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The aim of this review is to present some of the recent publications on cannabidiol (CBD; 2), a major non-psychoactive constituent of Cannabis, and to give a general overview. Special emphasis is laid on biochemical and pharmacological advances, and on novel mechanisms recently put forward, to shed light on some of the pharmacological effects that can possibly be rationalized through these mechanisms. The plethora of positive pharmacological effects observed with CBD make this compound a highly attractive therapeutic entity.  相似文献   

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Cannabis is one of the first plants used as medicine, and the notion that it has potentially valuable therapeutic properties is a matter of current debate. The isolation of its main constituent, Delta9-tetrahydrocannabinol (THC), and the discovery of the endocannabinoid system (cannabinoid receptors CB1 and CB2 and their endogenous ligands) made possible studies concerning the pharmacological activity of cannabinoids. This paper reviews some of the most-important findings in the field of THC pharmacology. Clinical trials, anecdotal reports, and experiments employing animal models strongly support the idea that THC and its derivatives exhibit a wide variety of therapeutic applications. However, the psychotropic effects observed in laboratory animals and the adverse reactions reported during human trials, as well as the risk of tolerance development and potential dependence, limit the application of THC in therapy. Nowadays, researchers focus on other therapeutic strategies by which the endocannabinoid system might be modulated to clinical advantage (inhibitor or activator of endocannabinoid biosynthesis, cellular uptake, or metabolism). However, emerging evidence highlights the beneficial effects of the whole cannabis extract over those observed with single components, indicating cannabis-based medicines as new perspective to revisit the pharmacology of this plant.  相似文献   

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Over the past 50 years, a considerable research in medicinal chemistry has been carried out around the natural constituents of Cannabis sativa L. Following the identification of Delta9-tetrahydrocannabinol (Delta9-THC) in 1964, critical chemical modifications, e.g., variation of the side chain at C3 and the opening of the tricyclic scaffold, have led to the characterization of potent and cannabinoid receptor subtype-selective ligands. Those ligands that demonstrate high affinity for the cannabinoid receptors and good biological efficacy are still used as powerful pharmacological tools. This review summarizes past as well as recent developments in the structure-activity relationships of phytocannabinoids.  相似文献   

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Cannabis sativa, widely known as ‘Marijuana’ poses a dilemma for being a blend of both good and bad medicinal effects. The historical use of Cannabis for both medicinal and recreational purposes suggests it to be a friendly plant. However, whether the misuse of Cannabis and the cannabinoids derived from it can hamper normal body physiology is a focus of ongoing research. On the one hand, there is enough evidence to suggest that misuse of marijuana can cause deleterious effects on various organs like the lungs, immune system, cardiovascular system, etc. and also influence fertility and cause teratogenic effects. However, on the other hand, marijuana has been found to offer a magical cure for anorexia, chronic pain, muscle spasticity, nausea, and disturbed sleep. Indeed, most recently, the United Nations has given its verdict in favour of Cannabis declaring it as a non-dangerous narcotic. This review provides insights into the various health effects of Cannabis and its specialized metabolites and indicates how wise steps can be taken to promote good use and prevent misuse of the metabolites derived from this plant.  相似文献   

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Monoclonal antibody for delta‐9‐tetrahydrocannabiol (THC Ab), conjugated with protein A‐gold, was employed as a probe to detect THC localization in the gland and subjacent cells of chemically fixed bracts of Cannabis. THC was detected in the outer wall of the disc cells, fibrillar matrix, the surface feature of secretory vesicles, and sheath throughout development of the secretory cavity. The probe was absent from vesicles. Label was also present in anticlinal walls of disc cells and walls of dermal and mesophyll cells. Little or no THC Ab was present in disc cells and none were detected in control tissues. This distribution pattern of THC Ab was similar to that in tissues prepared by high pressure cryofixation‐cryosubstitution. Consistent association of THC with wall and wall‐derived materials suggests that cannnabinoids are synthesized outside the plasma membrane and bound to a wall component, where‐upon they are transported to the cavity with wall materials released from the disc cell wall during development of the secretory cavity  相似文献   

