Activate Now
ProHealth health Vitamin and Natural Supplement Store and Health
Home  |  Log In  |  My Account  |  View Cart  View Your ProHealth Vitamin and Supplement Shopping Cart
800-366-6056  |  Contact Us  |  Help
Facebook Google Plus
Fibromyalgia  Chronic Fatigue Syndrome & M.E.  Lyme Disease  Natural Wellness  Supplement News  Forums  Our Story
Store     Brands   |   A-Z Index   |   Best Sellers   |   New Products   |   Deals & Specials   |   Under $10   |   SmartSavings Club

Trending News

Repair Damaged Mitochondria and Reduce Fatigue Up to 45%

'Healthy' Foods Differ by Individual

Higher vitamin D levels may be protective against acute rhinosinusitis

Curcumin: The All In One Solution

Eating More Homemade Meals May Reduce Risk of Type 2 Diabetes

Vitamin D Supplementation Associated with Improved Exercise Performance

Saffron reduces oxidative stress in metabolic syndrome patients

Specific vitamin D levels linked to heart problems

Basic Vitamin A Primer

Irritable bowel syndrome may be associated with maternal inheritance and mitochondrial DNA control r...

Print Page
Email Article

Scripps Develops Potent Alternative to Opioid Pain Drugs, Inspired by Rare Plant Compound

  [ 12 votes ]   [ Discuss This Article ] • May 24, 2011

“Pharmacological studies confirmed that while it's not an opiate, it's nearly as potent as morphine," with “remarkably few if any side effects.”

Scientists from the Florida campus of The Scripps Research Institute have for the first time accomplished a laboratory synthesis of a rare natural product isolated from the bark of a plant widely employed in traditional medicine. This advance may provide the scientific foundation to develop an effective alternative to commonly prescribed narcotic pain treatments.

The study, published online May 23 by Nature Chemistry, defines a chemical means to access meaningful quantities of the rare natural product conolidine ["Synthesis of Conolidine, a Potent Non-Opioid Analgesic for Tonic and Persistent Pain"].

Based on data from mouse models, the study also suggests that synthetic conolidine is a potent analgesic as effective as morphine in alleviating inflammatory and acute pain, with few, if any, side effects.

In recent years, there has been significant interest in developing alternatives to opiate-based pain medications such as morphine. While widely prescribed for pain, morphine has a number of adverse side effects that range from the unpleasant to the lethal, including nausea, chronic constipation, addiction, and breathing depression.

The rare natural product central to the study is derived from the bark of a widely grown tropical flowering plant Tabernaemontana divaricata (also known as crepe jasmine).

Long a part of traditional medicine in China, Thailand, and India, extract from the leaves has been used as an anti-inflammatory applied to wounds, while the root has been chewed to fight the pain of toothache. Other parts of the plant have been used to treat skin diseases and cancer.

Conolidine belongs to a larger class of natural products, called C5-nor stemmadenines, members of which have been described as opioid analgesics, despite a substantial discrepancy between potent in vivo analgesic properties and low affinity to opiate receptors. Conolidine is an exceptionally rare member of this family for which no therapeutically relevant properties had ever been described. Despite the potential value of conolidine and related C5-nor stemmadenines as leads for therapeutics, efficient methods to prepare these molecules were lacking.

A Classic Problem in Chemical Synthesis - Solved

"This was a classic problem in chemical synthesis," said Glenn Micalizio, an associate professor in the Department of Chemistry, who initiated and directed the study, "which we were able to solve effectively and efficiently - an achievement that made subsequent assessment of the potential therapeutic properties of this rare natural product possible."

Micalizio and his colleagues began working on the synthesis of the molecule after they arrived at Scripps Florida in 2008.

Testing For Potency

Once the synthesis was complete, research shifted to pharmacology for evaluation. The pharmacological assessment, performed in the laboratory of Scripps Florida Associate Professor Laura Bohn, showed that the new synthetic compound has surprisingly potent analgesic properties.

"Her pharmacological studies confirmed that while it's not an opiate, it's nearly as potent as morphine," Micalizio said.

