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Anti-inflammatory effects of Mitragyna speciosa

Anti-inflammatory effects of Mitragyna speciosa

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July 4, 2017 By John Reed 1 Comment

Inflammation is a response to pathogens, chemical, or based onneurogenic loops. The methanolic solution of Mitragyna speciosa has anti-inflammatory properties. Intraperitoneal administration of an M. speciosa extract was able to inhibit the development of a carrageenaninduced paw oedema with a maximal inhibition during first 3 h after the challenge. The solution may exert its anti-inflammatory effect by inhibiting the synthesis, release and action of a number of hyperalgesic mediators. Thereby, it suppresses the early phase of acute inflammation. Arachidonic acid and its metabolites can be responsible for the inhibitory activity of the extract for a period of 4 h. Daily administration of the M. speciosa extract was also able to inhibit the growth of granuloma tissue as characterized by proliferation of modified macrophages, fibroblasts and highly vascularized and reddened mass tissue. (Zurina, 2013)

Kratom leaf and Kratom extracts have been shown to mildly inhibit the body’s ability to feel pain, as well as having mild, anti-depressant, and muscle relaxant effects. The key word here, is mild. For most humans, the painkilling effect of Kratom was on par with over the counter medications like aspirin or ibuprofen.

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Side effects of Maend Da

From a practical standpoint, taking five grams of Kratom instead of a few hundred milligrams of aspirin, is not going to make sense for most people. If it simply possessed anti-inflammatory and analgesic properties, nobody would be interested in Kratom.

Besides the aforementioned mild pain relief, it was noticed a slight opiate-style body high, and a very pronounced mood elevation. We would imagine that Kratom could successfully be used as an anti-depressant. It also has a stimulant effect that is unlike prescription opiates and generally the opposite of anti-depressants. At lower doses, I didn’t have the drowsy feeling that would normally accompany a traditional opiate-based painkiller.

From a practical standpoint, Kratom probably has very little potential as a “social” drug. Dumping a tablespoon of powder in your mouth isn’t really the same as passing a joint, and putting ten grams of powder into capsules can get time-consuming.

Some users have say that the pain relief allows them to train harder, heavier, and for longer. So anecdotally, we could say that a strong trend for the use of Kratom (as a painkiller) athletics…

With that in mind, Kratom has proven effective in alleviating withdrawal symptoms from central nervous system depressants like opiates and alcohol, and I would suspect that it has utility in treating addiction to painkillers also.

You could train using kratom, and you cannot notice any change in either soreness or recovery and it didn’t seem to have any effect on strength or stamina. This is partly why it’s gotten popular with athletes, because although it appears to work on the opioid receptors to dull pain, it doesn’t seem to negatively inhibit performance.

Despite its popularity, there are still some unanswered questions regarding its potential side-effects. Research in this area is lacking, although there strong evidence to suggest that case reports of negative effects have been greatly influenced by user polypharmacy (i.e. people damaging their bodies, or even dying with Kratom in their system, were almost always found with traces of something else in their system).

The spoil-sports over at the World Anti-Doping Agency have already placed Kratom on their monitoring list, and its use is banned in competition (its most logical use for performance enhancement). Naturally, it can be detected in urine, but a typical employer or sporting organization isn’t testing for it.

Unfortunately, the legal status of the herb is somewhat up in the air. The FDA has issued an import alert (meaning they’ll stop it at the border if anyone tries to bring it in), though it’s not illegal or banned per se.

On the state level, Tennessee, Vermont, New Jersey, and Wyoming have banned it’s sale, but that’s irrelevant if someone buys it online from another state. There is more restrictive legislation in the works, and a lobbying group has been started by Kratom sellers and enthusiasts to keep it (sort of) legal.

 

The various alkaloids that it contains and it complex interactions together promote these health benefits to its users. Some of the alkaloids which specifically help in giving the herb its anti-inflammatory properties are:

  • Epicatechin: Its antioxidant properties can promote overall health.  Its interactions with the lipid system can also improve longevity. Its physical performance benefits stem from its mitochondrial enhancement properties. Epicatechin promotes a lean body composition as well. Epicatechin can promote healthy visual and spatial memory by upregulating genes associated with learning.

It also has the following properties- Antioxidant, antihepatitic, antiaggregant, antiseptic, antidiuretic, anti-mutagenic, antiperoxidant, and antiviral.

  • Rhynchophylline: This anti-inflammatory alkaloid comprises of about 1% of the total alkaloid content of the leaf. It is rich in other properties like- Vasodilation, antiaggregant, antihypertensive, antipyretic, calcium channel blocker, anti-arrhythmic and anthelmintic.

 

References:

– http://www.phytochemicals.info/phytochemicals/epicatechin.php

– Zurina, H., Mustapha, M., “From Kratom to mitragynine and its derivatives: Physiological and behavioural effects related to use, abuse, and addiction”, Neuroscience and Biobehavioral Reviews 37,  pp. 138-151, 2013.

