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Kevin F Elwood, Robert W Wong
PURPOSE: To describe a case of transient, partial, central retinal artery occlusion with paracentral acute middle maculopathy optical coherence tomography presentation in a young healthy patient after ingestion of the synephrine-containing supplement, Havok. METHODS: Retrospective case report with fundus photography, fluorescein angiography, and optical coherence tomography. RESULTS: A 20-year-old man presented with severe acute vision loss in the right eye...
March 8, 2018: Retinal Cases & Brief Reports
Jianping Zhao, Mei Wang, Bharathi Avula, Ikhlas A Khan
Phenethylamines (PEAs) are popular substances found in weight-loss and sports nutrition supplements. They are generally pharmacologically active and primarily affect the sympathetic nervous system. Many PEAs are synthetic chemicals and are on the prohibited list of the World Anti-Doping Agency. In this study, nuclear magnetic resonance (NMR) spectroscopy was applied to detect and identify the presence of PEAs in sports dietary supplements without the need for chromatographic separation or pre-knowledge on formulation...
January 26, 2018: Journal of Pharmaceutical and Biomedical Analysis
Cun-Yu Li, Yun Ma, Li-Cheng Liu, Qian Lu, Guo-Ping Peng
Based on the solution-diffusion effect and the charge effect theory in nanofiltration separation, the correlation between initial concentration and mass transfer coefficient was constructed to establish a mathematic model of synephrine in mass transfer process and verify its applicability. The experimental results showed that there was a linear relationship between operation pressure and membrane flux. Meanwhile, the membrane flux was gradually decayed with the increase of solute concentration. Besides, mass transfer coefficient and initial concentration of synephrine showed power function correlation with each other by solution-diffusion effect and the charge effect, and the regression coefficients were greater than 0...
December 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Yue Song, Tingting Chai, Shengting Lou, Yuechen Zhao, Xining Zhang, Shuming Yang, Yongzhong Qian, Jing Qiu
To detect and quantify synephrine in feed, an effective analytical method based on quick, easy, cheap, effective, rugged and safe solid-phase extraction coupled to ultra high performance liquid chromatography with tandem mass spectrometry was developed with isotopic internal standards. Pretreatment was performed using quick, easy, cheap, effective, rugged and safe solid-phase extraction with primary secondary amine (PSA) and C18 sorbent (C18) as sorbents in combination with Oasis MCX column clean-up to extract and purify feed samples...
January 10, 2018: Journal of Separation Science
Markus Zilker, Fritz Sörgel, Ulrike Holzgrabe
Pharmaceutical manufacturers have to study the stability of drug products before marketing according to ICH guideline Q1A(R2); data of those investigations aim to set expiry dates. The expiry date on the container of a remedy assures the physician and the patient a stability of the drug in its formulation i.e. within a specification of 95-105%. Only few studies show that shelf-lives of pharmaceutical products are often longer than expiration dates. The objective of the study presented here was determining the content of nine expired ampoules manufactured in the last century and identifying the impurity profile by means of HPLC-UV and HPLC-MS, respectively...
December 13, 2017: Journal of Pharmaceutical and Biomedical Analysis
N S Deshmukh, S J Stohs, C C Magar, A Kale, B Sowmya
Bitter orange ( Citrus aurantium L.) extracts are widely used in dietary supplements and bitter oranges are used in various juices and food products. p -Synephrine, the primary active constituent, comprises approximately 90% of total protoalkaloids. This study, performed per OECD 408 guidance, examined the 90-day subchronic safety/toxicity of an extract standardized to 50% p -synephrine at doses of 100, 300 and 1000 mg/kg/day to male and female rats. No adverse effects were observed with respect to any of the observed parameters of clinical signs, functional observations of sensory reactivity, grip strength and motor activity, ophthalmology, body weights, hematology, food consumption, urinalysis, organ weights, as well as gross and microscopic pathology at termination at any of the doses in either sex...
2017: Toxicology Reports
Mohd Shara, Sidney J Stohs, Mahmoud M Smadi
Extracts of bitter orange (BOE, Citrus aurantium L.) and its primary protoalkaloid p-synephrine are extensively consumed as dietary supplements. p-Synephrine is also present in foods and juices prepared from various Citrus species. The safety of p-synephrine has been questioned as a result of structural similarities with ephedrine. This study assessed the cardiovascular (stimulant) and hemodynamic effects of BOE (49 mg p-synephrine) daily given to 16 healthy subjects for 15 days in a placebo-controlled, cross-over, double-blinded study...
