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Paul Erasto, Justin Omolo, Richard Sunguruma, Joan J Munissi, Victor Wiketye, Charles de Konig, Atallah F Ahmed
The Phytochemical investigation on MeOH extract on the bark of Aristolochia brasiliensis Mart. & Zucc (Aristolochiaceae) led to the isolation of major compound (1) as light brown grainy crystals. The compound was identified as 1-(4-hydroxybenzyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol (higenamine) on the basis of spectroscopic analysis, including 1D and 2D NMR spectroscopy. The compound was evaluated for its antimycobacterial activity against Mycobacterium indicus pranii (MIP), using Galleria mellonella larva as an in vivo infection model...
January 22, 2018: Natural Products and Bioprospecting
Krzysztof Grucza, Dorota Kwiatkowska, Katarzyna Kowalczyk, Mariola Wicka, Mirosław Szutowski, Piotr Chołbiński
Higenamine (Norcoclaurine) is a very popular substance in Chinese medicine and is present in many plants. The substance may be also found in supplements or nutrients, consumption of which may result in violation of anti-doping rules. Higenamine is prohibited in sport at all times and included in Class S3 (β-2-agonists) of the World Anti-Doping Agency (WADA) 2017 Prohibited List. The presence of higenamine in urine samples at concentrations greater than or equal to 10 ng/mL constitutes an adverse analytical finding (AAF)...
October 30, 2017: Drug Testing and Analysis
Eisuke Kato, Shunsuke Kimura, Jun Kawabata
β2-Adrenergic receptor (β2AR) agonists are employed as bronchodilators to treat pulmonary disorders, but are attracting attention for their modulation of glucose handling and energy expenditure. Higenamine is a tetrahydroisoquinoline present in several plant species and has β2AR agonist activity, but the involvement of each functional groups in β2AR agonist activity and its effectiveness compared with endogenous catecholamines (dopamine, epinephrine, and norepinephrine) has rarely been studied. Glucose uptake of muscle cells are known to be induced through β2AR activation...
December 15, 2017: Bioorganic & Medicinal Chemistry
Xiaoxia An, Chunli Long, Xiaomin Deng, Aihua Tang, Junyan Xie, Li Chen, Zhengang Wang
Diabetic gastroparesis (DGP) is a common complication of diabetes mellitus (DM). The numerous clinical symptoms of DGP and the great cost on the treatment of DGP seriously lowered the patients' life quality. However, the pathogenic mechanism of DGP is still elusive till now. In this study, we aimed to explore the effect of higenamine on the proliferation and apoptosis of gastric smooth muscle cells (SMCs) in DGP rat model. The DGP rat model was built by intraperitoneal injection of Streptozotocin (STZ) into male Sprague-Dawley (SD) rats...
November 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Eisuke Kato, Ryohei Iwata, Jun Kawabata
Higenamine is a tetrahydroisoquinoline present in several plants that has β-adrenergic receptor agonist activity. Study of the biosynthesis of higenamine has shown the participation of norcoclaurine synthase, which controls the stereochemistry to construct the (S)-isomer. However, when isolated from nature, higenamine is found as the racemate, or even the (R)-isomer. We recently reported the isolation of higenamine 4'-O-β-d-glucoside. Herein, its (R)- and (S)-isomers were synthesized and compared to precisely determine the stereochemistry of the isolate...
August 31, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Masato Okano, Mitsuhiko Sato, Shinji Kageyama
Higenamine is a key component of traditional Chinese herbal medicine. The fruit of Nandina domestica (which contains this component) is available as an ingredient in the so-called Nanten-nodo-ame throat lozenge found on the Japanese market, which is an over-the-counter pharmaceutical and is easy to purchase for Japanese athletes. However, higenamine is a non-selective β2-agonist, which is exemplified in the prohibited list of the World Anti-Doping Agency (WADA). Therefore, some have raised a concern regarding the potential cause of increased unintentional higenamine doping cases in the Asian region...
