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1.
J Pharm Biomed Anal ; 246: 116188, 2024 Aug 15.
Article in English | MEDLINE | ID: mdl-38733761

ABSTRACT

The World Anti-Doping Agency (WADA) has included higenamine in the ß2 agonist (S3) category of the Prohibited List since 2017 due to its pharmacological effects on adrenergic receptors. Although higenamine contained in Chinese herbal medicines has been identified by previous studies, comprehensive investigation on the higenamine content of Chinese herbs and their concentrated preparations is still required. This study aimed to determine the levels of higenamine in Chinese medicinal materials and their concentrated preparations used in Chinese medicine prescriptions in Taiwan. The levels of higenamine in Chinese medicinal materials, including Cortex Phellodendri, Flos Caryophylli, Fructus Euodiae, Fructus Kochiae, Plumula Nelumbinis, Radix Aconiti Preparata, Radix Aconiti Lateralis Preparata, and Radix Asari, and their concentrated preparations were determined by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Our results showed that the amounts of higenamine were detected and quantified in studied Chinese medicinal materials and their concentrated preparations, except for Flos Caryophylli, Radix Aconiti Preparata, and Radix Aconiti Lateralis Preparata. Plumula Nelumbinis and Cortex Phellodendri have higher levels of higenamine when compared to other Chinese herbs tested in the present study. The highest level of higenamine was 2100 µg/g found in the Plumula Nelumbinis medicinal material. In contrast with Plumula Nelumbinis and Cortex Phellodendri, higenamine levels below 10 µg/g were found in other most of the studied Chinese medicinal materials and their concentrated preparations. This study confirmed that various Chinese herbs and their concentrated preparations contained higenamine, and it provided more coherent and comprehensive information for reducing the potential risk of higenamine misuse in sports.


Subject(s)
Alkaloids , Doping in Sports , Drugs, Chinese Herbal , Tandem Mass Spectrometry , Tandem Mass Spectrometry/methods , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/analysis , Doping in Sports/prevention & control , Alkaloids/analysis , Alkaloids/chemistry , Chromatography, Liquid/methods , Tetrahydroisoquinolines/analysis , Tetrahydroisoquinolines/chemistry , Humans , Substance Abuse Detection/methods , Taiwan , Chromatography, High Pressure Liquid/methods , Liquid Chromatography-Mass Spectrometry
2.
Drug Test Anal ; 2024 Apr 23.
Article in English | MEDLINE | ID: mdl-38653500

ABSTRACT

To prevent athletes from unintentional doping, the anti-doping authorities in Taiwan have launched several sports-prohibited substances inquiry services since 2008. This study aimed to enhance the prevention of sports-prohibited substance misuse by analyzing data collected from major nationwide service systems, enabling the identification of trends in athletes' exposure to drugs and prohibited substances. The study collected over 30,000 data points from three major national anti-doping inquiry systems, spanning from 2008 to 2022. The information of the users consulted products, prohibited substances, and sports disciplines in the data were calculated and categorized. The usage of inquiry systems has shown an increasing trend from 2008 to 2022. Athletes comprised the majority of users (> 40%), significantly outnumbering other user groups (all below 20%). Among the inquiries, Western medicine accounted for the highest percentage (up to 79.6%), and it also contained the majority of the prohibited substances. Interestingly, traditional Chinese medicines had a higher chance (35.9%) of containing prohibited substances, as indicated by the mobile application. The prohibited substances mainly belonged to class S6 stimulants and S9 glucocorticoids. Among the daily medicinal products and nutritional supplements encountered by sports personnel, approximately 30% of them were found to contain prohibited substances. Future educational efforts should focus on raising awareness about traditional Chinese medicines and drugs for the common cold, ADHD, and pain relief, as well as their regulation, to prevent the misuse of prohibited substances.

3.
BMC Med Educ ; 23(1): 808, 2023 Oct 27.
Article in English | MEDLINE | ID: mdl-37891558

ABSTRACT

BACKGROUND: Taiwan's unique health behaviour, such as extensive exposure to Chinese Herbal Medicine (CHM), has introduced a risk of inadvertent doping among competing athletes. Pharmacy professionals have an imperative role in advising athletes on the safe use of medicines. This study provides an overview of anti-doping knowledge and educational needs among pharmacists in Taiwan and examines influencing factors. METHODS: A cross-sectional online questionnaire survey consisting of five domains, namely demographic characteristics, source of prohibited substances, identification of prohibited substances, understanding of doping control, and education needs on anti-doping, was distributed to the registered pharmacists in Taiwan. In total, 491 responses were included in the analyses. RESULTS: Respondents (65% female, aged 41.9 ± 11.4 years, with 68% having a Bachelor's degree) reported a moderate anti-doping knowledge score of 37.2 ± 4.9, ranging from 21 to 48 (out of 51). Fifteen per cent of them had the experience of being counselled about drug use in sports. Higher knowledge scores were observed in younger respondents, showing an age-dependent effect (p < 0.001). Individuals practising in southern Taiwan (compared to northern Taiwan) and those working at clinics (compared to hospitals) exhibited lower knowledge. Most of the respondents (90%) knew that stimulant ephedrine is prohibited in sports, but few had recognised diuretic furosemide (38%) and CHM (7%) containing ß2-agonist higenamine. Approximately 90% of respondents agreed with the need for anti-doping education. CONCLUSIONS: This study highlights the heterogeneity of anti-doping knowledge among pharmacy professionals and provides practical relevance in organising future educational topics and research-based activities.


