.gif "IP Gear")
- Joined
- Apr 9, 2021
- Messages
- 1,721
Phytoecdysteroids extracted from plants and anabolic activity
Author: Type-IIx
Plant sources of Central Asia
Ajuga turkestanica, samples collected in canyons near Derbent (Surkhan Region, Uzbekistan) contained 22-acetylcyasterone (0.12%), cyasterone (0.025%), ecdysterone (0.20%), and turkesterone (0.17%) after extraction [1]. Mamatkhanov cites Usamanoz et al's analysis of the turkesterone content of the raw plant material of Ajuga turkestanica root as containing "a yield of 0.052% on the weight of the raw material [3]. A methanol and/or 80% ethanol extraction process yielded about 0.14% of turkesterone from Ajuga turkestanica gathered from the Surkhandar'inskaya Oblast, Uzbekistan [3].
Turkesterone is also derived from the Leuzea carthamoides [Asteraceae], a rich source native to Southern Siberia, Kazakhstan, the Altay region, and Western Sayan Mountains. It is present in a lower abundance in Vitex and Tapinella species as well.
Turkesterone 193.6(%) effect size in a proxy for protein anabolism†, versus
Ecdysterone 167.3 [1]
It is significant to note that:
Silenoside A
Cyasterone
were also present naturally, and showed greater anabolism in measured tissue than ecdysterone [1]†. The measured tissue being the liver. These compounds were derived from other phytoecdysteroid(PE)-containing plants from Central Asia.
Other sampled plants from Syrov et al. included Silene praemixta M. Pop. (Chimkent Region, Kazakhastan) [2-deoxy-α-ecdysone (0.12%), viticosterone E (0.0017%), 2-deoxyecdysterone (0.082%),
α-ecdysone (0.025%), ecdysterone (0.65%)], Silene brahuca Boiss (Tashkent Region, Uzbekistan) [0.094% of ecdysterone, 0.020% integristerone A], Silene scabrifolia Koin (Dzhizak Regi
on, Uzbekistan) [2-deoxy-α-ecdysone (0.20%), ecdysterone 22-O-benzoate (0.16%),...
In all, 23 plant-derived PEs from four plant species were demonstrated to increase protein anabolism†. This is not intended as an exhaustive list of Syrov and his team's work.
Anabolism in skeletal & non-skeletal muscle tissue
Net protein accretion§ (proxy for "anabolism," intact pubertal rats) [approximate %Δ]:
- Turkesterone (5mg / kg):
- liver: +10
- heart: +20
- muscle: +25
- kidney: +15
- v. prostate: +20
- Ecdysterone (5mg / kg):
- liver: +7
- heart: +4
- muscle: +10
- kidney: +5
- v. prostate: +4 [2]
Structural effects on protein anabolism in humans:
- 2,3-diol system
- C-20 hydroxy group
- C-11 hydroxy group
- turkesterone's 11-oxy group sharply increases its anabolic effect [1] [7]
For discussion of potential mechanisms of action in human skeletal muscle hypertrophy: Phytoecdysteroids potential mechanisms of action in hypertrophy
Protein synthesis increase associated with polyribosomal activity and acceleration of the translocation processes rather than induction of new RNA synthesis [7].
Discussion
In the early 2000s, the work of Dr. Syrov was considered significant in the study of the prevalence of PEs, their anabolic effects in mammals, and importantly to some possessing a particular entrepreneurial spirit, as a source of a potentially lucrative performance-enhancing compound, chiefly turkesterone, that has variously been described as "more anabolic than Dbol" [see ¶ below for origin of the conflation (intentional or otherwise) of methylandrostenediol with methandrostenolone]. Uzbek biochemists strove to demonstrate the richness of Uzbekistan in the field of study of PEs, as well as a source of unparalleled turkesterone purity. Dr. Syrov and members of his team penned several whitepapers signing off with a nod to the doping potential of the PEs. The early 2000s were the heyday for PE supplements. Syrov penned in 2000 [2], "[P]hytoecdysteroids are of interest as potential agents capable of stimulating protein synthesis in the organism without violating the endocrine system functioning. The most active [PE (turkesterone)] may present an alternative to [AAS], the administration of which has serious limitations both in chemotherapeutic practice and in sports, where these agents are classified as prohibited... [2]"
The plants described by Syrov, et al. represented an inexhaustive sample, yet one that included three plant genii containing a potent blend of PEs that could be extracted using straightforward extraction processes (ethanol-methanol) and covered tens or hundreds of thousands of kilometers of travel throughout Central Asia. Therefore, it is fair to say that it could not fairly be dismissed as a mere sample of convenience. There are plants containing high concentrations of PEs beyond those enumerated by Dr. Syrov, however. Chiefly, the genii Serratula and Leuzea [7].
