Tag Archives: THC

Preparation and characterization of Δ9-tetrahydrocannabinol-loaded biodegradable polymeric microparticles and their antitumoral efficacy on cancer cell lines.

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“Cannabinoids present an interesting therapeutic potential as antiemetics, appetite stimulants in debilitating diseases (cancer, AIDS and multiple sclerosis), analgesics, and in the treatment of multiple sclerosis and cancer, among other conditions.

However, despite their high clinical potential, only few dosage forms are available to date. In this paper, the development of Δ9-tetrahydrocannabinol (THC) biodegradable microspheres as an alternative delivery system for cannabinoid parenteral administration is proposed. Tetrahydrocannabinol was encapsulated into biodegradable microspheres by the oil-in-water (o/w) emulsion solvent evaporation method. Several formulations were prepared using different drug:polymer ratios. The influence of antioxidant (α-tocopherol acetate) concentration on the release of THC from the microparticles was studied. Elevated process yield and entrapment efficiencies were achieved.The in vitro drug release studies showed that the encapsulated drug was released over a two week period.

 As THC has shown therapeutic potential as anticancer drug, the efficacy of the microspheres was tested on different cancer cell lines.

 Interestingly, the microspheres were able to inhibit cancer cell proliferation during the nine-day study period.

 All the above results suggest that the use of biodegradable microspheres would be a suitable alternative delivery system for THC administration.”

http://www.ncbi.nlm.nih.gov/pubmed/23773072

Acute Δ9-tetrahydrocannabinol blocks gastric hemorrhages induced by the nonsteroidal anti-inflammatory drug diclofenac sodium in mice.

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“Nonsteroidal anti-inflammatory drugs (NSAIDs), which are among the most widely used analgesics in the world, cause gastrointestinal inflammation that is potentially life-threatening.

Although inhibitors of endocannabinoid catabolic enzymes protect against gastropathy in fasted NSAID-treated mice, the gastroprotective effects of Δ9-tetrahydrocannabinol (THC), the primary psychoactive component of marijuana, have yet to be investigated…

 These data indicate that the phytocannabinoid Δ9-THC protects against diclofenac-induced gastric inflammatory tissue damage at doses insufficient to cause common cannabinoid side effects.”

http://www.ncbi.nlm.nih.gov/pubmed/23769745

Synthetic Compounds From Marijuana Appear to Fight HIV

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“Synthetic anti-inflammatory compounds derived from the active ingredient of marijuana appear to show potential as anti-HIV agents, Wired.co.uk reports. Publishing their findings in the Journal of Leukocyte Biology, researchers from Temple University School of Medicine’s Department of Pathology and Laboratory Medicine and Center for Substance Abuse Research (CSAR) studied synthetic derivations of THC, or tetrahydrocannabinol, a key chemical compound in marijuana, in cultures of HIV-infected cells.

Cannabinoids, which are the primary active compounds in marijuana, bind to proteins called CB2 receptors on the surface of macrophage immune cells. The CB2 site may play a role in reducing inflammation in the central nervous system, which is a major concern for people living with HIV, even those whose virus is fully suppressed thanks to antiretrovirals (ARVs). It is the CB1 receptors, mostly found in neurons in the brain, however, that cause marijuana’s psychoactive effects. So synthetic THC that has been developed to bind only to CB2 receptors should not make people stoned.

It is believed that macrophage cells, which are found throughout the body, are a major component of the HIV reservoir and are probably the first cells infected after sexual transmission of the virus.

Using a non-clinical cell model, the investigators treated HIV-infected macrophages with one of three different synthetic compounds that bind to CB2. By periodically measuring the activity of the enzyme reverse transcriptase, which HIV needs to replicate itself, the investigators concluded after a seven-day period that all three compounds fought HIV replication.

The findings suggest that these “CB2 agonists” could be a potential addition to ARV therapy, and also that the human immune system could be prompted to fight the virus using similar mechanisms.”

http://www.aidsmeds.com/articles/pot_CB2_1667_23905.shtml

Turned-Off Cannabinoid Receptor Turns on Colorectal Tumor Growth – MDAnderson

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“Researchers find CB1 suppresses tumors, a new potential path for treatment, prevention.”

 “New preclinical research shows that cannabinoid cell surface receptor CB1 plays a tumor-suppressing role in human colorectal cancer, scientists report in the Aug. 1 edition of the journal Cancer Research.