Subject(s)
Doping in Sports , Sports , Humans , Female , Male , Doping in Sports/prevention & control , Pharmacists , Cross-Sectional Studies , Health Knowledge, Attitudes, Practice
4.
Environ Pollut ; 333: 122087, 2023 Sep 15.
Article in English | MEDLINE | ID: mdl-37348696

ABSTRACT

Biological testing is a key component of the current anti-doping programme implemented by the authorities to detect doping in sports. Strategies such as longitudinal individualised data analysis and sport-specific analysis have been developed to increase the comprehensiveness of the testing. However, the trends of drug misuse in sports might not be effectively captured through today's testing plan. Wastewater testing, assembling individual-level data of a designated group to produce population-level results in one single aggregated sample, can be employed to as a complementary strategy offering added value for doping control. This paper presents an updated summary of the status of anti-doping testing and analytical methodologies for wastewater. The available literature on wastewater-based analyses of drugs prohibited in sports is reviewed. Publications surrounding sporting activities or competitions and others relevant to sports doping are selected. We debate between potential strategies and major limitations of using wastewater monitoring in anti-doping. Knowledge gaps and research directions, specifically on metabolites, stability, sensitivity, and ethical and legal considerations, are discussed. Choosing different wastewater sampling sites allows target sub-population that involved competing athletes and potentially reveal sport-specific or athlete-level-specific behaviour. Sampling from on-board toilets or athlete villages could target international-level athletes, sampling from the dormitories of national training centres allows monitoring of national-level athletes on a daily basis, and sampling from sports stadiums provides a full picture of drug use in the general population during an event. Confounding occurs as (i) the presence of non-athlete composition and the difficulty of analyses to be completely selective to the athlete population; and (ii) the identification of compounds prescribed legitimately with Therapeutic Use Exemptions, only banned in-competition, and naturally occurring. The practicalities of the approach are contextualised in monitoring the non-threshold substances such as anabolic agents, selective androgen receptor modulators, metabolic modulators, and hypoxia-inducible factor activators.


Subject(s)
Doping in Sports , Drug Misuse , Sports , Humans , Wastewater , Substance Abuse Detection/methods , Athletes
5.
Drug Test Anal ; 15(1): 75-83, 2023 Jan.
Article in English | MEDLINE | ID: mdl-36097849

ABSTRACT

Beta-blockers have been prohibited by the World Anti-Doping Agency (WADA) in certain sports, but insufficient research data make it difficult to distinguish between therapeutic uses or misuses. This study aimed at investigating the urinary excretion pattern following beta-blocker ophthalmic drops and the potential risk of constituting an adverse analytical finding (AAF) in sports. Prescribed timolol and carteolol ophthalmic drops were used in healthy participants and glaucoma patients. The urine samples were then collected to investigate the urinary excretion pattern following acute and chronic administration of the above beta-blocker ophthalmic drops. The liquid chromatograph-tandem mass spectrometry method was applied for measuring urinary beta-blockers. Our results demonstrated that the levels of both urinary timolol and carteolol exceeded the minimum reporting levels (MRL) following acute and chronic administration. The highest levels of urinary timolol and carteolol observed in the present study were 255.7 and 923.8 ng/ml, respectively. Regarding the acute administration of timolol ophthalmic drop, 26.19 (11/42) of urine samples were detected with timolol higher than the MRL in timed and random sampling. In contrast, the acute administration of carteolol ophthalmic drops made the carteolol levels higher than the MRL among most urine samples. On the other hand, 36.36% (4/11) of urine samples were detected with beta-blockers higher than the MRL during the chronic administration of timolol and carteolol ophthalmic drops. In the context of receiving ophthalmic beta-blocker medications, the present study has highlighted the potential risk of constituting an AAF in specific sports and suggests strengthening athletes' awareness of therapeutic use exemptions.


