Analgesic and antiinflammatory activity of constituents of Cannabis sativa L

Department of Pharmacognosy, School of Pharmacy, University of London, England.
Inflammation (Impact Factor: 2.21). 09/1988; 12(4):361-71. DOI: 10.1007/BF00915771
Source: PubMed


Two extracts of Cannabis sativa herb, one being cannabinoid-free (ethanol) and the other containing the cannabinoids (petroleum), were shown to inhibit PBQ-induced writhing in mouse when given orally and also to antagonize tetradecanoylphorbol acetate (TPA)-induced erythema of mouse skin when applied topically. With the exception of cannabinol (CBN) and delta 1-tetrahydrocannabinol (delta 1-THC), the cannabinoids and olivetol (their biosynthetic precursor) demonstrated activity in the PBQ test exhibiting their maximal effect at doses of about 100 micrograms/kg. delta 1-THC only became maximally effective in doses of 10 mg/kg. This higher dose corresponded to that which induced catalepsy and is indicative of a central action. CNB demonstrated little activity and even at doses in excess of 10 mg/kg could only produce a 40% inhibition of PBQ-induced writhing. Cannabinoid (CBD) was the most effective of the cannabinoids at doses of 100 micrograms/kg. Doses of cannabinoids that were effective in the analgesic test orally were used topically to antagonize TPA-induced erythema of skin. The fact that delta 1-THC and CBN were the least effective in this test suggests a structural relationship between analgesic activity and antiinflammatory activity among the cannabinoids related to their peripheral actions and separate from the central effects of delta 1-THC.

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    • "There are anecdotal reports of Cannabis relieving the sign and symptoms of various disease conditions such as asthma, convulsion, multiple sclerosis (MS), ocular pressure, acute post-operative and intractable pain, as well as stimulating appetite and antispasmodic (Russo, 2011; Ben, 2006; Hazekamp and Grotenhermen, 2010; Noyes et al., 1975; Wade et al., 2003; Grant, 2001; Tomida et al., 2006; Formukong et al., 1988; Obonga, 2006; Regelson et al., 1976; Di Tomaso et al., 1996). Other medicinal values such as antiemetic and use in palliative or terminal care have been reported for inhaled Cannabis and oral tetrahydrocannabinol (THC) (Matsuda **Corresponding author. "
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    ABSTRACT: As part of development efforts for a suitable dosage form, crude Cannabis resin was formulated into suppository dosage form using theobroma oil and the physical properties of the suppositories were evaluated. The following physical properties were evaluated: appearance (texture, presence or absence of entrapped air, contraction holes), liquefaction time, uniformity of weight and in-vitro release profile of the crude marijuana resin from the suppositories. The torpedo shaped suppositories were smooth in texture with absence of entrapped air and contraction holes. The suppositories had uniform greenish brown colour and low weight variation. The liquefaction time was also low. The 300 mg Cannabis crude in 4 % Tween 85 showed highest melting time (11.67 ± 057 min) while the incorporation of Tween 85 improved the release profile (0.0452-0.0650 %) in different batches. It is possible to formulate marijuana suppositories with satisfactory physical properties; however, release profile of marijuana from the suppository bases was generally low even though the addition of Tween 85 greatly enhanced drug release.
    Full-text · Article · Nov 2014 · African journal of pharmacy and pharmacology
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    • "During the last years, phytocannabinoid studies revealed various beneficial properties of THC. Compared to these findings, the precursor of THC, THCA, as well as the metabolite cannabinol (CBN) do not seem to have psychoactive properties, but analgesic, anti-inflammatory and neuroprotective effects are described (Ruhaak et al., 2001; Formukong et al., 1988). The second main compound of Cannabis, cannabidiol (CBD) has lower psychoactive properties and is therefore considered as a promising candidate for medical purposes. "
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    ABSTRACT: Phytocannabinoids are potentially candidates for neurodegenerative disease treatment. Nonetheless, the exact mode of action of major phytocannabinoids has to be elucidated, but both, receptor and non-receptor mediated effects are discussed. Focusing on the often presumed structure-affinity-relationship, Ki values of phytocannabinoids cannabidiol (CBD), cannabidivarin (CBDV), cannabichromene (CBC), cannabigerol (CBG), cannabinol (CBN), THC acid (THCA) and THC to human CB1 and CB2 receptors were detected by using competitive inhibition between radioligand [3H]CP-55,940 and the phytocannabinoids. Resulting Ki values to CB1 range from 23.5 μM (THCA) to 14711 μM (CBDV), whereas Ki values to CB2 range from 8.5 μM (THC) to 574.2 μM (CBDV). To study the relationship between binding affinity and effects on neurons, we investigated possible CB1 related cytotoxic properties in murine mesencephalic primary cell cultures and N18TG2 neuroblastoma cell line. Most of the phytocannabinoids did not affect the number of dopaminergic neurons in primary cultures, whereas propidium iodide and resazurin formation assays revealed cytotoxic properties of CBN, CBDV and CBG. However, THC showed positive effects on N18TG2 cell viability at a concentration of 10 μM, whereas also CBC and THCA displayed slightly positive activities. These findings are neither linked to structural characteristics nor to the receptor binding affinity therewith pointing to another mechanism than a receptor mediated one.
    Full-text · Article · Oct 2014 · Neurotoxicology and Teratology
    • "High temperatures enhance the formation and uptake of MDMA toxic metabolites that increase oxidative stress[45], causing nerve terminal damage[46,47]and leading to neuroinflammation, manifested by glial activation, and axonal degeneration[42,48]. Cannabis derivatives, in particular THC have been widely reported to exhibit hypothermic, anti-inflammatory and anti-oxidant properties[43,129]. Indeed, MDMA and THC show opposite pharmacological effects, and several studies propose that the combination of MDMA and THC counterbalances many drug effects. "
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    ABSTRACT: The amphetamine derivative 3, 4 Methylenedioxymethanphetamine (MDMA) is a powerful central nervous system stimulant that displays numerous pharmacological effects, including neurotoxicity. MDMA, or ecstasy, acts by inducing the release of different neurotransmitters depending on the animal species and, in particular, it produces the release of serotonin and dopamine. MDMA induces rewarding and reinforcing effects in rodents, primates and humans, and is currently consumed as an illicit psychostimulant among young people. One of the most reported side effects is the hyperthermic effect and the neurotoxicity on central serotonergic and dopaminergic neurons, depending on the species of animal.It seems that MDMA may also produce neurotoxic effects in humans. To date, the most consistent findings associated to MDMA consumption in humans relate to cognitive deficits in heavy users. MDMA when consumed as an illicit psychostimulant is commonly co-used with other abuse, being frequently associated with cannabinoids. The interaction between MDMA and cannabis effects is complex. Cannabis derivatives act on endocannabinoids systems. Thus, at cellular levels, cannabinoids acting through CB1 cannabinoid receptors display opposite effects to those induced by MDMA, and they have been reported to develop neuroprotective actions, including the blockage of MDMA induced neurotoxicity, in laboratory animals. However, cannabis use is a recognized risk factor in the presentation and development of neuropsychiatric disorders, and also contributes to the development of psychological problems and cognitive failures observed in MDMA users. This paper represents a brief overview of the pharmacological interaction between MDMA and cannabis derivatives acting in the endocannabinoid system. We have evaluated recent findings in the literature of the most representative pharmacological effects displayed by both types of drugs. We analyze both, the synergic and opposite effects produced by these two compounds and we have found a gap regarding the negative consequences of long-term human consumption of MDMA alone or in combination with cannabis.
    No preview · Article · Apr 2013 · Current pharmaceutical design
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