AIM: This study aimed to investigate the phytochemical composition of Psychotria montana extract (PME) and evaluate its inhibitory effects on MCF7 breast cancer cells. METHODS: The chemical composition of PME was analyzed using UPLC-QToF-MS. The effects of PME on cell proliferation were evaluated using the MTT assay. Flow cytometry was used for cell cycle and apoptosis analysis. The effects of PME on the transcription of cell cycle control genes were assessed using real-time PCR. RESULTS: UPLC-QToF-MS analysis revealed major compounds of PME, including terpenoids and flavonoids, with the potential to inhibit proliferation, migration, and induce apoptosis in MCF7 cancer cells. PME effectively suppressed MCF7 cell proliferation under 2D culture, with a low IC50 value of 34.7 μg/ml. PME also hindered cell migration (p < 0.01) and reduced spheroid number (p < 0.001) and size (p < 0.001) in serum-free 3D culture. Apoptosis analysis via nuclear staining with DAPI and flow cytometry revealed an increase in the number of apoptotic cells after PME treatment (p < 0.001). Additionally, the PME induced cell cycle arrest at the G0/G1 phase (p < 0.05). PME altered the expression of cell cycle control genes (cyclins and CDKs) as well as cancer suppressor genes including p16, p27, and p53 at the transcriptional level (mRNA). The results of molecular docking suggest that the compounds present in PME exhibit a high binding affinity for CDK3, CDK4, CDK6, and CDK8 proteins, which are essential regulators of the cell cycle. CONCLUSION: Psychotria montana has the potential to inhibit cancer cells by inducing apoptosis and halting the cell cycle of MCF7 breast cancer cells.
- MeSH
- Apoptosis * drug effects MeSH
- Cell Cycle drug effects MeSH
- Antineoplastic Agents, Phytogenic pharmacology chemistry MeSH
- Humans MeSH
- MCF-7 Cells MeSH
- Breast Neoplasms * drug therapy pathology genetics metabolism MeSH
- Computer Simulation MeSH
- Cell Movement drug effects MeSH
- Cell Proliferation * drug effects MeSH
- Psychotria * chemistry MeSH
- Plant Extracts * pharmacology chemistry MeSH
- Molecular Docking Simulation MeSH
- Check Tag
- Humans MeSH
- Female MeSH
- Publication type
- Journal Article MeSH
Hlavním cílem tohoto textu je představit nové psychoaktivní látky zahrnující širokou a různorodou skupinu látek, většinou syntetického původu, zejména se stimulačními, sedativními a halucinogenními účinky. Tyto látky byly vyvinuty nebo znovu uvedeny na trh, aby na jedné straně nahradily tradiční návykové látky, jejichž výroba a zejména distribuce často cílí na obcházení legislativy. Na druhé straně se jedná o velký obchodní potenciál pro výrobce a distributory těchto látek. V textu jsou představeny různé podskupiny těchto látek, jako jsou syntetické kanabinoidy a opioidy, a jejich závažná zdravotní rizika, včetně neurotoxických a kardiovaskulárních komplikací. Dále se zaměřuje na specifické skupiny uživatelů, které tyto látky preferují, na jejich důvody pro užívání, včetně snahy vyhnout se detekci drog nebo zlepšit sexuální prožitek. Zvláštní pozornost je věnována i novým psychedelickým látkám a kratomu, včetně jejich farmakologických vlastností a zdravotních rizik. Článek zdůrazňuje složitost fenoménu nových psychoaktivních látek a nutnost zvýšené pozornosti zdravotnických pracovníků při identifikaci a léčbě intoxikací těmito látkami.
The main objective of this text is to introduce new psychoactive substances, which encompass a broad and diverse group of substances, mostly of synthetic origin, with primarily stimulating, sedative, and hallucinogenic effects. These substances were developed or reintroduced to the market to replace traditional addictive substances, and their production often aims to circumvent legislation. The text discusses various subgroups of these substances, such as synthetic cannabinoids and opioids, and their serious health risks, including neurotoxic and cardiovascular complications. It also focuses on specific user groups who prefer these substances and their reasons for use, including attempts to avoid drug detection or enhance sexual experiences. Special attention is also given to new psychedelic substances and kratom, including their pharmacological properties and health risks. The article emphasizes the complexity of the phenomenon of new psychoactive substances and the need for increased attention from healthcare professionals in identifying and treating intoxications with these substances.
- MeSH
- Dimethoxyphenylethylamine administration & dosage pharmacology MeSH
- Cannabinoids pharmacology adverse effects MeSH
- Ketamine administration & dosage pharmacology adverse effects MeSH
- Humans MeSH
- Mitragyna chemistry adverse effects MeSH
- Analgesics, Opioid adverse effects MeSH
- Psychotropic Drugs * pharmacology classification adverse effects MeSH
- Wakefulness-Promoting Agents pharmacology adverse effects MeSH
- Drug Users MeSH
- Check Tag
- Humans MeSH
- Publication type
- Research Support, Non-U.S. Gov't MeSH
- Review MeSH
Kratom představuje na našem území novou rostlinnou drogu, jejíž užívání se masivně rozšířilo v populaci mladých dospělých. Kratom má unikátní farmakologický profil s převažujícím agonistickým působením na opioidní a α-2 adrenergní receptory. Zatímco jsou rizika akutní intoxikace kratomem relativně nízká, tak jsou rizika chronického užívání a rozvoje závislosti jsou podceňovaná. Článek shrnuje základní toxikologická a epidemiologická data o kratomu.
