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Solanum glaucophyllum (a purple flower) produces active vitamin D3

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Dec 2013

Human Pharmacokinetic Profile of 1,25-Dihydroxyvitamin D3 - Glycoside of Herbal Origin.
J Steroid Biochem Mol Biol. 2013 Dec 5. pii: S0960-0760(13)00271-9. doi: 10.1016/j.jsbmb.2013.11.016.
Mathis GA, Toggenburger A, Pokorny R, Autzen S, Ibanez R, Romeis P, Bachmann H.
Appletree AG, Rudolf Diesel-Strasse 3, CH-8404 Winterthur, Switzerland. Electronic address: georg.mathis at appletree-cig.com.

A natural form of 1,25-dihydroxyvitamin D3 (1,25(OH)2D3), the active metabolite of vitamin D, was identified in glycosylated form in Solanum glaucophyllum (SG). Solbone P, an extract of SG with high and homogenous content of glycosylated 1,25(OH)2D3, was chemically characterized and produced under GMP conditions. Three different doses of glycosylated 1,25(OH)2D3 were given as single oral dose to 16 healthy volunteers in a first-in-man trial. The oral pharmacokinetic properties of 1,25(OH)2D3 of SG origin were established and the subjects were monitored until day 28 for safety reasons. This included regular monitoring of vital signs, electrocardiogram (ECG) data, calcium, phosphate and creatinine values.
Subjects were exposed to up to the equivalent of a 40-fold level of the recommended human daily dose for synthetic 1,25(OH)2D3 (0.5μg/subject/day) without experiencing any untoward effects. When compared with the historically established pharmacokinetics profile of synthetic 1,25(OH)2D3, glycosylated 1,25(OH)2D3 of herbal origin exhibited delayed absorption characteristics.
The phenomenon is species independent, as similar pharmacokinetic patterns were observed in rats and chickens. This modified release pattern may be attributed to the glycosylation of herbal 1,25(OH)2D3 because de-glycosylation by ubiquitous intestinal enzymes prior to intestinal uptake of the unmodified 1,25(OH)2D3 is the rate-limiting step.

The major relevance of this finding is that the human pharmacokinetic profile of glycosylated 1,25(OH)2D3of herbal origin is reminiscent of a delayed release formulation of free 1,25(OH)2D3, resulting in a wider therapeutic window, a potentially longer therapeutic effectiveness, and thus, a better pharmacologic tolerance.

PMID: 24316430

Solanum glaucophyllum as source of 1,25-dihydroxyvitamin D3. -1977

April 25, 1977 The Journal of Biological Chemistry, 252, 2580-2583.
J L Napoli, L E Reeve, J A Eisman, H K Schnoes and H F DeLuca

Vitamin D-deficient rats given an aqueous extract of the South American plant Solanum glaucophyllum accumulate 1,25-dihydroxyvitamin D3 in their blood and intestines at the time they show enhanced intestinal calcium absorption. The identity of the 1,25-dihydroxyvitamin D3 was established by co-chromatography with 1,25-dihydroxy[23,24-3H] vitamin D3 on Sephadex LH-20 columns, microparticulate silica gel columns, a reversed-phase column developed under high pressure, and by a specific 1,25-dihydroxyvitamin D3 binding assay. The chromatographic systems used are fully capable of resolving all of the known metabolites of vitamin D3. Serum of the S. glaucophyllum-treated rats showed 300 pg/ml of 1,25-dihydroxyvitamin D3 and no detectable 1,25-dihydroxyvitamin D2. Similarly, intestine of such rats had 230 pg/g of 1,25-dihydroxyvitamin D3. Control animals which received the vehicle instead of S. glaucophyllum had only 20 pg/ml of 1,25-dihydroxyvitamin D3 in their serum and 4.4 pg/g of 1,25-dihydroxyvitamin D2 in their intestine. These results demonstrate that S. glaucophyllum extracts must be a source of 1,25-dihydroxyvitamin D3; thus a significant basis for the calcinogenic properties of S. glaucophyllum must be the presence of a conjugated form of 1,25-dihydroxyvitamin D3, which is rendered available by digestion.