November 2017: Drug Testing and Analysis
Zhi Liang, Chang Xu, Lingna Dong, Yile Fu, Qiong Wu, Jie Zhao, Ling Ye, Zheng Cai, Menghua Liu, Bijun Xia, Lan Tang, Zhongqiu Liu
OBJECTIVES: Higenamine (HG), an active ingredient of Aconite root in Chinese herbal medicine, is mainly metabolized by UDP-glucuronosyltransferases (UGT). However, the systematic glucuronidation of HG in humans remains unclear. The purpose of this study was to investigate the glucuronidation of HG. METHODS: 12 recombinant human UGT (rUGT) isozymes were used to characterize the HG glucuronidation. Liver microsomes from male and female mice, rats, guinea pigs, dogs, and humans were used to determine the species and gender differences using liquid chromatography-mass spectrometry...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Nana Zhang, Zeqin Lian, Xueying Peng, Zijian Li, Haibo Zhu
ETHNOPHARMACOLOGICAL RELEVANCE: Aconitum has been used as local and traditional medicines in many asian regions for the treatment of various diseases such as collapse, syncope, painful joints, oedema, bronchial asthma et al. Higenamine, a plant-based alkaloid, was initially isolated from Aconitum and identified as the active cardiotonic component of Aconitum. It has been tested as a candidate of pharmacologic stress agent in the detection of coronary artery diseases (CADs) and now researchers have just accomplished the phase III clinical studies successfully in China...
January 20, 2017: Journal of Ethnopharmacology
Wenjiang Duan, Jianmin Chen, Yu Wu, Yong Zhang, Yuansheng Xu
Existing in Ranunculaceae Aconitum and tomato, with the chemical name 1-phydroxybenzyl-1,2,3,4-tetrahy-droisoquinoline, higenamine is widely distributed in China. Higenamine's anti-inflammatory, antioxidant and anti-apoptotic effects have been identified in previous studies. The present study attempted to determine the protective effect of higenamine against collagen-induced arthritis through heme oxygenase-1 (HO-1) and PI3K/Akt/Nrf-2 signaling pathways. A type II collagen (CII)-induced arthritis (CIA) model was established and clinical arthritis scores were used to appraise the curative effect of higenamine...
November 2016: Experimental and Therapeutic Medicine
Louise Deldicque, Marc Francaux
PURPOSE OF REVIEW: The purpose of this article is to collect the most recent data regarding the safety of well-known or emerging dietary supplements used by athletes. RECENT FINDINGS: From January 2014 to April 2016, about 30 articles have been published in the field. New data show that 90% of sports supplements contain trace of estrogenic endocrine disruptors, with 25% of them having a higher estrogenic activity than acceptable. About 50% of the supplements are contaminated by melamine, a source of nonprotein nitrogen...
November 2016: Current Opinion in Clinical Nutrition and Metabolic Care
Si Chen, Hailong Jiang, Yan Cao, Yun Wang, Ziheng Hu, Zhenyu Zhu, Yifeng Chai
Identifying the molecular targets for the beneficial effects of active small-molecule compounds simultaneously is an important and currently unmet challenge. In this study, we firstly proposed network analysis by integrating data from network pharmacology and metabolomics to identify targets of active components in sini decoction (SND) simultaneously against heart failure. To begin with, 48 potential active components in SND against heart failure were predicted by serum pharmacochemistry, text mining and similarity match...
April 20, 2016: Scientific Reports
Mei-ping Wu, Yi-shuai Zhang, Qian-mei Zhou, Jian Xiong, Yao-rong Dong, Chen Yan
Cardiomyocyte apoptosis contributes to ischemic cardiac injury and the development of heart failure. Higenamine is a key component of the Chinese herb aconite root that has been prescribed for treating symptoms of heart failure for thousands of years in the oriental Asian countries. It has been shown that higenamine has anti-apoptotic effects in a few cell types including cardiomyocytes. However, the pharmacological target and molecular mechanism of higenamine in the heart are still not fully illustrated. Herein, we report that higenamine protected myocyte apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR)...
February 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Yitong Liu, Michael F Santillo
A number of dietary supplements used for weight loss and athletic performance enhancement have been recently shown to contain a variety of stimulants, for which there is a lack of pharmacological and toxicological information. One concern for these emerging compounds is their potential to inhibit metabolic enzymes in the liver such as cytochromes P450 (CYP), which can lead to unexpected interactions among dietary supplements, drugs, and other xenobiotics. In this study, inhibition of human recombinant CYP2D6 and CYP3A4 by 27 amine stimulants associated with dietary supplements and their analogs was evaluated by luminescence assays...
March 2016: Drug Testing and Analysis
Jonathan Jeter, Kent J DeZee, Laura Kennedy
Rhabdomyolysis is a painful and potentially life-threatening injury in which muscle breaks down in response to an insult. In this case report, we describe the clinical course of a 22-year-old man who developed paraspinal muscle rhabdomyolysis and possible compartment syndrome in association with strenuous activity and the ingestion of an exercise supplement containing the stimulant higenamine. Although he did not experience any renal damage, he did experience a high level of pain acutely and for the next 4 months...
