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Mitragyna speciosa

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https://www.readbyqxmd.com/read/29076424/physicochemical-characterization-of-mitragyna-speciosa-alkaloid-extract-and-mitragynine-using-in-vitro-high-throughput-assays
#1
Wai Mun Kong, Zamri Chik, Zahurin Mohamed, Mohammed A Alshawsh
Mitragynine, a major active alkaloid of Mitragyna speciosa, acts as an agonist on μ-opioid receptors, producing effects similar to morphine and other opioids. It has been traditionally utilized to alleviate opiate withdrawal symptoms. Besides consideration about potency and selectivity, a good drug must possess a suitable pharmacokinetic profile, with suitable absorption, distribution, metabolism, excretion and toxicity (ADME-Tox) profile, in order to have a high chance of success in clinical trials. The purity of mitragynine in a Mitragyna speciosa alkaloid extract (MSAE) was determined using Ultra-Fast Liquid Chromatography (UFLC)...
October 26, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/29071751/pxr-mediated-induction-of-cyp3a4-cyp1a2-and-p-gp-by-mitragyna-speciosa-and-its-alkaloids
#2
Vamshi K Manda, Bharathi Avula, Olivia R Dale, Zulfiqar Ali, Ikhlas A Khan, Larry A Walker, Shabana I Khan
Kratom (Mitragyna speciosa), a native herb of Southeast Asia, is widely known for its psychoactive properties. Recent increase in the use of kratom as a recreational drug has increased the risk of its interaction with conventional drugs if taken concomitantly. A few reports are available related to the effects of kratom on the activity of cytochrome P450 enzymes (CYPs), but there are no reports of its effects on pregnane X receptor (PXR), a transcription factor that regulates the expression of CYPs and P-glycoprotein (P-gp)...
October 26, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28966251/enhancement-of-endothelial-barrier-permeability-by-mitragynine
#3
Toshiyuki Matsunaga, Yoshifumi Morikawa, Kyoko Kamase, Misato Horinouchi, Yasuhide Sasajima, Koichi Suenami, Kiyohito Sato, Yuji Takekoshi, Satoshi Endo, Ossama El-Kabbani, Akira Ikari
Persistent inhalation of mitragynine (MG), a major alkaloid in the leaves of Mitragyna speciosa, causes various systemic adverse effects such as seizure, diarrhea and arthralgias, but its toxicity to endothelial cells and effects on barrier function of the cells are poorly understood. In this study, we compared toxicities of MG and mitraphylline, another constituent of the leaves, against human aortic endothelial (HAE), bronchial BEAS-2B, neuronal SK-N-SH, hepatic HepG2, kidney HEK293, gastric MKN45, colon DLD1, lung A549, breast MCF7 and prostate LNCaP cells, and found that MG, but not mitraphylline, shows higher toxicity to HAE cells compared to the other cells...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28950813/a-review-on-the-antinociceptive-effects-of-mitragyna-speciosa-and-its-derivatives-in-animal-model
#4
Kok-Yong Chin, Wun Fui Mark-Lee
Mitragyna speciosa is a tropical plant with narcotic effects. The antinociceptive effects of its crude extracts, bioactive compounds and structurally modified derivatives have been examined in rodent models. This review aims to summarize the evidence on the antinociceptive effects of M. speciosa and its derivatives and explore whether they can offer an alternative to morphine in pain management. Methanolic and alkaloid extracts of M. speciosa were shown to attenuate the nociceptive response in rodents. Mitragynine and 7-hydroxymitragynine offered better antinociceptive effects than crude extracts...
September 25, 2017: Current Drug Targets
https://www.readbyqxmd.com/read/28947930/mitragyna-speciosa-balancing-potential-medical-benefits-and-abuse
#5
EDITORIAL
Genevieve M Halpenny
Mitragyna speciosa, also known as kratom, has the potential meet the need for pain medications that lack the addictiveness and overdose risk of classical opioid analgesics, such as morphine. This need is urgent because opioid addiction and overdose deaths have risen throughout diverse segments of U.S. society. Some opioid addicts have found relief in kratom preparations. The use of kratom as an analgesic has been validated by historical accounts and contemporary pharmacological research. Although kratom is a promising source of analgesic candidates, it is a euphoriant with potential for both abuse and addiction...