Odinokov et al. extracted 1.5% ecdysterone from the total yield of the juice of the Serratula coronata L. (Asteraceae) gathered in the South Urals territory (Russia), as well as isolating various other active PEs from the plant [9]. Folklore describes Siberians consuming hardy plants (now identified as containing high levels of PEs) to enhance stamina and ward off fatigue [5]. There is an abundance of research on PEs in the Chinese and Eurasian languages, indicating some prevalence of plants containing a wide spectrum of PEs in various concentrations.
Beyond the plant species enumerated, PEs are found as well in a variety of plants considered to have "nutraceutical" properties, providing a "whole body anabolism":
0.51mg/g of ecdysterone was extracted from wild quinoa using a DES extraction method [8].
Searching the literature, there are English-language references to other sources of anabolic PEs:
...
Biosynthesis and accumulation of 20-hydroxyecdysone in individual male and female spinach plants during the reproductive stage
DOI: 10.1016/j.plaphy.2018.06.027
Distribution and Biosynthesis of 20-Hydroxyecdysone in Plants of Achyranthes japonica Nakai
DOI: 10.1271/bbb.100410
Phytoecdysteroids in the genus Asparagus (Asparagaceae)
DOI: 10.1016/s0031-9422(00)00438-6
And many, many more studies like this.
Chinese PE products
Perhaps most interesting to the reader concerned with the quality of Chinese sources for PEs is the Cyanotis arachnoidea.
Cyanotis arachnoidea (China) is among the most potent sources of ecdysterone: its roots can contain up to 4-5% ecdysterone [10]. It is the source of ecdysterone in myriad commercially available ecdysterone-containing supplements. Dozens of companies, sometimes with a minimum order of 200kg of PE-containing extracts, offer several tons per year (some even climing to be able to supply over a ton per week for as low as 10 USD per kg), available for internet-based purchase worldwide [10].
A claimed "90% pure ecdysterone" supplement of Chinese origin was analyzed: 2 capsules (recommended daily dose) contained:
- 2-24mg ecdysterone (within safe limits, an effective human dose)
- ≤9mg 20E-acetate
- ≤11.7mg 20E3-acetate
- 0.2-0.8mg ajugasterone-like (newly discovered PE) compound
- 0.1-0.9mg shidasterone
- 0.3-1.8mg dacryhainansterone
- ≤0.3mg 5α-ecdysterone
- ≤0.7mg 2SR-S-20,26-dihydroxyecdysone + 2S-S20,26-dihydroxyecdysone,,[10],,
In this author's view, there are a few points to be made:
- "Chinese ecdysterone," i.e., Cyanotis arachnoidea is a potent source of the primary PE that has been extensively studied, efficacious, and quite safe
- This plant contains a similar profile of various understudied (in humans) PEs as compared to the Ajuga turkestanica- noteworthy, however, is its absence of turkesterone
- There is widespread prejudice against China even in the literature as a source country for alternative (Chinese traditional) medicine, and naturally contaminated and fraudulent products or marketing, and it is actually funny to read. This plant source is almost certainly perfectly safe to consume if you aim to consume a sane level of PEs.
- The appropriate stance in regard to the bioactive quantities and contents of any particular supplement product is a suspension of judgment in the absence of independent laboratory analysis (Refer to Phytoecdysteroids potential mechanisms of action in hypertrophy for a discussion regarding the findings of independent laboratory analysis on samples from commercially available supplements purported to contain ecdysterone). While the Ajuga turkestanica is considered a potent source of both ecdysterone and turkesterone, other plants contain ecdysterone in greater quantities as well as other active PEs, the particular effects of which are understudied or unknown in humans. Turkesterone in particular may not be the ideal choice for many users.
