Antidepressant Mechanism of Kaixinsan and Its Active Compounds Based on Upregulation of Antioxidant Thioredoxin.

Objectives: Kaixinsan (KXS), a traditional Chinese medicine formula, has been demonstrated to be effective in the treatment of depression. The present study applied a network pharmacology approach to dig out the new targets and mechanism of action of KXS and the active compounds in the treatment of depression.

Methods: A network pharmacology approach based on public databases including ADME (absorption, distribution, metabolism, and excretion) evaluation, targets prediction, construction of networks, and molecule docking was used and validated the predicted new antioxidant targets and mechanisms in vitro.

Immunosuppressive activity of a cycloartane triterpene glycoside from Beesia calthaefolia by inhibiting T cell proliferation.

BC-1 is a cycloartane triterpene glycoside isolated from the whole plant of Beesia calthaefolia. Our recent studies proved that BC-1 inhibited proliferation of splenic lymphocyte and phagocytosis of macrophages, and inhibited the increased production of TNF-α and IL-1β. However, it lacks of study about the immunomodulatory effect of BC-1 on purified T lymphocytes.

Triterpenoid Saponin AG8 from stapf. Induces Triple Negative Breast Cancer Cells Apoptosis through Oxidative Stress Pathway.

Triple-negative breast cancers (TNBCs) are associated with poor patient survival because of the absence of estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2) expressions. Our previous studies have shown that the triterpenoid saponin AG8 from stapf. inhibits the proliferation of MDA-MB-231 cells.

Antiangiogenic effects of AG36, a triterpenoid saponin from Ardisia gigantifolia stapf.

AG36 is a triterpenoid saponin from Ardisia gigantifolia stapf. Our recent studies proved that AG36 displayed prominent cytotoxicity against breast cancer cells both in vitro and in vivo. However, whether AG36 has antiangiogenic properties is unknown.

Triterpenoid Saponins from Ardisia gigantifolia and Mechanism on Inhibiting Proliferation of MDA-MB-231 Cells.

Seventeen 13,28-epoxy triterpenoid saponins obtained from Ardisia gigantifolia STAPF. were evaluated their anti-proliferative activities on MCF-7 cells. The structure-activity relationship analysis indicated that CH group at C-30, four saccharide units with L-rhamnose at R6 in the sugar units are crucial for the cytotoxic activity on MCF-7.

Proteomic Analysis of the Antidepressant Effects of Shen-Zhi-Ling in Depressed Patients: Identification of Proteins Associated with Platelet Activation and Lipid Metabolism.

Shen-Zhi-Ling (SZL) is a Chinese medicine formulated from a Kai-Xin-San decoction that is commonly used to treat depression caused by dual deficiencies in the heart and spleen. However, the underlying mechanisms remain unclear. We investigated biological changes in depression patients (DPs) exhibiting antidepressant responses to SZL treatment using proteomic techniques.

AG36 Inhibits Human Breast Cancer Cells Proliferation by Promotion of Apoptosis and .

AG36 is the biotransformation product of triterpenoid saponin from stapf. In this study, the antitumor activity and underlying molecular mechanisms of AG36 against human breast MCF-7, MDA-MB-231, and SK-BR-3 cancer cells were investigated. AG36 inhibited the viability of MCF-7, MDA-MB-231, and SK-BR-3 cells in a dose and time-dependent manner, with an IC of approximately 0.

Cycloartane triterpenes from Beesia calthaefolia and their anticomplement structure-activity relationship study.

Fifteen cycloartane triterpenes were isolated from Beesia calthaefolia and among them one was new cycloartane triterpenoid. The structure of new compound was determined by the application of spectroscopic analyses and chemical methods. The fifteen compounds were evaluated for their anticomplement activity by classic pathway.

[Identification of the metabolites of Dingzhi Xiaowan extract in depressive rat plasma, urine, feces and bile after intragastric administration].

Dingzhi Xiaowan is a widely used traditional Chinese medicine in treating depression, which is a similar formula of Kaixinsan. In this research, a rapid ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS(E)) method was established to analyze the metabolites of Dingzhi Xiaowan in depressive model rat plasma, bile, urine and feces. After we established Chronic unpredictable mild stress (CUMS) model rats and orally administrated Dingzhi Xiaowan, rat plasma, bile, urine and feces samples were collected and prepared.