Subject(s)
Carteolol , Sports , Humans , Timolol/adverse effects , Carteolol/adverse effects , Adrenergic beta-Antagonists , Ophthalmic Solutions/adverse effects
6.
Nutrients ; 14(8)2022 Apr 17.
Article in English | MEDLINE | ID: mdl-35458232

ABSTRACT

Astragalus membranaceus (AM) is classified as a high-class traditional herbal medicine, which has strengthened vitality and multifunctional pharmacological activities, but limited empirical evidence is available to support its effects in muscular hypertrophy. It evokes skeletal muscle hypertrophy by increasing anabolic pathway, which is essential to prevent sarcopenia in elderly population. In this study, we examined the effects of AM on skeletal muscle hypertrophy by focusing on the molecular mechanism. We employed an in vitro model to investigate whether AM-treated skeletal muscle, as represented by myotube C2C12 cells, was hypertrophic, and to further investigate the efficacy of AM-activated phosphorylation of PI3K/Akt/mTOR signaling that must occur prior to myotube hypertrophy. The results showed that the myotubes formed larger multinucleated myotubes with increased diameter and thickness (1.16-fold relative to control group, p < 0.05). Administration of PI3K and mTOR inhibitors abolished AM-induced muscular hypertrophy. Moreover, AM-induced PI3K-mediated myotube hypertrophy was accompanied by the activation of Akt and mTOR signaling. We concluded that the AM is a nutritional activator to enhance muscular hypertrophy by increasing PI3K/Akt/mTOR signaling phosphorylation. As the AM is effective in myotube hypertrophy, AM and its derivatives may be promising candidates for ergogenic aid to prevent sarcopenia.


Subject(s)
Astragalus propinquus , Phosphatidylinositol 3-Kinases , Sarcopenia , TOR Serine-Threonine Kinases , Aged , Astragalus propinquus/metabolism , Humans , Hypertrophy , Muscle Fibers, Skeletal , Phosphatidylinositol 3-Kinases/metabolism , Phosphorylation , Proto-Oncogene Proteins c-akt/metabolism , Sarcopenia/drug therapy , Sarcopenia/metabolism , Sarcopenia/prevention & control , TOR Serine-Threonine Kinases/metabolism
7.
Article in English | MEDLINE | ID: mdl-34574458

ABSTRACT

In the fight against sports doping, the Athlete Biological Passport (ABP) system aims to indirectly unveil the doping incidents by monitoring selected biomarkers; however, several unexplored extrinsic factors may dampen a fair interpretation of ABP profiles. Chinese herbal medicine (CHM) plays a pivotal role in the health care system, and some remedies have a long history of being used to treat anaemia. In this study, we addressed the concerns of whether the CHM administration could yield a measurable effect on altering the ABP haematological variables. Forty-eight healthy volunteers were randomly assigned to receive two-week oral administration of one of the six selected CHM products that are commonly prescribed in Taiwan (eight subjects per group). Their blood variables were determined longitudinally in the phases of baseline, intervention, and recovery over 5 weeks. Blood collection and analyses were carried out in strict compliance with relevant operating guidelines. In the groups receiving Angelicae Sinensis Radix, Astragali Radix, and Salviae Miltiorrhizae Radix et Rhizoma, a significant increased reticulocyte percentage and decreased OFF-hr Score were manifested during the intervention, and such effects even sustained for a period of time after withdrawal. All other variables, including haemoglobin and Abnormal Blood Profile Score, did not generate statistical significance. Our results show that the use of CHM may impact the ABP haematological variables. As a consequence, we recommend athletes, particularly those who have been registered in the testing pool, should be aware of taking specific Chinese herbal-based treatment or supplementation, and document any of its usage on the anti-doping forms.


Subject(s)
Doping in Sports , Drugs, Chinese Herbal , Sports , Athletes , Humans , Substance Abuse Detection
8.
Drug Test Anal ; 13(10): 1776-1782, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34309209

ABSTRACT

Higenamine is a ß2 -agonist that has been prohibited in sports by the World Anti-Doping Agency. Higenamine could potentially promote anabolism and lipolysis; however, its crucial pharmacokinetics data, particularly muscle distribution, remain unavailable. The present study aims to investigate the blood-to-muscle distribution as well as the urinary excretion of higenamine in laboratory rats. In the first experiment, the microdialysis technique was employed to continuously measure free, protein-unbound concentrations in blood and muscle for 90 min (sampling at a 5-min interval) after rats received IV infusion of higenamine. The mean half-lives of higenamine in blood and muscle were 17.9 and 19.0 min, respectively. The blood-to-muscle distribution ratio (AUCmuscle /AUCblood ) of higenamine was estimated to be 22%. In the second experiment, rats were orally administered with a single-dose higenamine, and their urine samples were profiled at a 12-h interval for up to 48 h. Results showed only a small portion of total consumption (1.44%, ranging 0.71%-2.50%) was excreted in the urine. Among these time points, about 43% cumulative amount of higenamine was eliminated within the first 12 h. Our data suggested that one-quarter of the unbound higenamine rapidly penetrates from the vessels into muscle, distributes to the interstitial fluid, then eliminates from the rat in a short span of time. The muscle tissue is likely to have a low binding affinity for higenamine, and renal excretion plays a minor role in its elimination. Together, our findings provide valuable pharmacokinetics data that may gain deeper insights into higenamine's role in skeletal muscle functions.