– https://www.ncbi.nlm.nih.gov/pubmed/19648761

Filed Under: Kratom (Mitragyna speciosa) Tagged With: kratom effects, Kratom Health, Mitragyna speciosa

Kratom Effects: the disputed ancient opioid plant with the debated effects

Kratom Effects: the disputed ancient opioid plant with the debated effects

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June 12, 2017 By John Reed Leave a Comment

Mitragyna speciosa is the scientific name of Kratom, a well-known tropical tree with a long history of traditional use in many parts of Africa, Southeast Asia, the Phillipines and New Guinea1,2. Kratom is a 4-16 meter high tree that belongs to the Rubiaceae or coffee family1,2 and is also known as Thom, Thang, Biak, Kakuam, Mambog, Ithang, and Ketum3,4 and there are different varieties of it with various stimulant, opioid or other effects5.  The most known varieties of Kratom that are sold on the internet are: Bali Kratom, Malaysian Kratom, red, green or white vein Thai kratom, Maeng Da Kratom, white-veined Borneo Kratom, New Guinea Kratom, Java Kratom, Sumatra red, the Rifat strain, the bumblebee strain, and red and green Riau6.

Historical uses of Kratom

Traditionally, in some Southeast Asian regions, the leaves of the tree were either chopped fresh or used dried and were used either for chewing or for tea preparation so as labor workers to combat fatigue and to become more productive7. Furthermore, it has long been used by people in Thailand or Malaya as a painkiller and opioid8. Nowadays, Kratom is actually consumed throughout the world for its stimulant effects and as an opioid substitute (in form of tea, chewed, smoked, in form of powder mixed with chocolate, milk or other ingredients or even ingested in the form of capsules).

Biochemical consistency of Kratom and registered effects

Several case studies have associated Kratom exposure with psychosis, seizures9, hepatotoxicity10, pulmonary and kidney injury11, cardiac12 or thyroid13 injury, other medical conditions, and deaths14. According to a recent study2 that analyzed one of the strongest varieties of Kratom, Maeng Da (Thai)15, different Kratom preparations may contain varying amounts of several phytochemicals, making their pharmacological and toxicological evaluation unique and difficult  (see Fig. 1).

Figure 1: An estimate of Thai kratom extract composition. The phytochemicals isolated from various parts of the tree include overall 40 structurally related alkaloids as well as several flavonoids, terpenoid saponins, polyphenols, and various glycosides2.

The debated effects of Kratom consumption

However, the clinical manifestations of Kratom effects are not well defined and the clinical studies are limited. Research data and many blogs and forums15-21 suggest that both positive and negative effects of Kratom exist.  The positive symptoms, according to some users include feeling relaxed, energetic, sociable, and euphoric. Other reports suggest that kratom increases sensory perception and users experience no pain22. On the other hand, the negative symptoms are mostly described as side effects or withdrawal symptoms that users mentioned. These effects are stomach ache, nausea and vomiting22, dry mouth, polyuria, anorexia, weight loss and frequent constipation7, tiredness and a loss of appetite23, and psychological symptoms such as hostility, aggression, anxiety, depressed mood, dysphoria, moodiness, annoyance, restlessness, visual alterations and unsteadiness24, low sexual drive, and irritability25, in addition to some other symptoms reported such as inability to work, muscle and bone pain, and jerky movements of the limbs7, and cold symptoms such as chills and sneeze. Some users also report symptoms like sweats, dizziness, vomiting, itching, mouth and throat numbness, and sedation24. One of the very characteristic cultural syndromes called the “rain panic,” which is of greatest concern for regular kratom users is the sense of frozen into the bone with muscle pain, joint aches, cough, sneezing, and trembling and was described by Saingam et al25.

More research on Kratom would reveal its benefits and its dangers

It is important to note that mortalities after Kratom consumption have been reported to occur in individuals with blood mitragynine concentrations between 0.45 and 1.0 μM26. Thus, it is difficult to draw conclusions about the safety of its consumption. For sure, more research about its’ pharmacokinetics and its’ side effects is needed and for the time being a careful intake would be wise.