SG as a source of Vitamin D for chickens Oct 2013

The efficacy of a standardised product from dried leaves of Solanum glaucophyllum as source of 1,25-dihydroxycholecalciferol for poultry.
Br Poult Sci. 2013 Oct;54(5):642-52. doi: 10.1080/00071668.2013.825692. Epub 2013 Sep 23.
Bachmann H, Autzen S, Frey U, Wehr U, Rambeck W, McCormack H, Whitehead CC.
a Herbonis AG , Augst , Switzerland.

  • 1. Chemical characterisation of an extract of Solanum glaucophyllum (SG) leaves affirmed the predominant presence of 1,25-dihydroxycholecalciferol (1,25(OH)2D3) glycosides. The compound 1-(ß-D-glucopyranosyl)-1α,25-dihydroxycholecalciferol was isolated for the first time from a natural source.
  • 2. Vitamin D activity of the extract was confirmed by the calcaemic properties shown in a quail eggshell bioassay. The results suggested a 1,25(OH)2D3 bioavailability of approximately 15%.
  • 3. A broiler feeding experiment replicated in time was carried out with 6 treatments. A basic control diet containing 25 μg cholecalciferol/kg was supplemented with 2.5 and 5 μg free 1,25(OH)2D3/kg, with a product based on dried SG leaves (Panbonis) providing 10 μg of 1,25(OH)2D3-glycosides/kg, with two concentrations of an SG extract providing 8.8 and 37.8 μg of 1,25(OH)2D3-glycosides/kg.
  • 4. Tibia breaking strength and stiffness were numerically greater in all treatment groups with free 1,25(OH)2D3 and with SG products compared to controls, though the overall treatment effects only had probabilities in the range of P = 0.07 to P = 0.1. Values for both characteristics increased progressively, with additions of synthetic 1,25(OH)2D3; values with the dried SG product were similar to those with 5 μg synthetic 1,25(OH)2D3/kg.
  • 5. Plasma calcium was mildly elevated (P < 0.05) in treatment groups. The SG extract treatment containing 37.8 μg 1,25(OH)2D3/kg gave the highest plasma calcium concentration and lowest bodyweight, signs of marginal hypervitaminosis D. Plasma 1,25(OH)2D3 concentrations were in the normal range for all treatments.
  • 6. Tibial dyschondroplasia occurred in only one replicate. The incidences were 31% in controls but considerably lower or zero with all other treatments.
  • 7. Bioavailability of 1,25(OH)2D3 in the SG product seemed to be higher in broiler chickens than in Japanese quails. 8
  • . It is concluded that the inclusion of the dried SG product as a source of vitamin D3 in broiler diets at a dietary concentration of 1 g/kg, providing 10 μg 1,25(OH)2D3/kg, is safe and efficacious.

PMID: 24053600

US Small business grant of $80,000: SG for laying hens – 2005

Development of Solanum glaucophyllum as a Source of Vitamin D for Laying Hens
Egg breakage and cracking is a major economical problem for the US poultry industry which can affect up to 10% of the eggs produced. The resulting approximately 500 million dollars in lost revenue to producers is a cost ultimately borne by consumers. To minimize damaged eggs, producers have attempted to increase calcium in the ration but have had limited success because the hen's ability to utilize additional calcium is metabolically limited. Feeding vitamin D metabolites to increase calcium deposited in the eggshell has also been tried, but the most effective metabolite, 1,25-dihydroxy-vitamin D3, is currently too expensive for commercial use. This proposal will further develop a naturally occurring metabolite of vitamin D for use in laying hen diets. The metabolite is produced by the plant Solanum glaucophyllum as a vitamin D3-glycoside. This metabolite has the potential to increase the active vitamin D levels in the hen, thus improving calcium metabolism and eggshell strength.

