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curcumin and piperine
Lane Simonian
Posted: Saturday, October 13, 2012 10:14 AM
Joined: 12/12/2011
Posts: 4983


 

Curcumin has often been suggested as treatment for Alzheimer's disease, but it has very low uptake rate into the bloodstream.  Scientists are working on improving the bioavailability of curcumin, but apparently a natural way already exists to do this: piperine in black pepper. 

 

http://www.ncbi.nlm.nih.gov/pubmed/9619120 

 

There are supplements with curcumin and piperine, but I have not seen any data regarding their effectiveness in treating Alzheimer's disease. This article suggests that these supplements might help. 

 

http://parkinsonsand5htp.blogspot.com/2012/04/turmericcurcumin-has-huge-therapeutic.html 

 

Turmeric was dubbed "the spice of life" in ancient times. It's called "the holy powder" in India today and figures prominently in the millions of curries served up every day on the Indian Subcontinent. Ayurveda medicine attributes life-enhancing qualities to turmeric.

Those of us in the West might dismiss these claims as folklore, but over the past decade clinical studies have shown that curcumin -- the active ingredient in turmeric -- has great promise as a remedy for:
 

  • Alzheimer's
  • Parkinson's
  • MS
  • Cancer
  • Diabetes
  • Arthritis
  • Depression

 

The Research Obstacle 
But there's a major obstacle, turmeric is not easily absorbed into our bodies. Clinical tests showing its potential were mostly based on injecting curcumin into mice. Oral consumption by humans -- even in large amounts -- doesn't show much therapeutic benefit.

 
Researchers are working on this absorption problem. They're developing compounds designed to provide curcumin with a delivery vehicle to survive the brutal human GI tract -- a pathway that usually destroys natural curcumin. Several synthetic methods in development include nano-particle engineering.

 
A more natural approach to the absorption problem involves combining turmeric with piperine, found in black pepper. Studies suggest that this addition may increase curcumin absoption by almost 2000%. 

 
Elderly, rural Indians -- with their traditional diets -- have among the world's lowest incidence of Alzheimer's. Their curries are prepared with complex spice combinations, including black pepper, that may enable their bodies to absorb more curcumin.
 
The Bigger Obstacle from Our Health System
Given turmeric's gigantic promise, why is research so limited?

Bharat Aggarwal, professor of cancer research at the University of Texas and a leading curcumin researcher, says that big, expensive human trials haven't happened because the drug companies can't make money selling a curry spice that's available at your local grocery store. But anecdotally, he says, "I have a thousand patients who correspond with me, and the response [to curcumin] has been overwhelming."

Reviewing the mounting evidence of the powerful role this substance can play as an anti-inflammatory agent, an essay on the Nutrition Wonderland website concluded:
So we have to leave this story where we have left so many before it. Turmeric and its flavonoid curcumin show massive therapeutic benefits for all sorts of diseases and maladies. Inflammatory pain from arthritis, elderly suffering from mental decline and women genetically predisposed to cancer would appear to benefit from this compound. But no doctor in his right mind would recommend such a protocol until it was rigorously studied against the barrage of unknown drug interactions, and, of course, amidst a minefield of malpractice litigation.
Here we wait, for additional study that will probably never come on the scale required to elevate curcumin to the echelon of a true pharmaceutical-type product. The advances are novel and interesting but remain in a medical gray area until the structure of the medical system is updated to take herbal medicine seriously. Let’s hope for a day when someone with a bit more training than the clerk at your local vitamin/herb store can legally guide you towards therapeutic herbal remedies. 
 

 

 

 

 


Lane Simonian
Posted: Saturday, October 13, 2012 10:21 AM
Joined: 12/12/2011
Posts: 4983


I posted this on another website regarding the usefulness of methoxyphenols in the treatment of Alzheimer's disease.  The article from which it comes is quite technical, but from what I could understand of it quite accurate as well. 

 

1). Numerous pieces of evidence suggest that curcumin may be a promising therapy for AD because it has different neuroprotective activities, including antioxidant [9], anti-inflammatory [10] and antiamyloidogenic properties [11]. Curcumin has been demonstrated to have a strong antioxidant neuroprotective effects, scavenging ROS [12] and neutralizing nitric-oxide-(NO-) based free radicals [13]. However, one of the issues of curcumin as a therapeutic agent in the treatment of AD is its poor water solubility [14], which is one reason for its low bioavailability following oral administration or through parenteral route [15]. The poor bioavailability is one of the causes of its failure in randomized control trials for AD.

The structural features of curcumin that can contribute to the antioxidant activity are the phenolic and the methoxy group on the phenyl ring and the 1,3-diketone system. Moreover, the antioxidant activity of curcumin increases when the phenolic group with a methoxy group is at the ortho position [16, 17]. The orthomethoxy group can form an intramolecular hydrogen bond with the phenolic hydrogen, making the H-atom abstraction from the orthomethoxyphenols surprisingly easy [18]. The H abstraction from these groups is responsible for the remarkable antioxidant activity of curcumin.