Subject(s)
Adrenergic beta-Agonists/pharmacokinetics , Alkaloids/pharmacokinetics , Doping in Sports/prevention & control , Tetrahydroisoquinolines/pharmacokinetics , Animals , Area Under Curve , Half-Life , Male , Microdialysis/methods , Rats , Rats, Sprague-Dawley , Tissue Distribution
9.
Sci Rep ; 11(1): 10790, 2021 05 24.
Article in English | MEDLINE | ID: mdl-34031457

ABSTRACT

The regenerative effect of Epimedium and its major bioactive flavonoid icariin (ICA) have been documented in traditional medicine, but their effect on sarcopenia has not been evaluated. The aim of this study was to investigate the effects of Epimedium extract (EE) on skeletal muscle as represented by differentiated C2C12 cells. Here we demonstrated that EE and ICA stimulated C2C12 myotube hypertrophy by activating several, including IGF-1 signal pathways. C2C12 myotube hypertrophy was demonstrated by enlarged myotube and increased myosin heavy chains (MyHCs). In similar to IGF-1, EE/ICA activated key components of the IGF-1 signal pathway, including IGF-1 receptor. Pre-treatment with IGF-1 signal pathway specific inhibitors such as picropodophyllin, LY294002, and rapamycin attenuated EE induced myotube hypertrophy and MyHC isoform overexpression. In a different way, EE induced MHyC-S overexpression can be blocked by AMPK, but not by mTOR inhibitor. On the level of transcription, EE suppressed myostatin and MRF4 expression, but did not suppress atrogenes MAFbx and MuRF1 like IGF-1 did. Differential regulation of MyHC isoform and atrogenes is probably due to inequivalent AKT and AMPK phosphorylation induced by EE and IGF-1. These findings suggest that EE/ICA stimulates pathways partially overlapping with IGF-1 signaling pathway to promote myotube hypertrophy.


Subject(s)
Chromones/pharmacology , Flavonoids/pharmacology , Morpholines/pharmacology , Myoblasts/cytology , Podophyllotoxin/analogs & derivatives , Signal Transduction/drug effects , Sirolimus/pharmacology , Animals , Cell Differentiation , Cell Line , Gene Expression Regulation/drug effects , Hypertrophy , Insulin-Like Growth Factor I/genetics , Insulin-Like Growth Factor I/metabolism , Mice , Myoblasts/drug effects , Myoblasts/metabolism , Myoblasts/pathology , Myosin Heavy Chains/genetics , Myosin Heavy Chains/metabolism , Podophyllotoxin/pharmacology
10.
Nutrients ; 14(1)2021 Dec 25.
Article in English | MEDLINE | ID: mdl-35010953

ABSTRACT

Exercise-induced muscle damage (EIMD) is characterized by a reduction in functional performance, disruption of muscle structure, production of reactive oxygen species, and inflammatory reactions. Ginseng, along with its major bioactive component ginsenosides, has been widely employed in traditional Chinese medicine. The protective potential of American ginseng (AG) for eccentric EIMD remains unclear. Twelve physically active males (age: 22.4 ± 1.7 years; height: 175.1 ± 5.7 cm; weight: 70.8 ± 8.0 kg; peak oxygen consumption [V˙O2peak] 54.1 ± 4.3 mL/kg/min) were administrated by AG extract (1.6 g/day) or placebo (P) for 28 days and subsequently challenged by downhill (DH) running (-10% gradient and 60% V˙O2peak). The levels of circulating 8-iso-prostaglandin F 2α (PGF2α), creatine kinase (CK), interleukin (IL)-1ß, IL-4, IL-10, and TNF-α, and the graphic pain rating scale (GPRS) were measured before and after supplementation and DH running. The results showed that the increases in plasma CK activity induced by DH running were eliminated by AG supplementation at 48 and 72 h after DH running. The level of plasma 8-iso-PGF2α was attenuated by AG supplementation immediately (p = 0.01 and r = 0.53), 2 h (p = 0.01 and r = 0.53) and 24 h (p = 0.028 and r = 0.45) after DH running compared with that by P supplementation. Moreover, our results showed an attenuation in the plasma IL-4 levels between AG and P supplementation before (p = 0.011 and r = 0.52) and 72 h (p = 0.028 and r = 0.45) following DH running. Our findings suggest that short-term supplementation with AG alleviates eccentric EIMD by decreasing lipid peroxidation and promoting inflammatory adaptation.