Author: Type-IIx
Plant sources of Central Asia
Ajuga turkestanica, samples collected in canyons near Derbent (Surkhan Region, Uzbekistan) contained 22-acetylcyasterone (0.12%), cyasterone (0.025%), ecdysterone (0.20%), and turkesterone (0.17%) after extraction [1]. Mamatkhanov cites Usamanoz et al's analysis of the turkesterone content of the raw plant material of Ajuga turkestanica root as containing "a yield of 0.052% on the weight of the raw material [3]. A methanol and/or 80% ethanol extraction process yielded about 0.14% of turkesterone from Ajuga turkestanica gathered from the Surkhandar'inskaya Oblast, Uzbekistan [3].
Turkesterone is also derived from the Leuzea carthamoides [Asteraceae], a rich source native to Southern Siberia, Kazakhstan, the Altay region, and Western Sayan Mountains. It is present in a lower abundance in Vitex and Tapinella species as well.
Turkesterone 193.6(%) effect size in a proxy for protein anabolism†, versus
Ecdysterone 167.3 [1]
It is significant to note that:
Silenoside A
Cyasterone
were also present naturally, and showed greater anabolism in measured tissue than ecdysterone [1]†. The measured tissue being the liver. These compounds were derived from other phytoecdysteroid(PE)-containing plants from Central Asia.
Other sampled plants from Syrov et al. included Silene praemixta M. Pop. (Chimkent Region, Kazakhastan) [2-deoxy-α-ecdysone (0.12%), viticosterone E (0.0017%), 2-deoxyecdysterone (0.082%),
α-ecdysone (0.025%), ecdysterone (0.65%)], Silene brahuca Boiss (Tashkent Region, Uzbekistan) [0.094% of ecdysterone, 0.020% integristerone A], Silene scabrifolia Koin (Dzhizak Regi
on, Uzbekistan) [2-deoxy-α-ecdysone (0.20%), ecdysterone 22-O-benzoate (0.16%),...
In all, 23 plant-derived PEs from four plant species were demonstrated to increase protein anabolism†. This is not intended as an exhaustive list of Syrov and his team's work.
Anabolism in skeletal & non-skeletal muscle tissue
Net protein accretion§ (proxy for "anabolism," intact pubertal rats) [approximate %Δ]:
- Turkesterone (5mg / kg):
- liver: +10
- heart: +20
- muscle: +25
- kidney: +15
- v. prostate: +20
- Ecdysterone (5mg / kg):
- liver: +7
- heart: +4
- muscle: +10
- kidney: +5
- v. prostate: +4 [2]
Structural effects on protein anabolism in humans:
- 2,3-diol system
- C-20 hydroxy group
- C-11 hydroxy group
- turkesterone's 11-oxy group sharply increases its anabolic effect [1] [7]
For discussion of potential mechanisms of action in human skeletal muscle hypertrophy: Phytoecdysteroids potential mechanisms of action in hypertrophy
Protein synthesis increase associated with polyribosomal activity and acceleration of the translocation processes rather than induction of new RNA synthesis [7].
Discussion
In the early 2000s, the work of Dr. Syrov was considered significant in the study of the prevalence of PEs, their anabolic effects in mammals, and importantly to some possessing a particular entrepreneurial spirit, as a source of a potentially lucrative performance-enhancing compound, chiefly turkesterone, that has variously been described as "more anabolic than Dbol" [see ¶ below for origin of the conflation (intentional or otherwise) of methylandrostenediol with methandrostenolone]. Uzbek biochemists strove to demonstrate the richness of Uzbekistan in the field of study of PEs, as well as a source of unparalleled turkesterone purity. Dr. Syrov and members of his team penned several whitepapers signing off with a nod to the doping potential of the PEs. The early 2000s were the heyday for PE supplements. Syrov penned in 2000 [2], "[P]hytoecdysteroids are of interest as potential agents capable of stimulating protein synthesis in the organism without violating the endocrine system functioning. The most active [PE (turkesterone)] may present an alternative to [AAS], the administration of which has serious limitations both in chemotherapeutic practice and in sports, where these agents are classified as prohibited... [2]"
The plants described by Syrov, et al. represented an inexhaustive sample, yet one that included three plant genii containing a potent blend of PEs that could be extracted using straightforward extraction processes (ethanol-methanol) and covered tens or hundreds of thousands of kilometers of travel throughout Central Asia. Therefore, it is fair to say that it could not fairly be dismissed as a mere sample of convenience. There are plants containing high concentrations of PEs beyond those enumerated by Dr. Syrov, however. Chiefly, the genii Serratula and Leuzea [7].
