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Rhodiola Profile
By David Tolson

Rhodiola is a genus of alpine plants containing over 200 different species that grow throughout Europe, Asia, and Alaska [1, 2], with over 70 of these in China [3]. At least 20 of these species have been used in Asian traditional medical systems, including R. alterna, R. brevipetiolata, R. crenulata, R. kirilowii, R. quadrifida, R. sachalinensis, R. sacra, and R. rosea [1]. A common Tibetan folk medicine, Rhodiola Radix, is a preparation of several Rhodiola plants that is used as a hemostatic, tonic and contusion [3-5].

One species, Rhodiola rosea (also known as "golden root"), is of particular interest. This species is widely distributed at high altitudes in Arctic and mountain regions throughout Europe and Asia, and has been a popular plant in traditional medicine in various areas of both Eastern Europe and Asia [1]. In Chinese medicine, it is used to enhance resistance against fatigue [2]. This species has been studied intensively in Russia and Scandinavia for over 35 years. The clearest benefit is adaptogenic and anti-stress activities, with memory support [1-5].

A number of pharmacologically active components have been identified in Rhodiola species, including organic acids, flavanoids, tannins, and phenolic glycosides [1]. Phenylpropanoid tyrosol (p. tyrosol), its glucoside salidroside (also known as rhodioloside or rhodosin), and phenylpropenoids rosin, rosarin, and rosavin all play important antioxidant and neurostimulant roles in the activity of Rhodiola rosea [2], with rhodioniside, rhodiolin, and rosiridin also implicated in R. rosea's adaptogenic activity [1]. Numerous other antioxidant compounds have been identified in Rhodiola species, including gallic acid, (-)-epigallocatechin 3-O-gallate, kaempferol, kaempferol 7-O-alpha-L-rhamnopyranoside, herbacetin 7-O-alpha-L-rhamnopyranoside, and rhodiolinin [6].

The mechanisms of action of Rhodiola rosea are many. These include antioxidant activity, propyl endopeptidase inhibition [2, 5], facilitation of monoaminergic activity, and opioid receptor activation. The enzyme propyl endopeptidase metabolizes various proline-containing neuropeptides including vasopressin, substance P, thyrotropin-releasing hormone, and alpha-melanocyte-stimulating hormone, all of which may play roles in learning and memory processes [5, 7]. Indeed, other propyl endopeptidase inhibitors improve spatial memory in animal models [7-8]. Rhodiola rosea may also inhibit monoamine oxidase (MAO) and catechol-O-methyltransferase (COMT) and facilitate the transport of neurotransmittors in the brain [1]. Another mechanism of action is the release of endorphins. Russian research indicates that Rhodiola rosea induces opioid peptide biosynthesis by activating opioid receptors in both the central and peripheral nervous system [1].

Rhodiola is among the herbs classified as adaptogens. The term "adaptogen" originated in Russia in 1947, and is defined as a substance that allows an organism to counteract adverse physical, chemical, or biological stressors by generating non-specific resistance. In 1969, specific criteria were created which need to be fulfilled before a substance qualifies as an adaptogen. Because Rhodiola rosea prevents a variety of deleterious effects caused by physical and intellectual stress and illness, it is classified as an adaptogen [1]. Rhodiola is also unique among adaptogens, in that it may be more effective than others in periods of acute stress, while most are primarily effective only in periods of chronic stress.

Because of its adaptogenic properties and its ability to increase the efficiency of mitochondrial respiration in skeletal muscle [3], Rhodiola is particularly useful for athletes, who regularly engage in taxing, high-intensity exercise, as it may both improve recovery and increase work output. As far as clinical trials in humans, the research in this area is sparse but very promising. A study with 1.5 grams per day of a Rhodiola crenulata root (which has a similar profile of active constituents to Rhodiola rosea) extract for 75 days found that it increased run time to exhaustion and maximum oxygen consumption in athletes [9]. Studies on the effect Rhodiola has on the work output of animals have also been done. Administration of Rhodiola for 10 days significantly increased the time that rats could spend running on a treadbane, with an even more significant increase after 20 days [10], and Rhodiola also increased the swimming times of rats in a "swim to the limit" test by 135-159% [1, 10].

In addition to increasing physical work capacity, Rhodiola rosea increases mental work capacity and induces a resistance to mental fatigue. In fact, it may directly support memory even in non-stressful conditions. Three double-blind placebo-controlled trials have recently been conducted in humans in this regard. The largest tested the effect of two doses of a standardized Rhodiola rosea extract in 160 19-21 year old cadets on mental capacity during a period of fatigue and stress. It found that both doses reduced the level of fatigue as measured by the antifatigue index (AFI) by over 10% [11]. Another study assessed the effect the same extract had on 56 young physicians on measures of mental fatigue, including tests of associative thinking, short-term memory, calculation and ability to concentrate, and speed of audio-visual perception during two weeks of night duty. There was a statistically significant improvement on all five tests used in the treatment group [12]. The last study looked at the effects a Rhodiola rosea extract had on physical and intellectual working capacity and measures of well being during a 20 day exam period in 40 students. The students that received Rhodiola had significant improvements. The treatment group also had 8.5% higher scores on the final exam [1, 13].