CB1 is well-established for relieving pain and nausea, elevating mood and stimulating appetite by serving as a docking station for the cannabinoid group of signaling molecules. It now may serve as a new path for cancer prevention or treatment.

“Potential application of cannabinoids as anti-tumor drugs is an exciting prospect, because cannabinoid agonists are being evaluated now to treat the side-effects of chemotherapy and radiation therapy,” DuBois said.

 “Turning CB1 back on and then treating with a cannabinoid agonist could provide a new approach to colorectal cancer treatment or prevention.”

Cannabinoids are a group of ligands that serve a variety of cell-signaling roles. Some are produced by the body internally (endocannabinoids). External cannabinoids include manmade versions and those present in plants, most famously the active ingredient in marijuana (THC).”

More:  http://www.mdanderson.org/newsroom/news-releases/2008/turned-off-cannabinoid-receptor-turns-on-colorectal-tumor-growth.html

Turned-off Cannabinoid Receptor Turns On Colorectal Tumor Growth – CB1 Suppresses Tumors, A New Potential Path For Treatment, Prevention

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“New preclinical research shows that cannabinoid cell surface receptor CB1 plays a tumor-suppressing role in human colorectal cancer, scientists report in the Aug. 1 edition of the journal Cancer Research.

CB1 is well-established for relieving pain and nausea, elevating mood and stimulating appetite by serving as a docking station for the cannabinoid group of signaling molecules. It now may serve as a new path for cancer prevention or treatment.

“Potential application of cannabinoids as anti-tumor drugs is an exciting prospect, because cannabinoid agonists are being evaluated now to treat the side-effects of chemotherapy and radiation therapy,” DuBois said. “Turning CB1 back on and then treating with a cannabinoid agonist could provide a new approach to colorectal cancer treatment or prevention.”

Cannabinoids are a group of ligands that serve a variety of cell-signaling roles. Some are produced by the body internally (endocannabinoids). External cannabinoids include manmade versions and those present in plants, most famously the active ingredient in marijuana (THC).”

More: http://www.medicalnewstoday.com/releases/117055.php

Cannabis Ingredient Can Help Cancer Patients Regain Their Appetites And Sense Of Taste

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“The active ingredient in cannabis can improve the appetites and sense of taste in cancer patients, according to a new study published online in the cancer journal, Annals of Oncology  today.

Loss of appetite is common among cancer patients, either because the cancer itself or its treatment affects the sense of taste and smell, leading to decreased enjoyment of food. This, in turn, can lead to weight loss, anorexia, a worse quality of life and decreased survival; therefore, finding effective ways of helping patients to maintain a good diet and consume enough calories is an important aspect of their treatment.

The majority of THC-treated patients (64%) had increased appetite, three patients (27%) showed no change, and one patient’s data was incomplete. No THC-treated patients showed a decrease in appetite. By contrast, the majority of patients receiving placebo had either decreased appetite (50%) or showed no change (20%).

Although there was no difference in the total number of calories consumed by both groups, the THC-treated patients tended to increase the proportion of protein that they ate, and 55% reported that savoury foods tasted better, whereas no patients in the placebo group reported an increased liking for these foods. (Cancer patients often find that meat smells and tastes unpleasant and, therefore, they eat less of it).

In addition, THC-treated patients reported better quality of sleep and relaxation than in the placebo group.”

More:  http://www.medicalnewstoday.com/articles/217062.php

Synthetic Agents Related To Active Ingredient In Marijuana Weaken HIV Infection – MedicalNewsToday

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“HIV, the virus that causes AIDS, is notorious for hiding within certain types of cells, where it reproduces at a slowed rate and eventually gives rise to chronic inflammation, despite drug therapy. But researchers at Temple University School of Medicine’s Department of Pathology and Laboratory Medicine and Center for Substance Abuse Research (CSAR) recently discovered that synthetic anti-inflammatory substances distantly related to the active ingredient of marijuana may be able to take the punch out of HIV while inside one of its major hideouts – immune cells known as macrophages.

The breakthrough comes at a crucial time in the HIV/AIDS pandemic…

To better understand the connection between inflammation and neurocognitive conditions linked to long-term exposure to HIV, Ramirez and colleagues looked specifically at the CB2 receptor, a protein located on the surface of macrophages. CB2 is a binding site for substances called cannabinoids, the primary active compounds of cannabis (marijuana), and it may play a role in blocking inflammation in the CNS. Unlike its counterpart, the CB1 receptor, which is found primarily on neurons in the brain, CB2 does not mediate the psychoactive effects for which cannabis is popularly known.