September 14, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28830758/the-medicinal-chemistry-and-neuropharmacology-of-kratom-a-preliminary-discussion-of-a-promising-medicinal-plant-and-analysis-of-its-potential-for-abuse
#6
REVIEW
Andrew C Kruegel, Oliver Grundmann
The leaves of Mitragyna speciosa (commonly known as kratom), a tree endogenous to parts of Southeast Asia, have been used traditionally for their stimulant, mood-elevating, and analgesic effects and have recently attracted significant attention due to increased use in Western cultures as an alternative medicine. The plant's active alkaloid constituents, mitragynine and 7-hydroxymitragynine, have been shown to modulate opioid receptors, acting as partial agonists at mu-opioid receptors and competitive antagonists at kappa- and delta-opioid receptors...
August 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28687506/effects-of-alkaloid-rich-extract-from-mitragyna-speciosa-korth-havil-on-naloxone-precipitated-morphine-withdrawal-symptoms-and-local-field-potential-in-the-nucleus-accumbens-of-mice
#7
Dania Cheaha, Chayaporn Reakkamnuan, Jakkrit Nukitram, Somsmorn Chittrakarn, Pimpimol Phukpattaranont, Niwat Keawpradub, Ekkasit Kumarnsit
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa (Korth.) Havil. (M. speciosa) is among the most well-known plants used in ethnic practice of Southeast Asia. It has gained increasing attention as a plant with potential to substitute morphine in addiction treatment program. However, its action on the central nervous system is controversial. AIM OF THE STUDY: This study investigated the effects of M. speciosa alkaloid extract on naloxone-precipitated morphine withdrawal and neural signaling in the nucleus accumbens (NAc, brain reward center) of mice...
July 5, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28559179/opioid-receptors-mediate-the-acquisition-but-not-the-expression-of-mitragynine-induced-conditioned-place-preference-in-rats
#8
Nurul H M Yusoff, Sharif M Mansor, Christian P Müller, Zurina Hassan
Mitragynine is the main psychoactive ingredient of the herbal drug preparation Kratom (Ketum), derived from the plant Mitragyna speciosa. Kratom is a widely abused drug in Southeast Asian and has a psychostimulant profile at low-medium doses, while high doses have opioidergic effects. Mitragynine was shown to possess opiate receptor affinity. However, its role in the behavioural effects of mitragynine is unclear. Here we asked whether the reinforcing effects of mitragynine are mediated by opiate receptors using a conditioned place preference (CPP) paradigm in rats...
August 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28551311/evaluation-of-pharmacokinetics-and-blood-brain-barrier-permeability-of-mitragynine-using-in-vivo-microdialysis-technique
#9
Wai Mun Kong, Zahurin Mohamed, Mohammed A Alshawsh, Zamri Chik
A microdialysis system coupled with a sensitive ultra-fast liquid chromatography-mass spectrometry (UFLC-MS) method was developed for the pharmacokinetic analysis of mitragynine in rat blood and striatum. Mitragynine is an active alkaloid of Mitragyna speciosa and has been proposed to be used for opioid withdrawal therapy. In this study, chromatographic separation was performed in a gradient elution mode with 0.1% formic acid and acetonitrile on a Zorbax Eclipse C18 column. The mass spectrometric (MS) analysis was carried out in a positive electrospray mode and mitragynine ion (m/z 399...