There have also been animal studies on the effect Rhodiola has on mental performance. In one of them, .1 mL of a Rhodiola rosea extract improved learning and memory within 24 hours and also improved long-term memory after 10 days in rats. However, two other doses of 20% as much and 10 times as much were ineffective, suggesting that there is a window of therapeutic activity [14]. Substantial neuroprotection has also been observed, with Rhodiola rosea having numerous benefits on metabolic processes in the brain [15].

Rhodiola also has adaptogenic activity in high altitude environments. Studies in humans living in high altitudes have found that Rhodiola improves sleep architecture and quality, along with other benefits [3, 16].

As stated earlier, there appears to be an ideal dosage range for Rhodiola above and below which it is ineffective. Unfortunately there is little literature in which the ideal dosage range has been explored in humans. The mental enhancement clinical trials described above used dosages of 370 and 555 mg, 170 mg, and 100 mg of Rhodiola rosea extract respectively, all standardized to 3.6% rosavin. In the first trial, there was a slight trend towards greater improvement in the lower dose. This would indicate that the ideal dosage for Rhodiola is in the range of 3.6-13.3 mg rosavin (total dosage varies based on the standardization of the extract), at least when using for 2-3 week periods. Rhodiola is also traditionally used in a cyclic fashion, with cycles ranging from a day to four months [1]. The general recommendation is for supplementation for 2-3 weeks prior and then throughout the duration of a high stress period, such as an exam, competition, or other deadline, followed by a period of abstinence. If Rhodiola is not already being regularly used, a dosage providing 10-20 mg rosavin is recommended prior to an expected stressful event. Few side effects are reported, but using over 30 mg of rosavin daily has been reported to cause insomnia and irritability [1].

If you have any questions or comments regarding this article, please email dvdtlsn@bulknutrition.com.


No part of this article may be reproduced in any form without the permission of David Tolson or Mike McCandless.


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References
1. Kelly GS. Rhodiola rosea: a possible plant adaptogen. Altern Med Rev. 2001 Jun;6(3):293-302 [pubmed]

2. Tolonen A, Pakonen M, Hohtola A, Jalonen J. Phenylpropanoid Glycosides from Rhodiola rosea. Chem Pharm Bull (Tokyo). 2003 Apr;51(4):467-70 [pubmed]

3. Ip SP, Che CT, Leung PS. Association of free radicals and the tissue renin-angiotensin system: prospective effects of Rhodiola, a genus of Chinese herb, on hypoxia-induced pancreatic injury. JOP. 2001 Jan;2(1):16-25 [pubmed]

4. Mook-Jung I, Kim H, Fan W, Tezuka Y, Kadota S, Nishijo H, Jung MW. Neuroprotective effects of constituents of the oriental crude drugs, Rhodiola sacra, R. sachalinensis and Tokaku-joki-to, against beta-amyloid toxicity, oxidative stress and apoptosis. Biol Pharm Bull. 2002 Aug;25(8):1101-4. [pubmed]

5. Fan W, Tezuka Y, Ni KM, Kadota S. Prolyl endopeptidase inhibitors from the underground part of Rhodiola sachalinensis. Chem Pharm Bull (Tokyo). 2001 Apr;49(4):396-401 [pubmed]

6. Lee MW, Lee YA, Park HM, Toh SH, Lee EJ, Jang HD, Kim YH. Antioxidative phenolic compounds from the roots of Rhodiola sachalinensis A. Bor. Arch Pharm Res. 2000 Oct;23(5):455-8 [abstract] [pubmed]

7. Bellemere G, Morain P, Vaudry H, Jegou S. Effect of S 17092, a novel prolyl endopeptidase inhibitor, on substance P and alpha-melanocyte-stimulating hormone breakdown in the rat brain. J Neurochem. 2003 Mar;84(5):919-29 [pubmed]

8. Shinoda M, Miyazaki A, Toide K. Effect of a novel prolyl endopeptidase inhibitor, JTP-4819, on spatial memory and on cholinergic and peptidergic neurons in rats with ibotenate-induced lesions of the nucleus basalis magnocellularis. Behav Brain Res. 1999 Feb 15;99(1):17-25 [abstract] [pubmed]

9. Bucci LR. Selected herbals and human exercise performance. Am J Clin Nutr. 2000 Aug;72(2 Suppl):624S-36S [pubmed]

10. Azizov AP, Seifulla RD. [The effect of elton, leveton, fitoton and adapton on the work capacity of experimental animals] Eksp Klin Farmakol. 1998 May-Jun;61(3):61-3 [abstract] [pubmed]