 

Taking into account that in vivo evidence showed that peroxynitrite induces Alzheimer-like tau hyperphosphorylation, nitration, and accumulation [26], it was reported that curcumin mediates the direct detoxification of reactive nitrogen species such as peroxynitrite, thus exerting an antioxidant activity [27].

 

Davinelli, Pleitropic Protective Effects of Phytochemicals in Alzheimer's Disease (2012).

 

http://www.hindawi.com/journals/oximed/2012/386527/ 

 

My only point is this if during the mid-1990s, a series of scientist found that peroxynitrite-mediated damage was widespread in Alzheimer's disease, would it not have made sense to at least see if inhibiting peroxynitrite formation, scavenging peroxynitrites, and partially repairing this damage might have some effect on cognitive function in Alzheimer's patients. Indeed, the evidence from small-sacle clinical trials using methoxyphenols that effectively reach the brain i.e. eugenol in rosemary essential oil via aromatherapy and several methoxyphenols (especially vanillic acid) in heat-processed ginseng suggests that the answer is yes. It's not my hypothesis; I have no financial stake in it nor any pride of ownership. I am just suggesting if your main interest is in treating this disease effectively this might be a good place to look.

 


Geo
Posted: Monday, October 15, 2012 10:38 PM
Joined: 6/20/2012
Posts: 34


Thanks for  that. I search for information on curcumin a lot.

There are many other ways proposed to increase bio-availability including nanoparticles, microemulsions and liposomes.

 

However I guess most people are interested in possible DIY methods that don't cost thousands in lab equipment.

These could include:

1.) Binding with casein in milk

 

http://www.ncbi.nlm.nih.gov/pubmed/19831420

2.) Encapsulating in hydrophobically modified starch

http://www.researchgate.net/publication/202982086_Enhanced_in_vitro_anti-cancer_activity_of_curcumin_encapsulated_in_hydrophobically_modified_starch

3.) Curcumin impregnated fenugreek


http://www.sciencedirect.com/science/article/pii/S1756464612000059

What I find interesting about these approaches is that they already exist in Indian cooking to some extent. Turmeric could bind and dissolve with the starch in rice, bind to the milk in diary food added during cooking and of course fenugreek is widely used in Indian cooking.

 


Lane Simonian
Posted: Tuesday, October 16, 2012 11:04 AM
Joined: 12/12/2011
Posts: 4983


Great information, Geo.  I was not aware of any of this.  Not only does it explain why more curcumin likely makes it to the brain via the Indian diet, but many Indian herbs also contain saponins (fenugreek, Bacopa monnieri, and Aswagandha root) that may also be helpful in the treatment of Alzheimer's disease.  I don't know if the expensive routes are any more effective in term of increasing the bioavailability of curumin, but if not these are potentially very good (and cheap) ways around the hdyrophobic nature of curcumin.
Geo
Posted: Wednesday, October 17, 2012 9:54 PM
Joined: 6/20/2012
Posts: 34


Thanks. Sorry about the formatting of my last post...this board handles spaces and newlines in a strange way.

On the hydrophobically modified starch there is some more info. here


http://www.racehorseherbal.com/phpbb/viewtopic.php?f=3&t=458

The owner of that site posts on a Yahoo group that I'm a a member of and he added some details about how he used the curcumin with HMS:

As I recall, I made a 1% solution of HMS and added a good amount of curcumin to it--probably at a rate of 1mg/ml. By adding an "excessive amount" not all will go into solution. Curcumin will dissolve at approx 1mg/ml of various organic solvents like DMSO, ethanol, etc., so I would use that number as a good starting part for how much curcumin to use. No use using any more than that in water.

They use a T-25 homogenizer which I do have and used, but I should think one could use a ultrasonic cleaner to about the same effect. If you have a magnetic stirrer, that might be good to use too and they can be bought used on ebay pretty cheap. Instead of using a centrifuge like the paper used to remove any curcumin that did not go into solution, just filter out what didn't with a coffee filter, etc.


Lane Simonian
Posted: Thursday, October 18, 2012 12:17 AM
Joined: 12/12/2011
Posts: 4983


I enjoyed the site that you linked, too.  I am not certain what is the best way to increase the uptake of curcumin, but this is an interesting option.

 

Don't worry about the spacing; this board doesn't make it easy. 


Geo
Posted: Thursday, October 18, 2012 1:02 PM
Joined: 6/20/2012
Posts: 34


I know, we know so little about all this.

Something that caught my eye on that site was an abstract that mentioned during high heating of curcumin:

.

.

 

"Among several of the degradation compounds of curcumin, three major

ones were characterized as ferulic acid, vanillin and vanillic acid"

I think this board section was discussing ferulic acid a few weeks ago.


Geo
Posted: Thursday, October 18, 2012 1:24 PM
Joined: 6/20/2012
Posts: 34


I had a go impreganting fenugreek seeds with curcumin myself. The idea is that fenugreek acts as as a galactomannan and will absorbe and then release curcumin more slowly.