Subject(s)
Exercise/adverse effects , Lipid Peroxidation/drug effects , Muscular Diseases/drug therapy , Panax/chemistry , Phytotherapy , Plant Extracts/therapeutic use , Cytokines/genetics , Cytokines/metabolism , Double-Blind Method , Gene Expression Regulation/drug effects , Humans , Inflammation/drug therapy , Male , Muscular Diseases/etiology , Plant Extracts/chemistry , Young Adult
11.
Molecules ; 25(14)2020 Jul 08.
Article in English | MEDLINE | ID: mdl-32650503

ABSTRACT

Sesamin (SSM) is a water-insoluble compound that is easily eliminated by liver metabolism. To improve the solubility and bioavailability of SSM, this study developed and characterized a self-nanoemulsifying drug delivery system (SNEDDS) for the oral delivery of SSM and conducted pharmacokinetic assessments. Oil and surfactant materials suitable for SNEDDS preparation were selected on the basis of their saturation solubility at 37 ± 0.5 °C. The mixing ratios of excipients were determined on the basis of their dispersibility, transmittance (%), droplet sizes, and polydispersity index. An SNEDDS (F10) formulation comprising glyceryl trioctanoate, polyoxyethylene castor oil, and Tween 20 at a ratio of 10:10:80 (w/w/w) was the optimal formulation. This formulation maintained over 90% of its contents in different storage environments for 12 weeks. After the self-emulsification of SNEDDS, the SSM dispersed droplet size was 66.4 ± 31.4 nm, intestinal permeability increased by more than three-fold, relative bioavailability increased by approximately 12.9-fold, and absolute bioavailability increased from 0.3% to 4.4%. Accordingly, the developed SNEDDS formulation can preserve SSM's solubility, permeability, and bioavailability. Therefore, this SNEDDS formulation has great potential for the oral administration of SSM, which can enhance its pharmacological application value.


Subject(s)
Dioxoles , Drug Carriers , Lignans , Nanoparticles/chemistry , Animals , Dioxoles/chemistry , Dioxoles/pharmacokinetics , Dioxoles/pharmacology , Drug Carriers/chemistry , Drug Carriers/pharmacokinetics , Drug Carriers/pharmacology , Emulsions , Lignans/chemistry , Lignans/pharmacokinetics , Lignans/pharmacology , Male , Permeability , Polysorbates/chemistry , Rats , Rats, Sprague-Dawley , Solubility
12.
Pharm Biol ; 58(1): 545-552, 2020 Dec.
Article in English | MEDLINE | ID: mdl-32538243

ABSTRACT

Context: Danggui Buxue Tang (DBT), one of the popular Danggui (DG) decoctions, has traditionally been used to nourish 'qi' (vital energy) and enrich 'blood' (body circulation). DBT may possess performance-enhancing effects.Objective: This work determines whether DBT can improve physical capacity and alter energy expenditure under exercise training.Materials and methods: Forty male Wistar rats were assigned to four groups: sedentary (SE), exercise training (ET), ET supplemented with 0.3 g/kg rat/d DG extract, and ET supplemented with 1.8 g/kg rat/d DBT extract. The supplementations were administered via oral gavage. During the 21-day treatment period, the exercised groups were subjected to a protocol of swimming training with a gradually increased load. Physical performance evaluation was assessed using the forelimb grip strength test and an exhaustive swimming test. Muscle glycogen contents and exercise-related biochemical parameters were analysed.Results: Both herbal supplementations remarkably increased the grip strength (DG by 49.7% and DBT by 85.7%) and prolonged the swimming time (DG by 48.4% and DBT by 72.7%) compared with SE. DBT spared a certain amount of glycogen in the muscle cells under exercise training. Regarding the regulation of fuel usage, DBT had a positive impact alongside ET on promoting aerobic glycolysis via significantly decreasing serum lactate by 31.6% and lactic dehydrogenase levels by 61.8%.Conclusions: This study found that DBT could be considered a promising sports ergogenic aid for athletic population or fitness enthusiasts. Future work focussing on isolating the bioactive components that truly provide the ergogenic effects would be of interest.


Subject(s)
Adaptation, Physiological/drug effects , Adaptation, Physiological/physiology , Dietary Supplements , Drugs, Chinese Herbal/pharmacology , Physical Functional Performance , Swimming/physiology , Animals , Drugs, Chinese Herbal/isolation & purification , Male , Plant Extracts/isolation & purification , Plant Extracts/pharmacology , Plant Roots , Rats , Rats, Wistar
13.
Int J Mol Sci ; 21(7)2020 Apr 04.
Article in English | MEDLINE | ID: mdl-32260319

