Antitumorpharmacological mechanism of the oral liquid of Poriacocos polysaccharide.

ETHNOPHARMACOLOGICAL RELEVANCE: The liquid oral formulation of Poria cocos polysaccharides is composed of polysaccharides of Lentinusedodes, Ganodermalucidum and Poria cocos(1:1:2), which are all fungi used in traditional Chinese medicine. Polysaccharides extracted from these fungi have been reported to exhibit an antitumor effect by modulating the immune system. AIM OF THE STUDY: The present study aimed to clarify the antitumor mechanism of an orally administered liquid containing Poriacocos and to further provide clinical guidance. MATERIALS AND METHODS: In this study, the effects of an orally administered liquid containing Poriacocos polysaccharides on the solid tumors formed from sarcoma 180 cells in mice were evaluated. The protein expression of Bcl-2, caspase-3, and caspase-9in the thymus, spleen and liver tissues in the mice was determined by Western blot analysis. In addition, hematoxylin-eosin（H&E）staining and immunohistochemistry were performed on thymus, spleen and liver tissue and the positive staining rate was calculated for the three protein expression. RESULTS: The liquid oral formulation of Poriacocos polysaccharides reduced Bcl-2 protein levels and increased caspase-3 and -9 protein levels in sarcoma 180 cells. CONCLUSION: The mechanism underlying the antitumor effects of the oral liquid formulation of Poriacocos polysaccharides involved inhibition of Bcl-2 expression and activation of caspase-9 expression in sarcoma 180 cells. Furthermore, the downstream caspase-3 promoter cascade was activated and cell apoptosis was activated in sarcoma 180 cells.

Comparative Study on the Antivirus Activity of Shuang-Huang-Lian Injectable Powder and Its Bioactive Compound Mixture against Human Adenovirus III In Vitro.

Shuang-Huang-Lian injectable powder (SHL)-a classical purified herbal preparation extracted from Scutellaria baicalensis, Lonicera japonica, and Forsythia suspense-has been used against human adenovirus III (HAdV3) for many years. The combination herb and its major bioactive compounds, including chlorogenic acid, baicalin, and forsythia glycosides A, are effective inhibitors of the virus. However, no comprehensive studies are available on the antiviral effects of SHL against HAdV3. Moreover, it remains unclear whether the mixture of chlorogenic acid, baicalin, and forsythia glycosides A (CBF) has enhanced antiviral activity compared with SHL. Therefore, a comparative study was performed to investigate the combination which is promising for further antiviral drug development. To evaluate their antivirus activity in parallel, the combination ratio and dose of CBF were controlled and consistent with SHL. First, the fingerprint and the ratio of CBF in SHL were determined by high performance liquid chromatography. Then, a plaque reduction assay, reverse transcription polymerase chain reaction (PCR), real-time polymerase chain reaction (qPCR), and enzyme-linked immunosorbent assay (ELISA) were used to explore its therapeutic effects on viral infection and replication, respectively. The results showed that SHL and CBF inhibited dose- and time-dependently HAdV3-induced plaque formation in A549 and HEp-2 cells. SHL was more effective than CBF when supplemented prior to and after viral inoculation. SHL prevented viral attachment, internalization, and replication at high concentration and decreased viral levels within and out of cells at non-toxic concentrations in both cell types. Moreover, the expression of tumor necrosis factor alpha (TNF)-α, interleukin (IL)-1ß, and IL-6 was lower and the expression of interferon (IFN)-γ was higher in both cell types treated with SHL than with CBF. In conclusion, SHL is much more effective and slightly less toxic than CBF.

Comparative tissue distribution and excretion study of alkaloids from Herba Ephedrae-Radix Aconiti Lateralis extracts in rats.

Herba Ephedrae-Radix Aconiti Lateralis, composed of Ephedrae (Mahuang in Chinese) and Radix Aconiti Lateralis (Fuzi in Chinese), is a classical herbal combination proven to be effective in treating common cold, asthma, and rheumatoid arthritis. Alkaloids, bioactive components of the herbal extract, have been associated with many side effects. Nine alkaloids, including norephedrine, norpseudoephedrine, ephedrine, pseudoephedrine, methylephedrine, hypaconitine, benzoylaconine, benzoylmesaconine and benzoylhypaconine, were simultaneously quantified within 14.5min, by a validated ultra-performance liquid chromatography-tandem mass spectrometry method in various rat tissues, urine, and feces after oral administration of Mahuang-Fuzi and single-herb extracts. The results indicated that the alkaloids were widely distributed in the heart, liver, spleen, lung, kidney, and brain. Lower bioavailability and higher clearance of some alkaloids were observed for the herbal combination, but hypaconitine showed a longer residence time and lower clearance. Elimination kinetics demonstrated that ephedra and aconitum alkaloids were mainly excreted in urine and feces, respectively. The tissue distribution and excretion of ephedra and aconitum alkaloids are comprehensively reported for the first time for the Mahuang-Fuzi combination. Compared with single-herb extracts, lower extraction efficiencies of alkaloids in vitro were observed which may result in their lower intake. However, the combination showed a prolonged residence time and delayed elimination of aconitum alkaloids, which increases the risk of drug accumulation. The study demonstrated potential risks of intoxication with aconitum alkaloids, associated with the use of Fuzi in combination with Mahuang. Mahuang-Fuzi is a classical combination used in clinics, further investigation is needed.