.

However fenugreek seeds are like gravel chippings and I need to get some finely powdered seeds.

.


It got me thinking though that ispaghula husk used in constipation powders might also be suitable for that. The Wiki of ispaghula husk indeed says that it is being studied as a novel drug delivery method under the broad term 'gastroretentive' drug delivery systems.

.


I had a go mixing ispaghula husk with olive oil and curcumin and blending it ultrasonically. I have no real way of knowing how much it increases the bioavailibilty of curcumin. I just wanted to see what happened.

.

I did find out something interesting about olive oil though. I wanted to double check that treating olive oil with ultrasound wouldn't toxify it in some way and I found a paper suggesting the opposite, that ultrasound actually increases the radical scavenging activity and phenols in oilive oil:

.

http://www.ncbi.nlm.nih.gov/pubmed/22281378

.

Who knows which other oils could be enhanced like that. It could take years or even decades for that kind of research to be carried out.


Lane Simonian
Posted: Thursday, October 18, 2012 5:35 PM
Joined: 12/12/2011
Posts: 4983


Finding ways to increase the bioavailability of phenolic compounds and to increase the concentration of phenols may indeed be critical for treating Alzheimer's disease.  Every bit of information you provide, Geo, is intriguing and potentially very useful. 

 

The problem with ferulic acid is the opposite of that of curcumin: it is water soluble but not very lipid soluble--so it enters the bloodstream easily, but not into the brain. Methoxyphenols/phenolic acids such as eugenol, vanillin, vanillic acids, ferulic acid, and coumaric acid are among the best antioxidants for the treatment of Alzheimer's disease.  The heat processing of ginseng (similar to the hear processing of curcumin) appears to increase the concentration of many of these phenolic acids.

 

http://www.ncbi.nlm.nih.gov/pubmed/19298205 

 

https://docs.google.com/viewer?a=v&q=cache:W8AbO4EWg9IJ:www.ddtjournal.com/action/downloaddoc.php?docid%3D23+heat-processed+ginseng+relaxing+no3&hl=en&gl=us&pid=bl&srcid=ADGEESi1jJkImuhPjq-cQPlxDovXwM7VebFXS7CMz47bIWF-5RmLnF3PfzabPorrBfWmkemhywVLUZjGS7Dmf_OOPu72g70oxMySNDqhKmh_ZcXHwDpfb2UJqWA6QAML2BON9Kqd2-D_&sig=AHIEtbSuqRRjFDhq5NkR7qR_rC6vPXNkjg 

 

I have focused on eugenol in various essential oils as a potentially effective treatment for Alzheimer's disease but vanillin in vanilla essential oil may also be effective.

 

 

.Vanillin, the active component of vanilla, has antioxidant activity and appears to offset some of the oxidative damage that occurs in the brains of patients with Alzheimer’s disease particularly the formation of a compound called peroxynitrite. Peroxynitrite plays a role in other degenerative diseases of the brain such as Parkinson’s disease. Although research in this area is still in its infancy, it may hold future promise for people dealing with these debilitating diseases.

 

http://www.erzuliecosmetics.com/component/content/article/37-ingredient-glossary/89-vanilla-essential-oil 

 

Find the right methoxyphenols in the right concentrations and I am almost certain you can partially reverse Alzheimer's disease.

 


Lane Simonian
Posted: Friday, October 19, 2012 12:07 AM
Joined: 12/12/2011
Posts: 4983


This little excerpt gives some indication as to which compounds are the best peroxynitrite scavengers and thus most likely to effectively treat Alzheimer's disease: 

 

Peroxynitrite scavenging of flavonoids: structure activity relationship

CGM Heijnen, GRMM Haenen, JAJM Vekemans… - Environmental …, 2001 - Elsevier
... For example, ferulic acid (IC 50 =1.41 μM) is expected to be a potent peroxynitrite scavenger since the activity of its OH group is enhanced by an electron-donating substituent, an OCH 3 moiety, at the ortho position. The same active centre is shown in vanillic acid and eugenol ...  

 

 

 


Lane Simonian
Posted: Friday, October 19, 2012 10:19 AM
Joined: 12/12/2011
Posts: 4983


Another case where heating a compound (in this case ferulic acid) may increase its antioxidant capacity. 

 

https://docs.google.com/viewer?a=v&q=cache:sQozoIQg63oJ:www.mdpi.com/1420-3049/14/6/2118/pdf+syringic+acid+hydrophobic&hl=en&gl=us&pid=bl&srcid=ADGEESgB8a3lK52NgJjN3btvka7BWoR1PgTXbx17AD7NullgwVuyBYhMbsVHY9bWoWZgqjU-L2XhNwBm0XPmZVAX6AnM3aZ5XUJMlpaaPlEydh9s-IYRgqSlysKr2ilBIANwhpN-tVi3&sig=AHIEtbT1Djoof1zPTCYir2XLRj0JJ1dF7Q