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References

  1. Hassan Z, Muzaimi M, Navaratnam V, Yusoff NH, Suhaimi FW, Vadivelu R, Vicknasingam BK, Amato D, von Hörsten S, Ismail NI, Jayabalan N, Hazim AI, Mansor SM, Müller CP From Kratom to mitragynine and its derivatives: physiological and behavioural effects related to use, abuse, and addiction Neurosci Biobehav Rev. 2013 Feb; 37(2):138-51.
  2. Cinosi E, Martinotti G, Simonato P, et al. Following “the Roots” of Kratom (Mitragyna speciosa): The Evolution of an Enhancer from a Traditional Use to Increase Work and Productivity in Southeast Asia to a Recreational Psychoactive Drug in Western Countries.BioMed Research International. 2015
  3. Fluyau, Dimy, and Neelambika Revadigar. “Biochemical Benefits, Diagnosis, and Clinical Risks Evaluation of Kratom.”Frontiers in Psychiatry 8 (2017): 62. PMC. Web. 11 June 2017.
  4. Gruley B Is Kratom a Deadly Drug or a Life-Saving Medicine? BloomBerg December 2016 https://www.bloomberg.com/news/features/2017-06-08/no-one-has-ever-made-a-corruption-machine-like-this-one
  5. Warner ML, Kaufman NC, Grundmann O (2016). “The pharmacology and toxicology of kratom: from traditional herb to drug of abuse”. J. Legal Med. (Review). 130 (1): 127–38.
  6. Raffa R.B.Kratom and Other Mitragynines: The Chemistry and Pharmacology of Opioids from a Non-Opium Source. CRC Press Taylor & FrancisGroup; Boca Raton, FL, USA: 2014.
  7. Suwanlert S A study of kratom eaters in Thailand. Bull Narc. 1975 Jul-Sep; 27(3):21-7.
  8. Ahmad K, Aziz Z Mitragyna speciosa use in the northern states of Malaysia: a cross-sectional study. J Ethnopharmacol. 2012 May 7; 141(1):446-50.
  9. Nelsen JL, Lapoint J, Hodgman MJ, Aldous KM Seizure and coma following Kratom (Mitragynina speciosa Korth) exposure. J Med Toxicol. 2010 Dec; 6(4):424-6.
  10. Pantano, F., Tittarelli, R., Mannocchi, G., Zaami, S., Ricci, S., Giorgetti, R., … Marinelli, E. (2016). Hepatotoxicity Induced by “the 3Ks”: Kava, Kratom and Khat. International Journal of Molecular Sciences, 17(4)
  11. McIntyre IM, Trochta A, Stolberg S, Campman SC Mitragynine ‘Kratom’ related fatality: a case report with postmortem concentrations.J Anal Toxicol. 2015 Mar; 39(2):152-5.
  12. Lu J, Wei H, Wu J, Jamil MF, Tan ML, Adenan MI, Wong P, Shim W Evaluation of the cardiotoxicity of mitragynine and its analogues using human induced pluripotent stem cell-derived cardiomyocytes. PLoS One. 2014; 9(12):e115648.
  13. Sheleg SV, Collins GB A coincidence of addiction to “Kratom” and severe primary hypothyroidism. J Addict Med. 2011 Dec; 5(4):300-1.
  14. Karinen R, Fosen JT, Rogde S, Vindenes V An accidental poisoning with mitragynine. Forensic Sci Int. 2014 Dec; 245():e29-32.
  15. https://www.salviaextract.com/blog/green-malaysian-the-most-popular-kratom-strain/
  16. http://www.sagewisdom.org/kratomguide.html
  17. https://azarius.net/encyclopedia/15/Kratom_Mitragyna_speciosa/
  18. http://ensobotanicals.com/truth-maeng-da-kratom/
  19. http://kratomguides.com/maeng-da-kratom-benefits-side-effects-dosage/
  20. http://discoverkratom.org/maeng-da-review/
  21. https://www.kratomscience.com/strains-effects-and-dosage/
  22. Swogger MT, Hart E, Erowid F, Erowid E, Trabold N, Yee K, Parkhurst KA, Priddy BM, Walsh Z Experiences of Kratom Users: A Qualitative Analysis. J Psychoactive Drugs. 2015 Nov-Dec; 47(5):360-7.
  23. Kapp FG, Maurer HH, Auwärter V, Winkelmann M, Hermanns-Clausen M Intrahepatic cholestasis following abuse of powdered kratom (Mitragyna speciosa). J Med Toxicol. 2011 Sep; 7(3):227-31.
  24. Singh D, Narayanan S, Vicknasingam B Traditional and non-traditional uses of Mitragynine (Kratom): A survey of the literature. Brain Res Bull. 2016 Sep; 126(Pt 1):41-46.
  25. Saingam D, Assanangkornchai S, Geater AF, Balthip Q Pattern and consequences of krathom (Mitragyna speciosa Korth.) use among male villagers in southern Thailand: a qualitative study. Int J Drug Policy. 2013 Jul; 24(4):351-8.
  26. Saidin NA, Holmes E, Takayamab H, Gooderham NJ.The cellular toxicology of mitragynine, the dominant alkaloid of the narcotic-like herb, Mitragyna speciosa Korth. Toxicol Res (2015) 4:1173.

Filed Under: Kratom (Mitragyna speciosa) Tagged With: Kratom, kratom effects, Thai kratom

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