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Hemp (Cannabis sativa L.) belongs to the Cannabaceae family. It is very rich in chemical constituents, especially the cannabinoids which has not been reported in any other plant, and has broad pharmacological properties. Hemp as a multi-purpose crop is a good source of fibers, seed, fixed and volatile oil. It is known that the cannabinoid content of hemp is related to genetic factors, as well as plant's growth stages and environmental factors such as latitude, altitude, weather, particularly moisture availability and nutrient supply during the growing season. The present study was designed to produce hemp that contains allowable concentration of THC (<3 %) by comparing different varieties of hemp, different stages of plant growth, and different geographical locations where it was planted. To achieve this, seeds of two native populations from Iran (Fars and Yazd Provinces) and one foreign variety from France (Fedora17, as an industrial hemp cultivar) with its progenies (Fedora17-2) were cultivated in 3 research fields (Gilan, Golestan and Alborz provinces) in Iran. The following plant materials were extracted with methanol/chloroform and analyzed by HPLC: foliage in the vegetative stage, inflorescent in the flowering stage, inflorescent of seeds in the seeding stage and the mature seed. The THC concentration of Fedora17 (Fed17) in all three geographical locations was found to be under 0.03 % or even non-detectable. Same result was also observed in its progenies (Fed17-2), indicating stability of the trait in this cultivar. The THC concentration of the Yazd variety that was planted in Alborz and Gilan regions was less than 0.080 % in all growth stages. The female flowers planted in Golestan, showed a THC concentration of 1.029 % which was more than the allowed THC concentration of <3 %. The THC concentration in all growth stages of all of the different varieties planted varied from 0 to 1.392 %. The above results indicates that the type of cannabinoid produced depends on the difference in genetic prosperities of the different seed types as well as the growth stage in which the plant material was extracted. On the other hand, the climate and the region in which the seeds were planted had little influence on the THC concentration.  相似文献   

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Blood coagulation studies were conducted to determine the possible anti-/prothrombotic effect of an organic cannabis extract and the three major cannabinoids, THC, CBD and CBN. The in vitro effect of the cannabis extract on thrombin activity produced an IC50 value of 9.89 mg/ml, compared to THC at 1.79 mg/ml. It was also found that the extract, THC and CBN showed considerable inhibition of thrombin-induced clot formation in vitro with IC50 values of 600, 87 and 83 microg/ml for the extract, THC and CBN respectively. In an in vivo model used to determine clotting times of lean and obese rats treated with a cannabis extract, 50% clotting times were found to be 1.5 and 2 fold greater than their respective control groups, supporting the results obtained in the in vitro model. The study thus shows that Cannabis sativa and the cannabinoids, THC and CBN, display anticoagulant activity and may be useful in the treatment of diseases such as type 2 diabetes in which a hypercoagulable state exists.  相似文献   

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The acute side effects caused by cannabis use are mainly related to psyche and cognition, and to circulation. Euphoria, anxiety, changes in sensory perception, impairment of memory and psychomotor performance are common effects after a dose is taken that exceeds an individually variable threshold. Cannabis consumption may increase heart rate and change blood pressure, which may have serious consequences in people with heart disease. Effects of chronic use may be induction of psychosis and development of dependency to the drug. Effects on cognitive abilities seem to be reversible after abstinence, except possibly in very heavy users. Cannabis exposure in utero may have negative consequences on brain development with subtle impairment of cognitive abilities in later life. Consequences of cannabis smoking may be similar to those of tobacco smoking and should be avoided. Use by young people has more detrimental effects than use by adults. There appear to be promising therapeutic uses of cannabis for a range of indications. Use of moderate doses in a therapeutic context is usually not associated with severe side effects. Current prohibition on cannabis use may also have harmful side effects for the individual and the society, while having little influence on prevalence of use. Harm is greatest for seriously ill people who may benefit from a treatment with cannabis. This makes it difficult to justify criminal penalties against patients.  相似文献   

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Cannabinoid withdrawal produces a hypofunction of mesencephalic dopamine neurons that impinge upon medium spiny neurons (MSN) of the forebrain. After chronic treatment with two structurally different cannabinoid agonists, Δ9‐tetrahydrocannabinol and CP55 940 (CP) rats were withdrawn spontaneously and pharmacologically with the CB1 antagonist SR141716A (SR). In these two conditions, evaluation of tyrosine hydroxylase (TH)‐positive neurons revealed significant morphometrical reductions in the ventrotegmental area but not substantia nigra pars compacta of withdrawn rats. Similarly, confocal analysis of Golgi–Cox‐stained sections of the nucleus accumbens revealed a decrease in the shell, but not the core, of the spines' density of withdrawn rats. Administration of the CB1 antagonist SR to control rats, provoked structural abnormalities reminiscent of those observed in withdrawal conditions and support the regulatory role of cannabinoids in neurogenesis, axonal growth and synaptogenesis by acting as eu‐proliferative signals through the CB1 receptors. Further, these measures were incorporated into a realistic computational model that predicts a strong reduction in the excitability of morphologically altered MSN, yielding a significant reduction in action potential output. These pieces of evidence support the tenet that withdrawal from addictive compounds alters functioning of the mesolimbic system and provide direct morphological evidence for functional abnormalities associated with cannabinoid dependence at the level of dopaminergic neurons and their postsynaptic counterpart and are coherent with recent hypothesis underscoring a hypodopaminergic state as a distinctive feature of the ‘addicted brain’.  相似文献   