UPLC-Q-TOF-MS(E) analysis of the constituents of Ding-Zhi-Xiao-Wan, a traditional Chinese antidepressant, in normal and depressive rats.

Ding-Zhi-Xiao-Wan (DZXW) is a traditional Chinese medicine widely used for treating depression. To clarify the bioactive constituents of DZXW, a new rapid ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS(E)) method was established in this study, with the whole extract of the formula separated into multiple components to facilitate the analytical process. In total, 97 compounds were detected and 88 were identified in DZXW.

One new cycloartane triterpene glycoside from Beesia calthaefolia.

One new cycloartane triterpene glycoside (1) was isolated from the whole plant of Beesia calthaefolia. Its structure was elucidated on the basis of extensive spectroscopic data analysis. Its inhibitory effect was measured by the classical pathway of the complement system, and compared with those of known related cycloartane glycosides 2 and 3, previously isolated by us from the same plant.

AG4, a compound isolated from Radix Ardisiae Gigantifoliae, induces apoptosis in human nasopharyngeal cancer CNE cells through intrinsic and extrinsic apoptosis pathways.

3β-O-{α-L-Pyran rhamnose-(1→3)-[β-D-xylopyranose-(1→2)]-β-D-glucopyranose-(1→4)-[β-D-lucopyranose-(1→2)]-α-L-pyran arabinose}-cyclamiretin A (AG4) is a saponin component obtained from the Giantleaf Ardisia Rhizome (Rhizoma Ardisiae Gigantifoliae). The present study aimed to investigate the antitumor potential of AG4 and its possible mechanisms in human nasopharyngeal carcinoma cells (CNE). We exposed tumor cells to AG4 to investigate which cell line was the most sensitive to AG4.

Biotransformation on the triterpenoid saponin of Ardisia gigantifolia by Aspergillus avenaceus AS 3.4454.

Compound 1, a triterpenoid saponin from Ardisia gigantifolia Stapf. showing potential anti-tumor activity, was transformed into three derivatives (2-4) by Aspergillus avenaceus 3.4454.

Two new triterpenoid saponins obtained by microbial hydrolysis with Alternaria alternata AS 3.6872.

Compound 1, a triterpenoid saponin from Ardisia gigantifolia Stapf showing potential anti-tumour activity, was hydrolysed into two deglycosyl derivatives (2 and 3) by Alternaria alternata AS 3.6872. Both these derivatives are new compounds.

Antitumor activity of triterpenoid saponin-rich Adisia gigantifolia extract on human breast adenocarcinoma cells in vitro and in vivo.

The aim of this study was to explore whether the ethanolic extract of Ardisia gigantifolia rhizomes (AGB-5), a traditional herbal medicine from China, could affect the proliferation of human breast adenocarcinoma (MCF-7) cells in vitro and to explore the antitumor effects of AGB-5 in BALB/c mice engrafted with MCF-7 cells. The results showed that AGB-5 markedly inhibited the proliferation of MCF-7 cells with an IC50 value of 11.89±1.

Effect of Tenuifoliside A isolated from Polygala tenuifolia on the ERK and PI3K pathways in C6 glioma cells.

Tenuifoliside A (TFSA) is a bioactive oligosaccharide ester component of Polygala tenuifolia Wild, a traditional Chinese medicine which was used to manage mental disorders effectively. The neuroprotective and anti-apoptotic effects of TFSA have been demonstrated in our previous studies. The present work was designed to study the molecular mechanism of TFSA on promoting the viability of rat glioma cells C6.

Antidepressant and neuroprotective effect of the Chinese herb kaixinsan against lentiviral shRNA knockdown brain-derived neurotrophic factor-induced injury in vitro and in vivo.

Depression has been associated with reduced expression of brain-derived neurotrophic factor (BDNF) in the hippocampus. Previous studies have demonstrated that the herbal medicine formula, 'kaixinsan' (KXS), could ameliorate the severity of depression and increase cAMP response element-binding protein expression. There is direct evidence suggesting that the reduction of the BDNF protein in specific brain sites can provoke depressive-like behaviour or affect neurogenesis in vivo.

Cycloartane-type triterpene glycosides from Beesia calthaefolia and their anticomplement activity.