September 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28544011/changing-trends-in-the-use-of-kratom-mitragyna-speciosa-in-southeast-asia
#10
Darshan Singh, Suresh Narayanan, Balasingam Vicknasingam, Ornella Corazza, Rita Santacroce, Andres Roman-Urrestarazu
OBJECTIVE: Kratom (Mitragyna speciosa. Korth) is an indigenous medicinal plant of Southeast Asia. This review paper aims to describe the trends of kratom use in Southeast Asia. DESIGN: A literature review search was conducted through ScienceDirect, Scopus, ProMed and Google Scholar. Twenty-five articles illustrating kratom use in humans in Southeast Asia were reviewed. RESULTS: Kratom has long been used by rural populations in Southeast Asia as a remedy for common ailments, to fight fatigue from hard manual work, as a drink during social interaction among men, and in village religious functions...
May 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28501425/the-effects-of-kratom-on-restraint-stress-induced-analgesia-and-its-mechanisms-of-action
#11
José Luis Vázquez López, Lorenz Schild, Thomas Günther, Stefan Schulz, Hartmud Neurath, Axel Becker
ETHNOPHARMACOLOGICAL RELEVANCE: Mitragyna speciosa and its extracts are called kratom (dried leaves, extract). They contain several alkaloids with an affinity for different opioid receptors. They are used in traditional medicine for the treatment of different diseases, as a substitute by opiate addicts, and to mitigate opioid withdrawal symptoms. Apart from their medical properties, they are used to enhance physical endurance and as a means of overcoming stress. PURPOSE: The aim of this study was to determine the mechanisms underlying the effects of kratom on restraint-stress-induced analgesia which occurs during or following exposure to a stressful or fearful stimulus...
June 9, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28484399/biochemical-benefits-diagnosis-and-clinical-risks-evaluation-of-kratom
#12
REVIEW
Dimy Fluyau, Neelambika Revadigar
BACKGROUND: Kratom (Mitragyna speciosa) is a tropical tree with a long history of traditional use in parts of Africa and Southeast Asia. Kratom is also known as Thom, Thang, and Biak. Its leaves and the teas brewed from them have long been used by people in that region to manage pain and opioid withdrawal and to stave off fatigue. Kratom is actually consumed throughout the world for its stimulant effects and as an opioid substitute (in form of tea, chewed, smoked, or ingested in capsules)...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28330725/a-botanical-phytochemical-and-ethnomedicinal-review-of-the-genus-mitragyna-korth-implications-for-products-sold-as-kratom
#13
REVIEW
Paula N Brown, Jensen A Lund, Susan J Murch
ETHNOPHARMACOLOGICAL RELEVANCE: The genus Mitragyna (Rubiacaeae) has been traditionally used in parts of Africa, Asia and Oceania. In recent years, there has been increased interest in species of Mitragyna with the introduction of products to western markets and regulatory uncertainty. AIM OF THE STUDY: This paper reviewed the traditional ethnomedicinal uses of leaves for species belonging to the genus Mitragyna with reference to the botany and known chemistry in order to highlight areas of interest for products currently being sold as kratom...
April 18, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28293192/indole-alkaloids-from-plants-as-potential-leads-for-antidepressant-drugs-a-mini-review
#14
Hazrulrizawati A Hamid, Aizi N M Ramli, Mashitah M Yusoff
Depression is the most common illness observed in the elderly, adults, and children. Antidepressants prescribed are usually synthetic drugs and these can sometimes cause a wide range of unpleasant side effects. Current research is focussed on natural products from plants as they are a rich source of potent new drug leads. Besides Hypericum perforatum (St. John's wort), the plants studied include Passiflora incarnata L. (passion flower), Mitragyna speciosa (kratom), Piper methysticum G. Forst (kava) and Valeriana officinalis L...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28284435/identification-of-cannabis-sativa-l-using-the-1-kbthca-synthase-fluorescence-in-situ-hybridization-probe
#15
Pattraporn Jeangkhwoa, Achirapa Bandhaya, Puangpaka Umpunjun, Ngarmnij Chuenboonngarm, Nathinee Panvisavas
This study reports a successful application of fluorescence in situ hybridization (FISH) technique in the identification of Cannabis sativa L. cells recovered from fresh and dried powdered plant materials. Two biotin-16-dUTP-labeled FISH probes were designed from the Cannabis-specific tetrahydrocannabinolic acid synthase (THCAS) gene and the ITS region of the 45S rRNA gene. Specificity of probe-target hybridization was tested against the target and 4 non-target plant species, i.e., Humulus lupulus, Mitragyna speciosa, Papaver sp...