11. Shevtsov VA, Zholus BI, Shervarly VI, Vol'skij VB, Korovin YP, Khristich MP, Roslyakova NA, Wikman G. A randomized trial of two different doses of a Rhodiola rosea extract versus placebo and control of capacity for mental work. Phytomedicine. 2003 Mar;10(2-3):95-105 [abstract] [pubmed]

12. Darbinyan V, Kteyan A, Panossian A, Gabrielian E, Wikman G, Wagner H. Rhodiola rosea in stress induced fatigue--a double blind cross-over study of a standardized extract with a repeated low-dose regimen on the mental performance of healthy physicians during night duty. Phytomedicine. 2000 Oct;7(5):365-71 [abstract] [pubmed]

13. Spasov AA, Mandrikov VB, Mironova IA. [The effect of the preparation rodakson on the psychophysiological and physical adaptation of students to an academic load] Eksp Klin Farmakol. 2000 Jan-Feb;63(1):76-8 [abstract] [pubmed]

14. Petkov VD, Yonkov D, Mosharoff A, Kambourova T, Alova L, Petkov VV, Todorov I. Effects of alcohol aqueous extract from Rhodiola rosea L. roots on learning and memory. Acta Physiol Pharmacol Bulg. 1986;12(1):3-16 [abstract] [pubmed]

15. Pogorelyi VE, Makarova LM. [Rhodiola rosea extract for prophylaxis of ischemic cerebral circulation disorder] Eksp Klin Farmakol. 2002 Jul-Aug;65(4):19-22 [abstract] [pubmed]

16. Ha Z, Zhu Y, Zhang X, Cui J, Zhang S, Ma Y, Wang W, Jian X. [The effect of rhodiola and acetazolamide on the sleep architecture and blood oxygen saturation in men living at high altitude] Zhonghua Jie He He Hu Xi Za Zhi. 2002 Sep;25(9):527-30 [abstract] [pubmed]

17. Maimeskulova LA, Maslov LN. [Anti-arrhythmic effect of phytoadaptogens] Eksp Klin Farmakol. 2000 Jul-Aug;63(4):29-31 [abstract] [pubmed]

18. Lishmanov IuB, Naumova AV, Afanas'ev SA, Maslov LN. [Contribution of the opioid system to realization of inotropic effects of Rhodiola rosea extracts in ischemic and reperfusion heart damage in vitro] Eksp Klin Farmakol. 1997 May-Jun;60(3):34-6 [abstract] [pubmed]

19. Maslova LV, Kondrat'ev BIu, Maslov LN, Lishmanov IuB. [The cardioprotective and antiadrenergic activity of an extract of Rhodiola rosea in stress] Eksp Klin Farmakol. 1994 Nov-Dec;57(6):61-3 [abstract] [pubmed]

20. Afanas'ev SA, Alekseeva ED, Bardamova IB, Maslova LV, Lishmanov IuB. [Cardiac contractile function following acute cooling of the body and the adaptogenic correction of its disorders] Biull Eksp Biol Med. 1993 Nov;116(11):480-3 [abstract] [pubmed]

21. Wu XL, Zeng WZ, Wang PL, Lei CT, Jiang MD, Chen XB, Zhang Y, Xu H, Wang Z. Effect of compound rhodiola sachalinensis A Bor on CCl(4)-induced liver fibrosis in rats and its probable molecular mechanisms. World J Gastroenterol. 2003 Jul;9(7):1559-62 [pubmed]

22. Nan JX, Jiang YZ, Park EJ, Ko G, Kim YC, Sohn DH. Protective effect of Rhodiola sachalinensis extract on carbon tetrachloride-induced liver injury in rats. J Ethnopharmacol. 2003 Feb;84(2-3):143-8 [pubmed]

23. Iaremii IN, Grigor'eva NF. [Hepatoprotective properties of liquid extract of Rhodiola rosea] Eksp Klin Farmakol. 2002 Nov-Dec;65(6):57-9 [abstract] [pubmed]

24. Salikhova RA, Aleksandrova IV, Mazurik VK, Mikhailov VF, Ushenkova LN, Poroshenko GG. [Effect of Rhodiola rosea on the yield of mutation alterations and DNA repair in bone marrow cells] Patol Fiziol Eksp Ter. 1997 Oct-Dec;(4):22-4 [abstract] [pubmed]

25. Bocharova OA, Matveev BP, Baryshnikov AIu, Figurin KM, Serebriakova RV, Bodrova NB. [The effect of a Rhodiola rosea extract on the incidence of recurrences of a superficial bladder cancer (experimental clinical research)] Urol Nefrol (Mosk). 1995 Mar-Apr;(2):46-7. [abstract] [pubmed]






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