ABSTRACT

Andrographolide (AG), a major diterpene lactone isolated from Andrographis paniculata (Burm. f.) Nees (Acanthaceae), possesses a wide spectrum of biological activities. However, its poor water solubility and low bioavailability limit its clinical application. Therefore, this study aimed to develop a solid dispersion (SD) formulation to increase the aqueous solubility and dissolution rate of AG. Different drug-polymer ratios were used to prepare various SDs. The optimized formulation was characterized for differential scanning calorimetry, Fourier transform infrared spectroscopy, and powder X-ray diffraction. The analysis indicated that the optimized SD enhanced AG solubility and dissolution rates by changing AG crystallinity to an amorphous state. The dissolution behaviors of the optimum SD composed of an AG-polyvinylpyrrolidone K30-Kolliphor EL ratio of 1:7:1 (w/w/w) resulted in the highest accumulated dissolution (approximately 80%). Pharmacokinetic studies revealed that Cmax/dose and the AUC/dose increased by 3.7-fold and 3.0-fold, respectively, compared with AG suspension. Furthermore, pretreatment using the optimized AG-SD significantly increased the swimming time to exhaustion by 1.7-fold and decreased the plasma ammonia level by 71.5%, compared with the vehicle group. In conclusion, the optimized AG-SD formulation appeared to effectively improve its dissolution rate and oral bioavailability. Moreover, the optimized AG-SD provides a promising treatment against physical fatigue.


Subject(s)
Diterpenes/administration & dosage , Drug Compounding/methods , Fatigue/drug therapy , Administration, Oral , Ammonia/blood , Animals , Biological Availability , Calorimetry, Differential Scanning , Disease Models, Animal , Diterpenes/pharmacokinetics , Fatigue/metabolism , Male , Rats , Suspensions , X-Ray Diffraction
14.
Nutrients ; 12(2)2020 Jan 21.
Article in English | MEDLINE | ID: mdl-31973198

ABSTRACT

Since 2017, higenamine has been added to the World Anti-Doping Agency (WADA) prohibited list as a ß2-agonist prohibited at all times for sportspersons. According to WADA's report, positive cases of higenamine misuse have been increasing yearly. However, higenamine occurs naturally in the Chinese herb lotus plumule-the green embryo of lotus (Nelumbo nucifera Gaertn) seeds-commercially available as concentrated powder on the Asian market. This study evaluated the major phytochemical components of lotus plumule products using an appropriate extraction method, followed by a human study in which the products were orally administered in multiple doses to investigate the risk of doping violations. Comparing various extraction methods revealed that optimized microwave-assisted extraction exhibited the highest extraction efficiency (extraction time, 26 min; power, 1046 W; and temperature, 120 °C). Subsequently, the alkaloids in lotus plumule products were quantitatively confirmed and compared. Human study participants (n = 6) consumed 0.8 g of lotus plumule (equivalent to 679.6 µg of higenamine) three times daily for three consecutive days. All participants' urinary higenamine concentrations exceeded the WADA reporting cut-off of 10.0 ng/mL. Accordingly, lotus plumule consumption may engender adverse analytical findings regarding higenamine. Athletes should avoid consuming lotus plumule-containing products during in- and out-of-competition periods.


Subject(s)
Alkaloids/analysis , Lotus/chemistry , Performance-Enhancing Substances/analysis , Phytochemicals/analysis , Plant Extracts/chemistry , Tetrahydroisoquinolines/analysis , Adult , Doping in Sports , Female , Humans , Male , Sports/standards
15.
Nutrients ; 11(11)2019 Oct 23.
Article in English | MEDLINE | ID: mdl-31652711

ABSTRACT

Ubiquinol (QH), a reduced form of coenzyme Q10, is a lipid antioxidant that is hydro-soluble and is commonly formulated in commercial supplements. Ubiquinol has been increasingly reported to exert antioxidant functions, in addition to its role in the cell energy-producing system of mitochondria and adenosine triphosphate (ATP) production. The aim of this study was to assess the potential beneficial effects of QH on anti-fatigue and ergogenic functions following physiological challenge. Forty 8-week-old male Institute of Cancer Research (ICR) mice were divided into four groups (n = 10 for each group): Group 1 (vehicle control or oil only); Group 2 (1X QH dose or 102.5 mg/kg); Group 3 (2X QH dose or 205 mg/kg); Group 4 (6X QH dose or 615 mg/kg). Anti-fatigue activity and exercise performance were studied using the forelimb grip strength experiment and exhaustive weight-loaded swimming time, and levels of serum lactate, ammonia, glucose, BUN (blood urea nitrogen), creatine kinase (CK), and free fatty acids (FFA) after an acute exercise challenge. The forelimb grip strength and exhaustive weight-loaded swimming time of the QH-6X group were significantly higher than those of the other groups. QH supplementation dose-dependently reduced serum lactate, ammonia, and CK levels and increased the FFA concentration after acute exercise. In addition, QH increased the liver and muscle glycogen content, an important energy source during exercise. Therefore, the results suggest that QH formulation is a safe dietary supplement for amelioration of fatigue and for promoting exercise performance.


