Saikosaponin B1

Recognition and identification of active components from Radix Bupleuri using human neuroblastoma SH-SY5Y cells[Reference: WebLink]

Biomed. Chromatogr., 2015, 30(3):191-6.

Aim to screen active components of Radix bupleuri (a traditional Chinese herb) and discover novel anti-schizophrenic candidate drugs by using human neuroblastoma SH-SY5Y cells. SH-SY5Y cells were used for preparation of the stationary phase in the Cell Membrane Chromatography (CMC) model.
METHODS AND RESULTS:
Retention components by the SH-SY5Y/CMC model were collected and then analyzed by GC/MS under the optimized conditions in offline conditions. After investigating the suitability and reliability of the SH-SY5Y/CMC method using amisulpride and haloperidol as standard compounds, this method was applied to screening active components from the extracts of Radix bupleuri. Retention components of SH-SY5Y/CMC model were saikosaponin A, Saikosaponin B1, saikosaponin B2, saikosaponin C and saikosaponin D, which were identified by the GC/MS method. In vitro pharmacological trials-MTT, Saikosaponin B1, saikosaponin B2 and saikosaponin C could protect SY5Y cells. The protect effect of Saikosaponin B1 and saikosaponin C were concentration dependent. Saikosaponin A and saikosaponin D inhibited cell viability at concentrations greater than 30 μg/mL (P<0.05). Via SH-SY5Y/CMC method and SH-SY5Y MTT trial, we rapidly detected target components from Radix bupleuri, accurately identified them and found out their different effects on SH-SY5Y cells.
CONCLUSIONS:
Saikosaponin B1, saikosaponin B2 and saikosaponin C may be as anti-schizophrenic candidate drugs.

A distinct characteristic of the quiescent state of human dermal fibroblasts in contracted collagen gel as revealed by no response to epidermal growth factor alone, but a positive growth response to a combination of the growth factor and saikosaponin b1.[Pubmed: 2084519]

Matrix. 1990 Dec;10(6):412-9.

It is known that fibroblasts cultured in a reconstituted collagen gel contract the gel, resulting in a high density of collagen fibrils comparable to that in dermis. Our previous study indicated that human fibroblasts in the contracted collagen gel did not proliferate in the presence of 10% serum even though there was no apparent cell-cell contact. We interpreted this cell growth inhibition as being caused by a high level of cell-collagen fibril interactions or cell-matrix contact inhibition.
METHODS AND RESULTS:
In the present study, the effect of epidermal growth factor (EGF) on fibroblast proliferation in the contracted collagen gel was compared with that on cells in other quiescent states. Non-dividing cells at confluency on a plastic dish or on collagen gel responded to the added EGF and multiplied, while the cells in the contracted collagen gel did not show any growth response to EGF at concentrations up to 100 ng/ml. Binding assay of [125I]-EGF to the cells showed that the number of binding sites and the binding constant obtained from Scatchard analysis were essentially unchanged in the contracted collagen gel, indicating that EGF receptors were not masked by collagen fibrils but that the signal transduction after binding of EGF was blocked. The block in the signal transduction was suppressed by the addition of Saikosaponin B1.
CONCLUSIONS:
These results suggested that the quiescent fibroblasts in the contracted collagen gel were in a distinct state from previously known quiescent states of cultured cells, namely quiescent states due to cell-cell contact inhibition at confluency or to deficiency of growth factors. The mechanism of the effect of Saikosaponin B1, which has a potent saponin activity, is discussed.

J Sep Sci. 2014 Dec;37(23):3587-94.

Separation of triterpenoid saponins from the root of Bupleurum falcatum by counter current chromatography: the relationship between the partition coefficients and solvent system composition.[Pubmed: 25223791]

Each fraction obtained was collected and dried, which yielded the following five saikosaponins from 700 mg of injected sample: Saikosaponin B1 (8.7 mg), saikosaponin A (86 mg), saikosaponin B3 (17 mg), saikosaponin B2 (41 mg), and saikosaponin C (33 mg). Saikosaponin A showed the most potent cytotoxicity against human cancer cells (gastric cancer, AGS cells; breast cancer, MCF-7 cells; and hepatoma, HepG2 cells) after 24 h. The IC50 values for the above three cell types were 34.6, 33.3, and 23.4 μmol/L, respectively.