Two new 9,19-cycloartane triterpenes (1, 2), together with three known compounds (3-5), were isolated from the whole plant of Beesia calthaefolia. Their structures were determined by the application of spectroscopic analyses and chemical methods. Compound 1 showed moderate anticomplement activity similar to that of the positive control (rosmarinic acid), while compounds 3 and 4 showed weak activity.

Effects of (20S*,24R*)-epoxy-9,19-cyclolanstane-3β,12β,16β,25-pentaol-3-O-β-D-xylopyranoside extracted from rhizoma Beesia on immunoregulation and anti-inflammation.

(20S*,24R*)-epoxy-9,19-cyclolanstane-3β,12β,16β,25-pentaol-3-O-β-D-xylopyranoside (BC1) is a kind of natural bioactive substance extracted from Beesia calthaefolia (Maxim.)Ulbr. This study was designed to evaluate the effects of BC1 on the proliferation of lymphocytes, phagocytosis of peritoneal macrophage, and cytokine secretion, such as tumor necrosis factor (TNF)-α and interleukin (IL)-1β, and the foot pad thickness index, which is beneficial for understanding the mechanism of BC1 on immunoregulation and anti-inflammation and also will benefit our further research.

A representative prescription for emotional disease, Ding-Zhi-Xiao-Wan restores 5-HT system deficit through interfering the synthesis and transshipment in chronic mild stress-induced depressive rats.

Ethnopharmacological Relevance: Ding-Zhi-Xiao-Wan (DZ, also known as Kai-Xin-San) is a famous traditional Chinese medicine used for the treatment of emotional disease. Previously, we have found that in a variety of animal models of depression (such as tail suspension model, model of chronic fatigue and forced swimming model) DZ demonstrated significant antidepressant behavior and promoted the production of 5-hydroxytryptamine (5-HT). However, the mechanisms of 5-HT regulation are still unclear.

Cycloartane triterpenes from Beesia calthaefolia (Maxim.).

Three new cycloartane triterpenoids (1-3) and two known compounds (4, 5) were isolated from the whole plant of Beesia calthaefolia. Their structures were elucidated by 1D and 2D NMR, HRESIMS and optical rotation spectral data. All isolates were investigated for their inhibitory effects on the classical pathway of the complement system.

Methanolysis of triterpenoid saponin from Ardisia gigantifolia stapf. and structure-activity relationship study against cancer cells.

Thirteen 13,28-epoxy triterpenoid saponins were isolated from Ardisia gigantifolia stapf. and one potential anti-tumor saponin was methanolysised by H2SO4 to afford four new compounds. The seventeen compounds were evaluated for their anti-proliferative activity on A549, HCT-8 and Bel-7402 cells.

A new triterpenoid saponin from Ardisia gigantifolia.

A new triterpenoid saponin, named 3-O-β-d-glucopyranosyl-(1 → 3)-β-d-xylopyranosyl-(1 → 2)-[α-l-rhamnopyranosyl-(1 → 3)]-β-d-glucopyranosyl-(1 → 4)-[β-d-glucopyranosyl-(1 → 2)]-α-l-arabinopyranosyl-3β,16α,28,30-tetrahydroxy-olean-12-ene (1), along with four known triterpenoids (2-5), was isolated from the rhizomes of Ardisia gigantifolia. Their structures were elucidated by spectroscopic methods. Compounds 1-4 showed cytotoxic activity against Hela, EJ, BCG, and HepG-2 cell lines.

New cycloartane triterpene glycosides from Beesia calthaefolia.

Two new cycloartane triterpene glycosides (compounds 1 and 4) were isolated from the whole plants of Beesia calthaefolia with two known glycosides (compounds 2 and 3). Compounds 1 and 4 were assigned as (20S(*),24R(*))-16β-acetoxy-20, 24-epoxy-9, 19-cyclolanostane-3β,12β,15α,18,25-pentaol-3-O-β-d-xylopyranoside and (20S(*),24 R(*))-16β-acetoxy-20,24-epoxy-9,19-cyclolanostane-3β,15α,18,25-tetraol-3-O-β-d-xylopyranoside, respectively. Their structures were elucidated on the basis of extensive spectroscopic data analyses and comparison with spectroscopic data reported.