March 2017: Science & Justice: Journal of the Forensic Science Society
https://www.readbyqxmd.com/read/28089300/mitragynine-concentrations-in-two-fatalities
#16
Olwen Domingo, Gabriele Roider, Andreas Stöver, Matthias Graw, Frank Musshoff, Hans Sachs, Wolfgang Bicker
Two cases of fatalities are reported of which the recreational use of Mitragyna speciosa ("kratom") could be confirmed. One of these cases presents with one of the highest postmortem mitragynine concentrations published to date. Our results show that even extremely high mitragynine blood concentrations following the consumption of kratom do not necessarily have to be the direct cause of death in such fatalities as a result of an acute overdose. The two cases are compared with regard to the differences in mitragynine concentrations detected and the role of mitragynine in the death of the subjects...
February 2017: Forensic Science International
https://www.readbyqxmd.com/read/27999544/mitragyna-speciosa-leaf-extract-exhibits-antipsychotic-like-effect-with-the-potential-to-alleviate-positive-and-negative-symptoms-of-psychosis-in-mice
#17
Kamini Vijeepallam, Vijayapandi Pandy, Thubasni Kunasegaran, Dharmani D Murugan, Murali Naidu
In this study, we investigated the antipsychotic-like effect of methanolic extract of Mitragyna speciosa leaf (MMS) using in vivo and ex vivo studies. In vivo studies comprised of apomorphine-induced climbing behavior, haloperidol-induced catalepsy, and ketamine-induced social withdrawal tests in mice whereas the ex vivo study was conducted utilizing isolated rat vas deferens preparation. Acute oral administration of MMS (50-500 mg/kg) showed an inverted bell-shaped dose-response in apomorphine-induced cage climbing behavior in mice...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27951469/-evaluation-of-ion-mobility-spectrometry-for-the-detection-of-mitragynine-in-kratom-products
#18
Nathan Fuenffinger, Melissa Ritchie, Ashley Ruth, Connie Gryniewicz-Ruzicka
An ion mobility spectrometry (IMS) method was developed for the rapid detection of mitragynine, the most abundant alkaloid in Mitragyna speciosa also known as kratom. The peak corresponding to the mitragynine protonated ion exhibited a reduced ion mobility of 0.95±0.00014cm(2)/(Vs), and the mitragynine limit of detection using IMS was 0.5ng. The IMS method was applied to the analysis of 15 commercial samples suspected of containing kratom. IMS results were compared to those obtained from liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis of the same samples...
February 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27893147/update-on-the-pharmacology-and-legal-status-of-kratom
#19
Walter C Prozialeck
Kratom (Mitragyna speciosa) is a plant indigenous to Southeast Asia. Its leaves and the teas brewed from them have long been used by people in that region to stave off fatigue and to manage pain and opioid withdrawal. In a comprehensive review published in 2012, Prozialeck et al presented evidence that kratom had been increasingly used for the self-management of opioid withdrawal and pain in the United States. At the time, kratom was classified as a legal herbal product by the US Drug Enforcement Administration...
December 1, 2016: Journal of the American Osteopathic Association
https://www.readbyqxmd.com/read/27768072/rapid-high-throughput-species-identification-of-botanical-material-using-direct-analysis-in-real-time-high-resolution-mass-spectrometry
#20
Ashton D Lesiak, Rabi A Musah
We demonstrate that direct analysis in real time-high resolution mass spectrometry can be used to produce mass spectral profiles of botanical material, and that these chemical fingerprints can be used for plant species identification. The mass spectral data can be acquired rapidly and in a high throughput manner without the need for sample extraction, derivatization or pH adjustment steps. The use of this technique bypasses challenges presented by more conventional techniques including lengthy chromatography analysis times and resource intensive methods...
October 2, 2016: Journal of Visualized Experiments: JoVE
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