• In various models of pain, the new synthetic compound performed spectacularly, suppressing acute pain and inflammatory-derived pain, two key measures of efficacy.

• Not only that, but the new compound passed easily through the blood-brain barrier, and was present in the brain and blood at relatively high concentrations up to four hours after injection.

Bohn herself was surprised by the compound's potency and by the fact it so readily enters the brain.

"While the pain-relieving properties are encouraging, we are still challenged with elucidating the mechanism of action," she said. "After pursuing more than 50 probable cellular targets, we are still left without a primary mechanism."

Remarkably Few If Any Side Effects

So far, the compound has shown remarkably few, if any, side effects, but that is something of a double-edged sword (from a research perspective).

"The lack of side effects makes it a very good candidate for development," Bohn said. "On the other hand, if there were side effects, they might provide additional clues as to how the compound works at the molecular level."

That remains a mystery.

• While the synthetic compound might be as effective as morphine, it doesn't act at any of the receptors associated with opiates.

• In fact, it misses most of the major neurotransmitter receptors completely, suggesting it may be highly tuned towards relieving pain while not producing multiple side effects.

While still in the early stages of development, further characterizations of conolidine may suggest further development as a human therapeutic for the treatment of pain.

This research was made possible by Scripps Florida start-up funds, resulting from a one-time appropriation of federal economic development funds by the State of Florida, as well as support from Palm Beach County

Source: Scripps Florida news release, May 23, 2011

Post a Comment

Featured Products From the ProHealth Store
Mitochondria Ignite™ with NT Factor® Optimized Curcumin Longvida® Ultra ATP+, Double Strength

Looking for Vitamins, Herbs and Supplements?
Search the ProHealth Store for Hundreds of Natural Health Products

Article Comments

Be the first to comment on this article!

Post a Comment

Free Chronic Fatigue Syndrome and Fibromyalgia Newsletters
Subscribe to
Subscribe Now!
Receive up-to-date ME/CFS, Fibromyalgia & Lyme Disease treatment and research news
 Privacy Guaranteed  |  View Archives

Repair Damaged Mitochondria and Reduce Fatigue Up to 45%

Featured Products

Ultra EPA  - Fish Oil Ultra EPA - Fish Oil
Ultra concentrated source of essential fish oils
Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium
FibroSleep™ FibroSleep™
The All-in-One Natural Sleep Aid
Energy NADH™ 12.5mg Energy NADH™ 12.5mg
Improve Energy & Cognitive Function
Mitochondria Ignite™ with NT Factor® Mitochondria Ignite™ with NT Factor®
Reduce Fatigue up to 45%

Natural Remedies

SAD? Coping with Seasonal Affective Disorder
Astaxanthin - A Little-Known but Power-Packed Nutrient Astaxanthin - A Little-Known but Power-Packed Nutrient
The Surprising Benefits of Probiotics - What You Didn't Know The Surprising Benefits of Probiotics - What You Didn't Know
Guarding Against the Dangers of Vitamin D Deficiency Guarding Against the Dangers of Vitamin D Deficiency
SAM-e: a Hard-Working Molecule that May Help Ease Pain & Brighten Mood SAM-e: a Hard-Working Molecule that May Help Ease Pain & Brighten Mood

What is Fibromyalgia?
Fibromyalgia Diagnosis
Fibromyalgia Symptoms
Fibromyalgia Causes
Fibromyalgia Treatments
Fibromyalgia Diet
Fibromyalgia Medications
M.E. & CFS
What is M.E./CFS?
M.E./CFS Diagnosis
M.E./CFS Symptoms
M.E./CFS Causes
M.E./CFS Treatments
M.E./CFS Diet
M.E./CFS Medications
What is Lyme Disease?
Lyme Disease Diagnosis
Lyme Disease Symptoms
Lyme Disease Causes
Lyme Disease Treatments
Lyme Disease Diet
Lyme Disease Medications
M.E. & CFS
Lyme Disease
General Health
ProHealth on Facebook  ProHealth on Twitter  ProHealth on Pinterest  ProHealth on Google Plus
Credit Card Processing