Subject(s)
Dietary Supplements , Fatigue/prevention & control , Lipid Metabolism/drug effects , Physical Conditioning, Animal , Ubiquinone/analogs & derivatives , Animal Feed/analysis , Animals , Male , Mice , Mice, Inbred ICR , Muscle Strength/drug effects , Specific Pathogen-Free Organisms , Swimming , Ubiquinone/administration & dosage , Ubiquinone/pharmacology
16.
Nutrients ; 10(9)2018 Sep 18.
Article in English | MEDLINE | ID: mdl-30231484

ABSTRACT

This study was to investigate the protective and recovery effects of Danggui Buxue Tang (DBT) supplementation on exercise performance, hepcidin, iron status, and other related biochemical parameters after being challenged by a single bout of intense aerobic exercise. A total of 36 recreationally active males were pair-matched and randomly assigned to receive DBT or a placebo for 11 days, while using clusters based on their aerobic capacities. On the eighth day of the supplementation, the participants performed a 13-km run with maximal effort. Blood and urine samples were collected and analysed before treatment (Pre-Tre) and immediately after (Post-Ex), 24 h after (24-h Rec), and 72 h after (72-h Rec) the run. DBT supplementation dramatically shortened the finish times by 14.0% (12.3 min) when compared with that in the placebo group. Significant group × time effects were observed in serum hepcidin and iron levels. DBT supplementation repressed hepcidin levels at Post-Ex and 24-h Rec, thereby causing a significant increase in iron levels by 63.3% and 31.4% at Post-Ex and 72-h Rec, respectively. However, DBT supplementation had no significant anti-inflammatory or haemolysis-preventative effects. Short-term DBT supplementation shortened the running time and repressed exercise-induced hepcidin levels, thereby boosting iron levels and accelerating iron homeostasis during recovery.


Subject(s)
Dietary Supplements , Drugs, Chinese Herbal/administration & dosage , Hepcidins/blood , Physical Endurance/drug effects , Running , Adult , Biomarkers/blood , Down-Regulation , Humans , Iron/blood , Male , Recovery of Function , Taiwan , Time Factors , Treatment Outcome , Young Adult
17.
J Strength Cond Res ; 32(7): 2091-2095, 2018 Jul.
Article in English | MEDLINE | ID: mdl-29385002

ABSTRACT

Hsu, CC, Fong, TH, Chang, HM, Su, B, Chi, CP, Kan, NW, and Hsu, MC. Low second-to-fourth digit ratio has high explosive power? A prepubertal study. J Strength Cond Res 32(7): 2091-2095, 2018-A recent study reported that lower limb explosive power had no correlation with the index finger: ring finger (2D:4D) ratio. However, many studies hypothesized that a lower 2D:4D ratio (reflecting a relative higher testosterone exposure) predicts higher physical fitness. The aim of this study was to replicate the study of explosive power and the 2D:4D ratio in a sample of Taiwanese children. A total of 541 Taiwanese prepubertal children (257 girls and 284 boys aged 9-10 years) participated in this study. This study analyzed the relationship between the 2D:4D ratio and explosive power. Explosive power of the lower limbs was assessed using the standing long jump (SLJ) test. The lengths of the second and fourth fingers of the right hand were measured to calculate the 2D:4D ratio. The SLJ length was correlated with the 2D:4D ratios (r = -0.144, p = 0.015) in boys. After controlling for age and the body mass index, this correlation remained significant (r = -0.134, p = 0.024). For girls, 2D:4D ratios were not significantly correlated with SLJ scores. These results indicate that the SLJ distance was negatively correlated with the 2D:4D ratio in boys, but not in girls. These findings might suggest that prenatal testosterone exposure is negatively correlated with the explosive power in men, but not in women.


Subject(s)
Fingers/anatomy & histology , Lower Extremity/physiology , Physical Fitness/physiology , Child , Exercise Test/methods , Female , Humans , Male , Sex Characteristics , Taiwan
18.
Drug Test Anal ; 10(2): 350-356, 2018 Feb.
Article in English | MEDLINE | ID: mdl-28444836

ABSTRACT

Consumption of Ephedra alkaloids is prohibited in-competition by the World Anti-Doping Agency (WADA). In Taiwan, colds are often treated with Chinese herbal formulae containing Herba Ephedrae. We screened products sold in Taiwan and preliminarily assessed their relationships with WADA threshold violations. Fifty-six concentrated powder products, including 19 Chinese herbal formulae that contained Herba Ephedrae, were collected. The content of Ephedra alkaloids, namely ephedrine (E), methylephedrine (ME), norpseudoephedrine (NPE; cathine), pseudoephedrine (PE), and norephedrine (NE; phenylpropanolamine), was determined using a validated high-performance liquid chromatography method. The results revealed that the phenotypic indicators of the collected products, E/PE and E/total ratios, were 1.52-4.70 and 0.49-0.72, respectively, indicating that the Herba Ephedrae species in these products was probably E. sinica or E. equisetina, but not E. intermedia. The contents of E, ME, NPE, PE, and NE and the total alkaloid contents in the daily doses of the products were 0.45-34.97, 0.05-4.87, 0.04-3.61, 0.15-12.09, and 0.01-2.00 mg and 0.68-53.64 mg, respectively. The alkaloid contents followed a relatively consistent order (E > PE > ME ≈ NPE > NE), even for products from different manufacturers. We calculated that single doses of 50.0% and 3.6% of the products would result in the WADA thresholds of E and NPE being exceeded, respectively. Our data provide critical information for athletes and medical personnel, who should be wary of using complex Chinese herbal formulae in addition to over-the-counter products.


