Hederacolchiside E

Planta Med. 2004 Jun;70(6):561-3.

Antioxidant activity of saponins isolated from ivy: alpha-hederin, hederasaponin-C, hederacolchiside-E and hederacolchiside-F.[Pubmed: 15241892]

The antioxidant activities of alpha-hederin and hederasaponin C from Hedera helix, and Hederacolchiside E and hederacolchiside F from Hedera colchica were investigated, in this study.
METHODS AND RESULTS:
The antioxidant properties of the saponins were evaluated using different antioxidant tests: 1,1-di-phenyl-2-picryl-hydrazyl (DPPH.) free radical scavenging, total antioxidant activity, reducing power, superoxide anion radical scavenging, hydrogen peroxide scavenging, and metal chelating activities. Alpha-hederin, hederasaponin C, as well as Hederacolchiside E and hederacolchiside F exhibited a strong total antioxidant activity. At the concentration of 75 pg/mL, these saponins showed 94, 86, 88 and 75% inhibition on lipid peroxidation of linoleic acid emulsion,respectively.
CONCLUSIONS:
These various antioxidant activities were compared with model antioxidants such as a-tocopherol, butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT).

Eur J Med Chem. 2018 Jan 1;143:376-389.

Synthesis, biological evaluation and structure-activity relationship studies of hederacolchiside E and its derivatives as potential anti-Alzheimer agents.[Pubmed: 29202401 ]

Inspired by the previously reported neuroprotective activity of Hederacolchiside E (1), we synthesized Hederacolchiside E for the first time along with eleven of its derivatives.
METHODS AND RESULTS:
The neuroprotective effects of these compounds were further evaluated against H2O2- and Aβ1-42-induced injury using cell-based assays. The derivatives showed obvious differences in activity due to structural variations, and two of them exhibited better neuroprotective effects than 1 in the Aβ1-42-induced injury model. Compound 7 was the most active derivative and had a relatively simple chemical structure. Moreover, 1 and 7 can significantly reduce the release of lactate dehydrogenase (LDH), level of intracellular reactive oxygen species (ROS) and extent of malondialdehyde (MDA) increase resulting from Aβ1-42 treatment, which demonstrated that these kinds of compounds show neuroprotective effects in Alzheimer's disease (AD) models via modulating oxidative stress.
CONCLUSIONS:
Compound 7 could be used as promising lead for the development of a new type of neuroprotective agent against AD.

Phytomedicine. 2005 Jun;12(6-7):440-4.

Acute anti-inflammatory activity of four saponins isolated from ivy: alpha-hederin, hederasaponin-C, hederacolchiside-E and hederacolchiside-F in carrageenan-induced rat paw edema.[Pubmed: 16008120 ]

METHODS AND RESULTS:
The anti-inflammatory potential of alpha-hederin (monodesmoside) and hederasaponin C from Hedera helix, and Hederacolchiside E and hederacolchiside F (bidesmosides) from H. colchica was investigated in carrageenan-induced acute paw edema in rats. Saponins and indomethacin were given orally in concentrations of 0.02 and 20mg/kg body wt. For the first phase of acute inflammation, indomethacin was found as the most potent drug. Alpha-hederin and hederasaponin C were found ineffective, while Hederacolchiside E and hederacolchiside F showed slight anti-inflammatory effects on the first phase. For the second phase of acute inflammation, indomethacin and hederacolchiside F were determined as very potent compounds. alpha-hederin was found ineffective for the second phase, either. Despite hederasaponin C and Hederacolchiside E were found effective in the second phase of inflammation, they were not found as effective as indomethacin and hederacolchiside F.
CONCLUSIONS:
As a conclusion, hederasaponin C, Hederacolchiside E and hederacolchiside F, may exert their anti-inflammatory effects by blocking bradykinin or other inflammation mediators. The latter affect may occur via affecting prostaglandin pathways. Regarding the structure activity relationship, it is likely that sugars at C3 position and Rha7-Glcl-6Glc moiety at C28 position are essential for the acute anti-inflammatory effect.

J Pharm Biomed Anal. 2008 Dec 15;48(5):1425-9.

LC-MS/MS method for determination of hederacolchiside E, a neuroactive saponin from Pulsatilla koreana extract in rat plasma for pharmacokinetic study.[Pubmed: 18947958 ]

METHODS AND RESULTS:
A simple, rapid, and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was applied to pharmacokinetic study of a neuroactive oleanolic-glycoside saponin, Hederacolchiside E from SK-PC-B70M, a standardized extract of Pulsatilla koreana in rat. Rat plasma samples were pretreated by protein precipitation with acetonitrile, eluted from C(18) column, and analyzed using electrospray ionization (ESI)-MS/MS in negative ion mode. Digoxin was used as an internal standard. The standard curves were linear (r>0.997) over the concentration ranges of 2-500 ng/mL. The intra- and inter-day precisions were measured to be below 9% and accuracy between 90 and 111% for all quality control samples at 2, 20, 100, and 500 ng/mL (n=5). The lower limits of quantification (LLOQ) for Hederacolchiside E was 2 ng/mL and the limit of detection (LOD) 0.5 ng/mL using 20 microL of plasma sample. Subsequently, Hederacolchiside E was determined in rat plasma samples after oral administration of SK-PC-B70M. The mean maximum plasma concentrations of Hederacolchiside E were 0.07, 0.13, and 0.36 microg/mL and the mean areas under the plasma concentration versus time curve 0.56, 1.27, and 6.46 microg h/mL at doses of 100, 200, and 400 mg/kg, respectively, which indicated non-linear pharmacokinetic pattern.
CONCLUSIONS:
In conclusion, this method was successfully applied to the pharmacokinetic study of Hederacolchiside E after an oral administration of SK-PC-B70M to rats.