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Cannabis sativa is an interesting crop for several industrial uses, but the legislations in Europe and USA require a tight control of cannabinoid type and content for cultivation and subsidies release. Therefore, cannabinoid survey by gas chromatography of materials under selection is an important step in hemp breeding. In this paper, a number of Cannabis accessions were examined for their cannabinoid composition. Their absolute and relative content was examined, and results are discussed in the light of both the current genetic model for cannabinoid’s inheritance, and the legislation’s requirements. In addition, the effectiveness of two different types of markers associated to the locus determining the chemotype in Cannabis was evaluated and discussed, as possible tools in marker-assisted selection in hemp, but also for possible applications in the forensic and pharmaceutical fields.  相似文献   

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药用民族植物学及其研究进展   总被引:6,自引:0,他引:6  
药用民族植物学是研究传统医药或民间医药中植物药及其相关内容的一门由多学科组成的交叉学科。随着科学界对传统医药知识认识的不断加深 ,药用民族植物学已经受到了世界范围内的普遍关注。本文从传统医药的概念、引起科学界对传统医药知识产生兴趣的原因、民族传统药物的特点、药用民族植物学在发达国家和发展中国家的研究状况等方面对药用民族植物学的研究进展作了综合评述。  相似文献   

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紫堇属藏药的药用民族植物学研究   总被引:3,自引:0,他引:3  
紫堇属植物在藏药中具有较悠久的历史,而且随着历史的发展藏医所使用的该属药用植物的种类也在不断增加.本文采用药用民族植物学研究中的文献研究法,对文献中有关藏医用该属药用植物资源的利用情况进行了整理和分析.结果发现,藏医对该属植物的命名具有一定的规律,但目前还没有人对此进行系统研究;不同地区的藏医在使用该属药用植物资源中存在着一定程度的差异,这可能与不同地区该属的种类分布不同有关;该属藏药植物中藏医主要用于治疗止血、肝胆疾病和流感等疾病.与丰富的该属植物种类相比,并结合藏医的利用情况,从该属植物中寻找新的药用资源具有一定的潜力.  相似文献   

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Cannabidiol (CBD) is a major, biologically active, but psycho-inactive component of cannabis. In this cell culture-based report, CBD is shown to displace the agonist, [3H]8-OH-DPAT from the cloned human 5-HT1a receptor in a concentration-dependent manner. In contrast, the major psychoactive component of cannabis, tetrahydrocannabinol (THC) does not displace agonist from the receptor in the same micromolar concentration range. In signal transduction studies, CBD acts as an agonist at the human 5-HT1a receptor as demonstrated in two related approaches. First, CBD increases [35S]GTPγS binding in this G protein coupled receptor system, as does the known agonist serotonin. Second, in this GPCR system, that is negatively coupled to cAMP production, both CBD and 5-HT decrease cAMP concentration at similar apparent levels of receptor occupancy, based upon displacement data. Preliminary comparative data is also presented from the cloned rat 5-HT2a receptor suggesting that CBD is active, but less so, relative to the human 5-HT1a receptor, in binding analyses. Overall, these studies demonstrate that CBD is a modest affinity agonist at the human 5-HT1a receptor. Additional work is required to compare CBD’s potential at other serotonin receptors and in other species. Finally, the results indicate that cannabidiol may have interesting and useful potential beyond the realm of cannabinoid receptors.  相似文献   

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Plants synthesize a myriad of isoprenoid products that are required both for essential constitutive processes and for adaptive responses to the environment. Two independent pathways for the biosynthesis of isoprenoid precursors coexist within the plant cell: the cytosolic mevalonic acid (MVA) pathway and the plastidial methylerythritol phosphate (MEP) pathway. In this study, we investigated the inhibitory effect of the MVA pathway on isoprenoid biosynthesized by the MEP pathway in Cannabis sativa by treatment with mevinolin. The amount of chlorophyll a, b, and total showed to be significantly enhanced in treated plants in comparison with control plants. Also, mevinolin induced the accumulation of carotenoids and α-tocopherol in treated plants. Mevinolin caused a significant decrease in tetrahydrocannabinol (THC) content. This result show that the inhibition of the MVA pathway stimulates MEP pathway but none for all metabolites.  相似文献   

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The last quarter century has borne witness to great advances in both the detection and treatment of numerous cancers. Even so, malignancies of the central nervous system, especially high-grade astrocytomas, continue to thwart our best efforts toward effective chemotherapeutic strategies. With prognosis remaining bleak, the time for serious consideration of alternative therapies has arrived. Various preparations of the marijuana plant, Cannabis sativa, and related synthetic and endogenous compounds, may constitute just such an alternative. Cannabinoids, although much maligned historically for their psychotropic effects and clear abuse potential, have long been used medicinally and are now staging an impressive comeback, as recent studies have begun to explore their powerful anti-tumoral properties. In this study, we review in vitro and in vivo evidence supporting the use of cannabinoids for treatment of brain tumors. We further propose the continued intense investigation of cannabinoid efficacies as novel anti-cancer agents, especially in models recapitulating such properties within the unique environment of the brain.  相似文献   

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