July 2015: Military Medicine
Eisuke Kato, Yosuke Inagaki, Jun Kawabata
Hypoglycemic effect is an efficient means to modulate elevated blood glucose levels in patients with diabetes. We found that the extract of lotus plumule (the germ of Nelumbo nucifera Gaertn. seed) showed potent glucose uptake enhancement activity against L6 myotubes, which results in a hypoglycemic effect. This activity was further investigated, and an active constituent was identified as a single bioactive compound, higenamine 4'-O-β-d-glucoside. Mechanistic studies employing phosphatidylinositol 3-kinase (PI3K) inhibitor, AMP-activated protein kinase (AMPK) inhibitor, or adrenergic receptor antagonist showed that the compound induced its activity through β2-adrenergic receptor...
July 1, 2015: Bioorganic & Medicinal Chemistry
Huamin Wei, Hongjin Wu, Wen Yu, Xu Yan, Xiaoyu Zhang
ETHNOPHARMACOLOGICAL RELEVANCE: Shenfu decoction (SFD) is a water extract of the dried root or root stalk of Panax ginseng C. A. Mey (Asian ginseng) and the lateral root of Aconitum carmichaeli Debx (prepared by Fuzi, Heishunpian in Chinese). It has been used to treat heart failure for over a thousand years. The main active components of SFD, ginsenosides and higenamine, enhance heart contractility, increase the coronary blood supply, improve ischemic myocardial metabolism, scavenge free radicals and protect myocardial ultrastructure...
July 1, 2015: Journal of Ethnopharmacology
Chao Liu, Chenyu Zhu, Guangsheng Wang, Rui Xu, Yaoming Zhu
INTRODUCTION: Intestinal ischemia and reperfusion (IR) syndrome is a life-threatening dilemma caused by diverse events. Higenamine (HG), an active ingredient of Aconiti Lateralis Radix Praeparata, has been traditionally used as a heart stimulant and anti-inflammatory agent in oriental countries. But the function of HG on intestine IR injury has never been investigated. MATERIALS AND METHODS: Mice underwent a 2 cm midline laparotomy, and the superior mesenteric artery (SMA) was obstructed by micro-vascular clamp to induce intestinal ischemia...
June 2015: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
Richard Calvert, Sanah Vohra, Martine Ferguson, Paddy Wiesenfeld
Some dietary supplements may contain cardiac stimulants and potential cardiotoxins. In vitro studies may identify ingredients of concern. A beating human cardiomyocyte cell line was used to evaluate cellular effects following phenylethylamine (PEA), higenamine, ephedrine or caffeine treatment. PEA and higenamine exposure levels simulated published blood levels in humans or animals after intravenous administration. Ephedrine and caffeine levels approximated published blood levels following human oral intake...
April 2015: Food and Chemical Toxicology
R J Bloomer, J M Schriefer, T A Gunnels
OBJECTIVE: Higenamine, an herbal agent also known as norcoclaurine, is thought to stimulate β-androgenic receptors and possess lipolytic activity. It is currently making its way into the dietary supplement market. To our knowledge, no studies have been conducted to determine the safety profile of oral higenamine when used alone and in conjunction with other commonly used lipolytic agents. METHODS: Forty-eight men were assigned to ingest either a placebo, higenamine, caffeine, or higenamine + caffeine + yohimbe bark extract daily for a period of 8 weeks...
October 2015: Human & Experimental Toxicology
Won Sup Lee, Jeong Won Yun, Arulkumar Nagappan, Jing Nan Lu, Min Jeong Kim, Jeong-Hee Lee, Dong Hoon Kim, Yung Hyun Choi, Hye Jung Kim, Ki Churl Chang, Jin-Myung Jung
CKD-712, a newly synthesized tetrahydroisoquinoline (THI) and an enantiomer (S form) of YS 49 (a derivative of higenamine) has been reported to suppress nuclear factor-κB (NF-κB) activity in normal cells. In the present study, we investigated the anticancer effects of THI at a low concentration where CKD-712 did not induce cell death in normal cells. At the range of concentrations used, CKD-712 induced cell growth arrest, and inhibited the invasion and motility of A549 cells as determined by cell cycle analysis, a Matrigel-coated chamber assay, and a wound-healing assay, respectively...
March 2015: Oncology Reports
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