November 12, 2017: Phytotherapy Research: PTR
Leela Krishna Vatsavai, Eswar Kumar Kilari
BACKGROUND: Type 2 diabetes is frequently seen in patients suffering from obesity. p-Synephrine and gliclazide are widely used medicines for the treatment of obesity and diabetes, respectively. Based on the relationship between obesity and diabetes, the present study was undertaken to determine the potential for herb-drug interactions between p-synephrine and gliclazide. METHODS: Influence of p-synephrine on the activity of gliclazide was determined by conducting single and multiple dose interaction studies in animal models...
November 3, 2017: Journal of Ayurveda and Integrative Medicine
Nicholas A Ratamess, Jill A Bush, Sidney J Stohs, Nicole L Ellis, Ira T Vought, Elizabeth A O'Grady, Jeremy D Kuper, Saif B Hasan, Jie Kang, Avery D Faigenbaum
The purpose was to examine cardiovascular responses to supplementation with p-synephrine alone and in combination with caffeine during quiet sitting. Sixteen subjects were given (in double-blind manner) either 103 mg of p-synephrine (S), 233 mg of caffeine +104 mg of p-synephrine (LC + S), 240 mg of caffeine (LC), 337 mg of caffeine +46 mg of p-synephrine (HC + S), 325 mg of caffeine (HC), or a placebo. The subjects sat quietly for 3 hr while heart rate (HR) and blood pressure were measured. Only HC + S and HC significantly increased mean systolic blood pressure (SBP) during the second hour and tended to increase mean SBP during the third hour...
January 2018: Phytotherapy Research: PTR
Jorge Gutiérrez-Hellín, Juan Del Coso
The aim of this investigation was to determine the effects different doses of p-synephrine on maximal fat oxidation during exercise. Seventeen healthy subjects volunteered to participate in a double-blind and randomised experimental design composed of four identical experimental trials. On four trials separated by 72 h, participants ingested a placebo or 1, 2 or 3 mg/kg of p-synephrine. After resting for 60 min to allow substance absorption, participants performed an exercise test of increasing intensity on a cycle ergometer while gas exchange was measured continuously...
October 11, 2017: Phytotherapy Research: PTR
N S Deshmukh, S J Stohs, C C Magar, S B Kadam
The primary active constituent in bitter orange extract (BOE) is p-synephrine. This study assessed the safety of a BOE standardized to 50% p-synephrine following short-term exposure to rats and by the Ames Test. Following 5000 mg/kg of the extract orally to female rats all animals survived. Administration at 2000 mg/kg to female rats for four days yielded no signs of toxicity. Five male and five female rats were administered the BOE at 0, 250, 500, 1000 and 2000 mg/kg/day for 14 days. No significant effects were observed at any dose with respect to body weights, food intake, absolute and relative organ weights, hematology, clinical chemistry, and pathology...
September 28, 2017: Regulatory Toxicology and Pharmacology: RTP
Parham Taslimi, Hülya Akıncıoglu, İlhami Gülçin
In this paper, synephrine and phenylephrine compounds showed excellent inhibitory effects against human carbonic anhydrase (hCA) isoforms I and II, α-amylase, α-glycosidase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). Synephrine and phenylephrine had Ki values of 199.02 ± 16.01 and 65.01 ± 5.00 μM against hCA I and 336.02 ± 74.01 and 92.04  ±  18.03 μM against hCA II, respectively. On the other hand, their Ki values were found to be 169.10  ±  80.03 and 88.03  ±  5...
August 11, 2017: Journal of Biochemical and Molecular Toxicology
Sidney J Stohs
Citrus aurantium L. (bitter orange) extracts that contain p-synephrine as the primary protoalkaloid are widely used for weight loss/weight management, sports performance, appetite control, energy, and mental focus and cognition. Questions have been raised about the safety of p-synephrine because it has some structural similarity to ephedrine. This review focuses on current human, animal, in vitro, and mechanistic studies that address the safety, efficacy, and mechanisms of action of bitter orange extracts and p-synephrine...
October 2017: Phytotherapy Research: PTR
Chun-Yan Shen, Tian-Xing Wang, Xi-Mei Zhang, Jian-Guo Jiang
Citrus aurantium L. var. amara Engl. (CAVA) was traditionally used as an edible and medicinal material in China. Total flavonoids (CAVAF), alkaloids (CAVAA), polysaccharides (CAVAP), coumarins (CAVAC), and neroli (CAVAO) were extracted from CAVA. Hesperidin, naringin, and neohesperidin composed 83.94% of CAVAF, and synephrine represented 50.56% of CAVAA. On the basis of 1,1-diphenyl-2-picrylhydrazyl radical (DPPH(•)), 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt radical cation (ABTS(•) (+)), hydroxyl radical ((•)OH), ferric-reducing antioxidant power (FRAP), and reducing power assays, the antioxidant activities of five components were comprehensively and comparatively investigated...