The abuse of herbal drug kratom has widely spread during past few years among the population of young adults. Kratom has a unique pharmacological profile and its alkaloids act predominantly as opioid and α-2 adrenergic agonists. While the risks of acute kratom intoxication are relatively low, the risks of chronic use and drug dependence development are underestimated. The article summarizes basic toxicological and epidemiological data on kratom.
- MeSH
- Alkaloids toxicity MeSH
- Humans MeSH
- Mitragyna * MeSH
- Adolescent MeSH
- Poisoning MeSH
- Substance-Related Disorders * MeSH
- Drug Users MeSH
- Check Tag
- Humans MeSH
- Adolescent MeSH
- Publication type
- Review MeSH
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- Keywords
- Kratom,
- MeSH
- Indole Alkaloids * agonists antagonists & inhibitors pharmacology therapeutic use MeSH
- Humans MeSH
- Mitragyna * anatomy & histology chemistry toxicity MeSH
- Substance-Related Disorders classification MeSH
- Receptors, Opioid drug effects MeSH
- Check Tag
- Humans MeSH
- Geographicals
- Czech Republic MeSH
- MeSH
- Addiction Medicine organization & administration statistics & numerical data trends MeSH
- Child MeSH
- Health Services Accessibility MeSH
- Cannabinoids adverse effects MeSH
- Central Nervous System Agents adverse effects MeSH
- Humans MeSH
- Mitragyna adverse effects MeSH
- Suicide, Attempted statistics & numerical data MeSH
- Substance-Related Disorders * diagnosis etiology psychology therapy MeSH
- Drug Overdose * diagnosis etiology psychology therapy MeSH
- Toxicology organization & administration statistics & numerical data MeSH
- Check Tag
- Child MeSH
- Humans MeSH
- Publication type
- Newspaper Article MeSH
- MeSH
- Child MeSH
- Cannabinoids * adverse effects MeSH
- Central Nervous System Agents adverse effects MeSH
- Humans MeSH
- Mitragyna * adverse effects MeSH
- Alcohol Drinking adverse effects MeSH
- Child Behavior Disorders etiology MeSH
- Check Tag
- Child MeSH
- Humans MeSH
- Publication type
- Newspaper Article MeSH
- Interview MeSH
- MeSH
- Drug and Narcotic Control MeSH
- Plants, Medicinal toxicity MeSH
- Humans MeSH
- Plant Leaves toxicity MeSH
- Mitragyna * toxicity MeSH
- Analgesics, Opioid toxicity MeSH
- Plant Poisoning MeSH
- Opioid-Related Disorders MeSH
- Risk Factors MeSH
- Drug Misuse * prevention & control trends MeSH
- Check Tag
- Humans MeSH
- Publication type
- Newspaper Article MeSH
- Geographicals
- Czech Republic MeSH
Termínem kratom jsou současně označovány stromy Mitragyna speciosa vyskytující se v jihovýchodní Asii a produkty získané z jeho listů. V sušině je obsažena řada biologicky účinných alkaloidů včetně více zastoupených látek mitragynin a 7-hydroxymitragynin působících na opioidní receptory. V tradiční asijské medicíně se kratom užívá například jako anestetikum, pro léčbu kašle, průjmu a pro zrychlení hojení ran. Nadměrné užívání kratomu může mít nežádoucí účinky a v některých zemích je k
Both the Mitragyna speciosa and products manufactured from its leaves are named kratom. The dry material of kratom contains a number of biologically active alkaloids, including two abundant substances mitragynine and 7-hydroxymitragynine that interact with opioid receptors. Kratom is used as an anesthetic, antitussive, antidiarrheal, and wound-healing drug. Adverse effects can follow the excessive intake of kratom, and it is also considered an addictive substance in some countries. This review describes kratom's origin, biological effects' mechanism, its therapeutic and adverse impact on an organism, and the legislative aspects of its sale are described here.
- MeSH
- Alkaloids administration & dosage pharmacology toxicity MeSH
- Central Nervous System Depressants administration & dosage pharmacology toxicity MeSH
- Mitragyna * anatomy & histology chemistry toxicity MeSH
- Narcotic Antagonists administration & dosage pharmacology toxicity MeSH
- Legislation, Drug MeSH
- Publication type
- Review MeSH
- MeSH
- Cetirizine administration & dosage pharmacology adverse effects MeSH
- Child MeSH
- Indole Alkaloids pharmacokinetics pharmacology MeSH
- Clarithromycin administration & dosage pharmacology adverse effects MeSH
- Drug Interactions * MeSH
- Humans MeSH
- Mitragyna adverse effects MeSH
- Neurobehavioral Manifestations drug effects MeSH
- Check Tag
- Child MeSH
- Humans MeSH
- Male MeSH
- Female MeSH
- Publication type
- Case Reports MeSH