Ramirez explained that there has been much pharmacological interest in developing agents that selectively target CB2. Ideally, these compounds would help limit chronic inflammatory responses and would not bind to CB1.

The most promising compounds are those derived from THC (tetrahydrocannabinol), the main active substance in cannabis.”

More: http://www.medicalnewstoday.com/releases/259980.php

Synthetic derivatives of THC may weaken HIV-1 infection to enhance antiviral therapies – MedicalXpress

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“A new use for compounds related in composition to the active ingredient in marijuana may be on the horizon: a new research report published in the Journal of Leukocyte Biology shows that compounds that stimulate the cannabinoid type 2 (CB2) receptor in white blood cells, specifically macrophages, appear to weaken HIV-1 infection. The CB2 receptor is the molecular link through which the pharmaceutical properties of cannabis are manifested. Diminishing HIV-1 infection in this manner might make current anti-viral therapies more effective and provide some protection against certain HIV-1 complications.

“The synthetic compounds we used in our study may show promise in helping the body fight HIV-1 infection,'” said Yuri Persidsky, M.D., Ph.D., a researcher involved in the work from the Department of Pathology and Laboratory Medicine at Temple University School of Medicine in Philadelphia, PA. “As compounds like these are improved further and made widely available, we will continue to explore their potential to fight other viral diseases that are notoriously difficult to treat.”

To make this discovery, scientists used a cell culture model to infect human macrophages with HIV-1 and added synthetic compounds similar to the active ingredient in marijuana to activate the CB2 receptor. At different times during the infection, samples from the culture were taken to see if the replication of the HIV virus was decreased. The researchers observed diminished HIV growth and a possible protective effect from some HIV-1 complications.

“HIV/AIDS has posed one of the most significant health challenges in modern medicine,” said John Wherry, Ph.D., Deputy Editor of the Journal of Leukocyte Biology. “Recent high profile vaccine failures mean that all options need to be on the table to prevent or treat this devastating infection. Research on the role of cannabinoid type 2 receptors and viral infection may one day allow targeting these receptors to be part of combination therapies that use exploit multiple weaknesses of the virus simultaneously.””

http://medicalxpress.com/news/2013-04-synthetic-derivatives-thc-weaken-hiv-.html

Scientists weaken HIV infection in immune cells using synthetic agents – MedicalXpress

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“HIV, the virus that causes AIDS, is notorious for hiding within certain types of cells, where it reproduces at a slowed rate and eventually gives rise to chronic inflammation, despite drug therapy. But researchers at Temple University School of Medicine’s Department of Pathology and Laboratory Medicine and Center for Substance Abuse Research (CSAR) recently discovered that synthetic anti-inflammatory substances distantly related to the active ingredient of marijuana may be able to take the punch out of HIV while inside one of its major hideouts – immune cells known as macrophages.

The results suggest that selective CB2 agonists could potentially be used in tandem with existing antiretroviral drugs, opening the door to the generation of new drug therapies for HIV/AIDS. The data also support the idea that the human immune system could be leveraged to fight HIV infection.

“Our study suggests that the body’s own natural defenses can be made more powerful to fight some of the worst symptoms of HIV,” Persidsky explained. He also noted that stimulating CB2 receptors in white blood cells could produce similar benefits against other viral infections.

 The most promising compounds are those derived from THC (tetrahydrocannabinol), the main active substance in cannabis.”

More: http://medicalxpress.com/news/2013-05-scientists-weaken-hiv-infection-immune.html

Intractable nausea and vomiting due to gastrointestinal mucosal metastases relieved by tetrahydrocannabinol (dronabinol).

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“Four years following resection of a Clark’s level IV malignant melanoma, a 50-year-old man developed widespred metastatic disease involving the liver, bones, brain, gastrointestinal mucosa, and lungs. One week after whole brain radiation therapy, he was admitted to the hospital for nausea, vomiting, and pain.

He was treated with several antiemetic drugs, but it was not until dronabinol was added that the nausea and vomiting stopped.

Dronabinol was an effective antiemetic used in combination with prochlorperazine in nausea and vomiting unresponsive to conventional antiemetics.”

http://www.ncbi.nlm.nih.gov/pubmed/9392925