August 2, 2017: Journal of Agricultural and Food Chemistry
Natalia Besil, Verónica Cesio, Horacio Heinzen, Amadeo R Fernandez-Alba
The matrix effects of ethyl acetate extracts from seven different citrus fruits on the determination of 80 pesticide residues using liquid chromatography coupled to high-resolution time-of-flight mass spectrometry (UHPLC-(ESI)-HR-TOF) at 4 GHz resolution mode were studied. Only 20% of the evaluated pesticides showed noticeable matrix effects (ME) due to coelution with natural products between tR = 3 and 11 min. Principal component analysis (PCA) of the detected coextractives grouped the mandarins and the orange varieties, but separated lemon, oranges, and mandarins from each other...
June 14, 2017: Journal of Agricultural and Food Chemistry
Matthias Bader, Tatjana Lang, Roman Lang, Thomas Hofmann
To validate the suitability of synephrine, known to be a highly abundant alkaloid in oranges, as a dietary biomarker for orange consumption, a highly sensitive and robust stable isotope dilution analysis (SIDA) as well as an ECHO method, using the analyte itself as a pseudointernal standard injected into the analysis run to provide an "echo peak" of the analyte, was developed to quantitate synephrine by liquid chromatography-tandem mass spectrometry (LC-MS/MS) in citrus juices and human urine before and after the ingestion of orange juice...
June 14, 2017: Journal of Agricultural and Food Chemistry
Nabil Killiny, Maria Filomena Valim, Shelley E Jones, Ahmad A Omar, Faraj Hijaz, Fred G Gmitter, Jude W Grosser
Huanglongbing (HLB) is currently considered the most destructive disease of citrus. Since its spread to the Americas, HLB has killed millions of trees and caused a sharp decline in production in many citrus growing regions. With the continuous spread of HLB disease in Florida and worldwide, there is an urgent need for the development of commercial citrus cultivars with a strong tolerance to HLB. Interestingly, field observations showed that some of the recently released mandarin hybrids such as 'Sugar Belle' were tolerant to HLB...
May 4, 2017: Plant Physiology and Biochemistry: PPB
Patrícia A S Tette, Letícia R Guidi, Esther M A F Bastos, Christian Fernandes, Maria Beatriz A Gloria
A LC-MS/MS method for synephrine as a biomarker for orange honey authenticity was developed and validated. The sample was extracted with 5% TCA and cleaned up with Florisil providing 83.7% recoveries. Ions transitions for quantification and identification were 168→135.0 and 168→107.0, respectively. The limits of detection and quantification were 0.66 and 1.0ng/g, respectively. Synephrine was detected in orange honey at levels from 79.2 to 432.2ng/g, but not in other monofloral honeys. It was also present in some wildflower honeys (9...
August 15, 2017: Food Chemistry
Nadiya Bakhiya, Rainer Ziegenhagen, Karen I Hirsch-Ernst, Birgit Dusemund, Klaus Richter, Katharina Schultrich, Sophie Pevny, Bernd Schäfer, Alfonso Lampen
Numerous food supplements contain phytochemical compounds as active ingredients. Although such supplements are often perceived by consumers as being risk-free, the safety of many of them is currently uncertain. The present review provides two examples for risk assessment for phytochemical ingredients that are used in certain supplements marketed for sportspeople-synephrine (extracted from fruits of Citrus aurantium) and hydroxycitric acid (HCA, isolated from fruits of Garcinia cambogia). Animal and human studies, as well as case reports, provide evidence for cardiovascular effects due to ingestion of high synephrine doses, especially in combination with caffeine and physical exertion...
June 2017: Molecular Nutrition & Food Research
Jong-Hee Kim, Yoonjung Park
Purpose: The purpose of this review is to discuss current views regarding the acute effects of phytochemicals, exercise, and exercise plus phytochemicals on fatty acid oxidation. Methods: Data acquired from human and animal studies were comprehensively assessed to determine the single and combined effects of phytochemicals and exercise on fatty acid oxidation. In addition, underlying mechanisms associated with those conditions that may contribute to the regulation of fat metabolism are discussed...
December 31, 2016: Journal of Exercise Nutrition & Biochemistry
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