Subject(s)
Alkaloids/analysis , Drugs, Chinese Herbal/analysis , Ephedra/chemistry , Ephedrine/analogs & derivatives , Phenylpropanolamine/analysis , Pseudoephedrine/analysis , Alkaloids/chemistry , Chromatography, High Pressure Liquid , Doping in Sports , Ephedra/metabolism , Ephedra/toxicity , Ephedrine/analysis , Ephedrine/chemistry , Phenylpropanolamine/chemistry , Pseudoephedrine/chemistry , Taiwan
19.
J Exerc Sci Fit ; 16(2): 68-72, 2018 Aug.
Article in English | MEDLINE | ID: mdl-30662496

ABSTRACT

BACKGROUND/OBJECTIVE: Although the functional movement screen (FMS) has been widely applied for screening athletes, no previous study has used FMS scores to examine the association between distinct training seasons in high school baseball players. The aims of this study were to ascertain the functional movement screen (FMS) scores differences between the preparative period (PPP) and the competitive period (CPP) among high school baseball players and further determine whether FMS can be used as a tool to predict injuries during two major periods. METHODS: Fifty-five male high school baseball players (age 15.3 ±â€¯1.7 years; height 1.7 ±â€¯0.8 m; weight 64.6 ±â€¯11.5 kg) volunteered. Athletic injuries were reported through a self-report questionnaire. Players performed the FMS during the PPP and the CPP. A receiver operator characteristic (ROC) curve to calculate a cutoff total composite score ≤ 14 for the relationship between the FMS score and injury. Sensitivity, specificity, positive predictive value (PPV), negative predictive value (NPV) and an area under the curve (AUC) were calculated. RESULTS: FMS individual task score and total composite score were significantly lower in the CPP than in the PPP. However, a cutoff total composite score ≤14 for risk of injury, determined through a ROC curve, represented a low sensitivity of 58%, NPV of 66%, an AUC of 69%, specificity of 79%, and PPV of 71%. CONCLUSION: Although the low sensitivity and NPV and AUC scores indicated that the FMS does not accurately predict the risk of injury, the FMS individual task and total composite scores differed significantly between the PPP and CPP. Therefore, FMS could be used as a tool to identify physical deficiencies between distinct training seasons; however, utilizing the FMS as a screening tool for injury prediction in particular during the CPP in this population would not be recommended.

20.
Drug Test Anal ; 10(5): 860-864, 2018 May.
Article in English | MEDLINE | ID: mdl-29155490

ABSTRACT

Triamcinolone (T) is a glucocorticoid commonly used to relieve inflammation and treat arthritis, severe allergies, and asthma; however, it is banned by the World Anti-Doping Agency in competition for athletes when administered orally, intravenously, intramuscularly, or rectally. The minimum required performance limit (MRPL) for urinary T is 30 ng/mL. However, the data about the urinary excretion of T after oral administration is limited. We investigate the elimination profile and determine whether single-dose administration of T would cause a positive doping result. Twelve healthy volunteers received a single-dose of 4-mg T rally, and urine samples were collected for 24 hours. A validated liquid chromatography-tandem mass spectrometry method was used to determine urinary T levels. Non-compartmental modeling was used to estimate the pharmacokinetic parameters. All the urinary T concentrations were much higher than the MRPL. The peak urinary T concentration was 3211.4 ± 860.3 ng/mL (mean ± SD), time to peak concentration was 1.7 ± 0.9 hours, and the estimated elimination half-life was 4.4 ± 2.8 hours. About 27.76% of the consumed dose was eliminated via urine within 24 hours of intake. After a single-dose oral administration, urinary T concentrations still exceeded the MRPL after 24 hours. This information could be useful for limiting the misuse of T. Athletes should be aware when using T in competition and acquire approval for a therapeutic use exemption prior to use. Moreover, the elimination profile of orally administered T may be crucial information for distinguishing different dosage routes.


Subject(s)
Glucocorticoids/urine , Substance Abuse Detection/methods , Tandem Mass Spectrometry/methods , Triamcinolone/urine , Adult , Chromatography, Liquid/methods , Doping in Sports , Female , Glucocorticoids/administration & dosage , Humans , Limit of Detection , Male , Triamcinolone/administration & dosage , Young Adult
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