Cancer: Leukemia, sarcoma
Action: Antibiotic, anti-apoptotic, anti-inflammatory, neuro-protective, pro-apoptotic, immunomodulating, MMPs regulation
Anti-inflammatory and Immunomodulating
Qingkailing and Shuanghuanglian (SHHL) are two commonly used Chinese herbal preparations with reported anti-inflammatory activity. The effects of these two preparations on the capacity of staphylococcal toxic shock syndrome toxin 1 (TSST-1), to stimulate the production of cytokines (IL-1β, IL-6, TNF-α, IFN-γ) and chemokines (MIP-1α, MIP-1β and MCP-1) by peripheral blood mononuclear cell (PBMC), was tested. Their effect on LPS-stimulated NF-κB transcriptional activity in a THP-1 cell line, and on human monocyte chemotactic response to chemoattractants, was also evaluated.
The results suggested that the pharmacological basis for the anti-inflammatory effects of Qingkailing and SHHL is the result of suppression of NF-κB regulated gene transcription, leading to suppressed production of pro-inflammatory cytokines and chemokines. Interference with leukocyte chemotaxis also contributes to the anti-inflammatory and immunomodulating effects of these medicinals. Identification of the responsible components in these two herbal preparations may yield compounds suitable for structural modification into potent novel drugs (Chen et al., 2002).
Leukemia
The MTT assay, cell morphology, DNA gel electrophoresis, and flow-cytometry were utilized to study the apoptotic effect of Qingkailing, and its active compounds, on the human acute promyelocytic leukemia (HL-60) cell line.
Qingkailing and its active compounds, Baicalin and hyodeoxycholic acid, exhibited strong cytotoxicity in inhibiting HL-60 cells, while Bezoar cholic acid showed a weaker effect. Apoptosis could be induced after being treated for 6 h by the former two compounds, displaying a typical apoptosis peak under flow-cytometry, but could not be induced by the latter.
Qingkailing could induce apoptosis in leukemia cells in vitro, which could serve as a mechanism of Qingkailing in the treatment of acute promyelocytic leukemia (Chen, Dong, & Zhang, 2001).
Qingkailing injection could prevent the decrease of MMP induced by injury of hypoxia-hypoglycemia-reoxygenation, stabilize MMP, inhibit cell apoptosis, and protect hippocampal neurons (Tsing, 2006).
Matrix Metalloproteinases (MMPs) Regulation
Matrix metalloproteinases (MMPs) play vital roles in many pathological conditions, including cancer, cardiovascular disease, arthritis and inflammation. Modulating MMP activity may therefore be a useful therapeutic approach in treating these diseases. Qingkailing is a popular Chinese anti-inflammatory formulation used to treat symptoms such as rheumatoid arthritis, acute hypertensive cerebral hemorrhage, hepatitis and upper respiratory tract infection.
One of the components of Qingkailing, Fructus gardeniae, strongly inhibits MMP activity. The IC50 values for the primary herbal extract and water extract against MMP-16 were 32 and 27 µg/ml, respectively. In addition, the herbal extracts influenced HT1080 human fibrosarcoma cell growth and morphology.
These data may provide molecular mechanisms for the therapeutic effects of Qingkailing and herbal medicinal Fructus gardenia (Yang et al., 2008).
Sources