Odinokov et al. extracted 1.5% ecdysterone from the total yield of the juice of the Serratula coronata L. (Asteraceae) gathered in the South Urals territory (Russia), as well as isolating various other active PEs from the plant [9]. Folklore describes Siberians consuming hardy plants (now identified as containing high levels of PEs) to enhance stamina and ward off fatigue [5]. There is an abundance of research on PEs in the Chinese and Eurasian languages, indicating some prevalence of plants containing a wide spectrum of PEs in various concentrations.
Beyond the plant species enumerated, PEs are found as well in a variety of plants considered to have "nutraceutical" properties, providing a "whole body anabolism":
0.51mg/g of ecdysterone was extracted from wild quinoa using a DES extraction method [8].
Searching the literature, there are English-language references to other sources of anabolic PEs:
...
Biosynthesis and accumulation of 20-hydroxyecdysone in individual male and female spinach plants during the reproductive stage
DOI: 10.1016/j.plaphy.2018.06.027
Distribution and Biosynthesis of 20-Hydroxyecdysone in Plants of Achyranthes japonica Nakai
DOI: 10.1271/bbb.100410
Phytoecdysteroids in the genus Asparagus (Asparagaceae)
DOI: 10.1016/s0031-9422(00)00438-6
And many, many more studies like this.
Chinese PE products
Perhaps most interesting to the reader concerned with the quality of Chinese sources for PEs is the Cyanotis arachnoidea.
Cyanotis arachnoidea (China) is among the most potent sources of ecdysterone: its roots can contain up to 4-5% ecdysterone [10]. It is the source of ecdysterone in myriad commercially available ecdysterone-containing supplements. Dozens of companies, sometimes with a minimum order of 200kg of PE-containing extracts, offer several tons per year (some even climing to be able to supply over a ton per week for as low as 10 USD per kg), available for internet-based purchase worldwide [10].
A claimed "90% pure ecdysterone" supplement of Chinese origin was analyzed: 2 capsules (recommended daily dose) contained:
- 2-24mg ecdysterone (within safe limits, an effective human dose)
- ≤9mg 20E-acetate
- ≤11.7mg 20E3-acetate
- 0.2-0.8mg ajugasterone-like (newly discovered PE) compound
- 0.1-0.9mg shidasterone
- 0.3-1.8mg dacryhainansterone
- ≤0.3mg 5α-ecdysterone
- ≤0.7mg 2SR-S-20,26-dihydroxyecdysone + 2S-S20,26-dihydroxyecdysone,,[10],,
In this author's view, there are a few points to be made:
- "Chinese ecdysterone," i.e., Cyanotis arachnoidea is a potent source of the primary PE that has been extensively studied, efficacious, and quite safe
- This plant contains a similar profile of various understudied (in humans) PEs as compared to the Ajuga turkestanica- noteworthy, however, is its absence of turkesterone
- There is widespread prejudice against China even in the literature as a source country for alternative (Chinese traditional) medicine, and naturally contaminated and fraudulent products or marketing, and it is actually funny to read. This plant source is almost certainly perfectly safe to consume if you aim to consume a sane level of PEs.
- The appropriate stance in regard to the bioactive quantities and contents of any particular supplement product is a suspension of judgment in the absence of independent laboratory analysis (Refer to Phytoecdysteroids potential mechanisms of action in hypertrophy for a discussion regarding the findings of independent laboratory analysis on samples from commercially available supplements purported to contain ecdysterone). While the Ajuga turkestanica is considered a potent source of both ecdysterone and turkesterone, other plants contain ecdysterone in greater quantities as well as other active PEs, the particular effects of which are understudied or unknown in humans. Turkesterone in particular may not be the ideal choice for many users.