SG for dairy cows - 2003

Abstraéis - Oral presentations at 11th ICPD, Acta vet. scand. Suppl. 98 - 2003
RL Horst1, JP Goff1, S. Gill2, ME Dallorso3, E. Pawlak2
'USDA/ARS, National Animal Disease Center, Ames, IA 50010; 2CAE, Buenos Aires, Argentina; 3Universidad Nacional de Lomas de Zamora, Buenos Aires, Argentina

Reducing cation-anion difference of diets (DCAD) fed just before parturition can prevent milk fever. However this dietary regimen does not entirely eliminate hypocalcemia. Milk fever can also be prevented by exogenous administration of the calcium regulating hormone 1,25-dihydroxyvitamin D. Unfortunately 1,25-dihydroxyvitamin D treatment remains expensive and the pre-partal diets used in most trials would be classified today as high in cations. Solanum glaucophyllum (Sg) is a plant that contains high levels of a glycoside form of 1,25-dihydroxyvitamin D. S. Glaucophyllum is widely distributed in the province of Buenos Aires in Argentina and in Brazil and causes the development of a calcinotic disease in cattle called "Enteque Seco". In order to become active the glycoside must be cleaved to liberate the 1,25(OH)2D3. Rumen microbes are very efficient at this process. Could ad-ministration of Sg leaves to cows that were already being fed a low DCAD pre-partum diet further improve calcium status at calving? Nine multiparous Jersey cows were fed a low DCAD diet prior to calving. Urine pH of cows was maintained below 7.0 in all cows the week prior to parturition. Five cows were daily given 2 or 3 g Sg leaves in gelatin boluses beginning 6 days (on average) before calving and continuing for the first 14 days of lactation. None of the four cows fed the low DCAD diet only developed milk fever. Their blood calcium concentration was 7.6, 7.0 and 8.0 mg/dl the day of calving and d 1 and 2 after calving respectively. Cows receiving Sg in addition to low DCAD diet had significantly higher blood calcium concentration during the periparturient period with blood calcium concentrations of 7.8, 8.8 and 9.3 mg/dl the day of calving and d 1 and 2 after calving respectively. Defining subclinical hypocalcemia as blood calcium <7.5 mg/dl, control cows suffered an average of 3 days of subclinical hypocalcemia and the Sg treated cows suffered 0.8 d of subclinical hypocalcemia the first 2 wk of lactation. Thus, Sg treatment improved calcium status in animals that were also being fed a low DCAD diet. Unfortunately, all cows receiving Sg suffered 1-2 days of hypocalcemia (1 cow developed milk fever) between 6 and 8 days after Sg treatment was ended. Mean blood calcium on d 22 of lactation of Sg cows was 6.9 mg/dl compared with 9.2 mg/dl in untreated cows. It appears that Sg treatment supplanted the cow's own calcium homeostasis mechanisms so that abrupt withdrawal of treatment left the cows temporarily unable to control blood calcium concentration. Additional experiments were conducted using a phased withdraw approach. Three cows were treated with Sg from 5 days prepartum to 7 postpartum (2 g Sg/d) from day 8-14 postpartum (1 g Sg/d) and day 15-21 postpartum (0.5 g Sg/d). The phased withdrawal approach re-sulted in normal calcium concentration for up to 2 weeks following cessation of Sg. These data suggest that Sg can be used successfully in the prevention of hypocalcemia and that a phased withdrawal approach to removing the exogenous source of 1,25-(OH)2D3 was successful in avoiding the hypocalcemic side effects associated with abrupt withdrawal.

Too much SG for pigs can be a problem if Vitamin D and Calcuim intake are not reduced - Feb 2017

Tolerance to 1,25 dihydroxyvitamin D3 glycosides from Solanum glaucophyllum by the growing pig
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SOLANUM GLAUCOPHYLLUM extraction has been patented

3 patents for SOLANUM GLAUCOPHYLLUM as a source for active Vitamin D

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Attached files

ID Name Comment Uploaded Size Downloads
8441 SG tolerance.pdf admin 17 Sep, 2017 452.72 Kb 1135
3367 SG2.jpg admin 10 Dec, 2013 16.77 Kb 25935
3366 SG1.jpg admin 10 Dec, 2013 9.80 Kb 7672