Timosaponin BII

Chinese Pharmacological Bulletin, 2009, 25(2):244-7.

Protective effects of timosaponin BII on primary neurons against beta amyloid peptide 25-35.[Reference: WebLink]

To study the protective effects of Timosaponin BII on primary neurons against beta amyloid peptide 25-35 induced toxicity.
METHODS AND RESULTS:
Immunofluorescence was used to identify primary neurons. MTT(tetrazolium salt) assay was used to measure neurons metabolic state. Spectrophotometric method was used to measure the release of LDH (lactate dehydrogenase), the activity of SOD (superoxide dismutase), the activity of AChE (acetylcholine) and the production of MDA(malonaldehyde) in the culture medium.Treatment with beta amyloid peptide 25-35 (20 μmol · L-1) for 24 h caused a significant damage in primary neurons. Timosaponin BII 10-4 10-5 mol · L-1 markedly improved neurons metabolic activity, decresed the release of LDH and the production of MDA, markedly increased the activity of SOD and decresed the activity of AChE.
CONCLUSIONS:
Timosaponin BII could significantly reduce the neurotoxicity induced by beta amyloid peptide 25-35 in primary neurons. The mechanism of which may be related with resisting oxidative damage and regulating the cholinergic system.

Arch Pharm Res . 2015;38(5):598-603.

Cytotoxic activities of chemical constituents from rhizomes of Anemarrhena asphodeloides and their analogues[Pubmed: 25005066]

Abstract Seven steroidal saponins (1-7) and two xanthones (8, 9) were isolated from the rhizomes of Anemarrhena asphodeloides. Then in order to discover more analogues, which may possess good biological activity, the structural modifications of 2 and 9 were performed by acid hydrolysis and acetylation. Consequently, one novel steroidal saponin (2d, Timosaponin BII-d), three compounds (2c, 2e and 2f) which were also the new products prepared by the diluted acid hydrolysis of 3 by our group previously, and four known compounds (2a, 2b, 9a and 9b) were obtained. The structures were elucidated by analyses of NMR and MS data. All the compounds were evaluated for their cytotoxicities against BEL-7402, HT-29, HeLa and MDA-MB-468 cell lines in vitro by Sulforhodamine protein coloration method. Compounds 1, 2, 2b, 4-6, 9a and 9b showed certain anti-proliferative activities against the four cell lines, in which compounds 2, 4 and 9b exhibited especially more potent activities. The structure-activity relationships of these compounds were simply discussed.

Planta Med. 2012 Jan;78(1):18-23. doi: 10.1055/s-0031-1280268.

Anti-diabetic effects of TongGuanWan, a Chinese traditional herbal formula, in C57BL/KsJ-db/db mice.[Pubmed: 22002851]

In the present study, the anti-diabetic effects of a traditional Chinese medicinal formula extract, TongGuanWan, were investigated in type 2 diabetic animals.
METHODS AND RESULTS:
It was orally administered to C57BL/KsJ-db/db mice once a day for 4 weeks at the doses of 62, 125, and 250 mg/kg body weight. TongGuanWan significantly lowered the blood glucose and glycosylated haemoglobin levels as well as improved the glucose tolerance in db/db mice. The serum triglyceride levels in the db/db mice were significantly decreased, whereas the high-density lipoprotein cholesterol levels were significantly increased, after treatment with this herbal formula. TongGuanWan also markedly decreased the animals' body weights compared to those of the control db/db group but did not alter food intake. The effects of TongGuanWan were compared to those of the drug rosiglitazone. In addition, five main constituents of TongGuanWan, mangiferin, berberine, cinnamic aldehyde, Timosaponin BII, and timosaponin AIII, were quantified using high performance liquid chromatography coupled with a diode array and an evaporative light scattering detector (HPLC-DAD-ELSD).
CONCLUSIONS:
These results suggest that TongGuanWan may be useful for the treatment of type 2 diabetes.

US20090075912[P]. 2009.

Use of Timosaponin BII in the Preparation Of A Medicament or Product for the Prevention and Treatment of Stroke[Reference: WebLink]

The invention disclosed the use of Timosaponin BII in the preparation of a medicament or product for the prevention and treatment of stroke. The experiments prove that Timosaponin BII can improve the neurological symptoms of cerebral ischemic rat, reduce infarct size, relieve brain water edema, improve hemorheology, reduce inflammatory injury of cerebral ischemia.

BMC Complement Altern Med. 2012 Oct 22;12:189.

Timosaponin-BII inhibits the up-regulation of BACE1 induced by ferric chloride in rat retina.[Pubmed: 23082924]

Our previous studies indicated that oxidative stress up-regulated the expression of β-amyloid precursor protein cleavage enzyme-1 (BACE1) in rat retina. Pharmacological reports have shown Timosaponin BII, a purified extract originating from Chinese medical herb Rhizoma Anemarrhenae, is characterized as an antioxidant.
METHODS AND RESULTS:
Our present study aimed to determine whether Timosaponin BII affected the expression of BACE1, β-amyloid precursor protein cleavage production of Aβ1-40 and β-C-terminal fragment (β-CTF) in rat retina, which were pre-treated with the oxidizing agent (solution of FeCl₃). Few distinctions of BACE1 distribution were observed among all groups (normal control group, model group, Timosaponin BII treated and vehicle control groups). Rat retinas in model group and vehicle control group manifested an apparent up-regulation of BACE1 expression. Meanwhile, the level of malonaldehyde (MDA), Aβ1-40 and β-CTF were increased. However, when comparing with the vehicle control group, the retinas in Timosaponin BII treated group showed significantly less BACE1 (p<0.05) and accumulated less Aβ1-40 or β-CTF (p<0.05). It also showed significantly decreased level of MDA (p<0.05) and prolonged partial thromboplastin time (p<0.05).
CONCLUSIONS:
Our data suggested that Timosaponin BII remarkably inhibited the up-regulation of BACE1 and reduced the over-production of β-CTF and Aβ in rat retina, which was induced by FeCl₃. The mechanism of Timosaponin BII on BACE1 expression may be related to its antioxidant property.

J Asian Nat Prod Res. 2010 Nov;12(11):955-61.

Hydrolysis of timosaponin BII by the crude enzyme from Aspergillus niger AS 3.0739.[Pubmed: 21061217 ]

Timosaponin BII (1), a steroidal saponin showing potential anti-dementia activity, was regioselectively hydrolyzed into its deglycosyl derivatives by the crude enzyme from Aspergillus niger AS 3.0739. Three biotransformation products, Timosaponin BII-a (2), Timosaponin BII-b (3), and Timosaponin BII-c (4), were purified and their structures were elucidated on the basis of 1D NMR, 2D NMR, FAB-MS, and HR-ESI-MS spectral data. Compounds 2 and 3 are new compounds.