters to estimate the drug maximum plasma concentration. Untargeted metabolomic analysis between pre-dose and maximum plasma concentration (Cmax) samples will be performed for metabolomic profiling to identify the dysregulation of human metabolic pathways that link to the pharmacodynamics effects. The metformin arm will focus on the individualised Cmax plasma concentration for metabolomics study and used as a model drug. After this, an investigation of the dose-dependent effects will be performed between pre-dose samples and median Cmax concentration samples in the AP 1000 mg and AP 2000 mg arms for metabolomics study. The study protocol utilises a crossover study design to incorporate a metabolomics-based study into pharmacokinetics trial in the drug development program. The combination analyses will complement the interpretation of pharmacological effects according to the bioavailability of the drug. Full article
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