[Natural 5α-reductase inhibitors in treatment of benign prostatic hyperplasia].

Benign prostatic hyperplasia(BPH) is a common disease of the male urinary system, and its incidence rate in China is increasing. However, the mechanism underlying the pathogenesis of BPH remains unclear. Some studies demonstrated that the incidence of BPH was related to the change in the levels of steroid hormones. Too high content of dihydrotestosterone(DHT) in the body may cause BPH and other related diseases. Testosterone(T) is converted to DHT by 5α-reductase(SRD5A). By inhibiting the activity of this enzyme, the production of DHT can be reduced, and then the incidence of BPH can be lowered. Therefore, it has drawn great attention to screen and discover safer and more effective 5α-reductase inhibitors from natural medicines to treat prostatic hyperplasia without affecting the physiological function of men. This review summarizes the characteristics and tissue distribution of 5α-reductase, the discovery of 5α-reductase inhibitors in traditional Chinese medicine and natural medicines, 5α-reductase inhibitors commonly used in clinical practice and their side effects, as well as the animal models of prostatic hyperplasia and common detection indicators, aiming to provide a reference for more in-depth understanding and research about BPH and development of drugs.

Current Insights into Phytochemistry, Nutritional, and Pharmacological Properties of Prosopis Plants.

Prosopis is a regional cash crop that is widely grown in arid, semiarid, tropical, and subtropical areas. Compared with other legume plants, Prosopis is underutilized and has great potentialities. Prosopis not only is a good source of timber, construction, fencing material, and gum, but also can be applied for food, beverage, feed, and medicine. Prosopis contains numerous phytochemical constituents, including carbohydrates, proteins, fatty acids, minerals, and vitamins, while varieties of phenolic compounds have also been identified from different parts of Prosopis. Flavonoids (especially C-glycosyl flavonoids), tannins, catechin, 4'-O-methyl-gallocatechin, mesquitol, and quercetin O-glycosides are significant phenolic contents in Prosopis. Various extracts of Prosopis displayed a wide range of biological properties, such as antioxidant, antihyperglycemic, antibacterial, anthelmintic, antitumor, and anticancer. Additionally, Prosopis has the potential to be an ideal diet that contains abundant dietary fiber, minerals, galactomannans, and low-fat content. However, the bioactivity and pharmacological properties associated with Prosopis were influenced by the bioavailability of phytochemicals, various antinutritional compounds, and the interactions of protein and phenolic compounds. The bioavailability of Prosopis is mainly affected by phenolic contents, especially catechin. The antinutritional compounds negatively affect the nutritional qualities of Prosopis, which can be prevented by heating. The protein-phenolic compound interactions can help the human body to absorb quercetin from Prosopis. This literature review aimed to provide systematic information on the physical, biochemical, pharmacological, and nutritional properties and potential applications of Prosopis.

Bioaccessibility and bioactivities of phenolic compounds from roasted coffee beans during in vitro digestion and colonic fermentation.

Bioaccessibility and bioactivity of phenolic compounds in coffee beans relate to roasting and digestion process. This study aimed to estimate phenolic content, antioxidant potential, bioaccessibility, and changes in short chain fatty acids (SCFAs) production during in vitro digestion and colonic fermentation of commercial roasted (light, medium and dark) coffee beans. There was no significant difference found among all three different roasting levels. TPC and DPPH were enhanced 15 mg GAE/g and 60 mg TE/g during gastrointestinal digestion, respectively. For colonic fermentation, the highest TPC and FRAP of all coffee beans was found at 2 and 4 h, respectively. The gastric bioaccessibility of most of the phenolic compounds were relatively higher due to thermal phenolic degradation. Total SCFAs production was only up to 0.02 mM because of thermal polysaccharide decomposition. Light roasted beans exhibited relatively higher phenolic bioaccessibility, antioxidant activities and SCFAs production, which would be more beneficial to gut health.

Analysis of chemical constituents and six compounds in Qu-feng-sheng-shi Granules via HPLC-ESI-Q/TOF-MSn and HPLC-UV technique.

Qu-feng-sheng-shi Granules (QFSSG), a common prescription for the treatment of chronic inflammation and allergic rhinitis, is widely used in the clinic as a traditional Chinese medicine. Chemical analysis and quality control studies of this formulation are relatively limited compared with pharmacological studies. In this study, a high-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (HPLC-ESI-Q/TOF-MSn ) was used to identify the components in this prescription. Next, to quantify six major compounds, an HPLC-UV method was developed and validated. The results showed that 53 compounds were identified based on the MSn data, retention time and previous reports, including 17 coumarins, 14 lignans, 10 chromones, nine phenylethanoid glycosides and three other compounds, were identified or tentatively assigned. Contents of six major bioactive compounds (4'-O-ß-glucopyranosyl-5-O-methylvisamminol, Prim-O-glucosylcimifugin, forsythin, magnolin, imperatorin, isoimperatorin) could be determined by HPLC simultaneously. In addition, the potential anti-inflammatory activity of six major compounds was determined too, and we found that four compounds (4'-O-ß-glucopyranosyl-5-O-methylvisamminol, Prim-O-glucosylcimifugin, forsythin, imperatorin) have a potent nitric oxide inhibitory effect. In conclusion, this work provided comprehensive information on the quality control of QFSSG and evaluated the potential biological activity of the main components in QFSSG, which can contribute to understanding and using it more scientifically.

Bi-directional solid fermentation products of Trametes robiniophila Murr with Radix Isatidis inhibit proliferation and metastasis of breast cancer cells.

BACKGROUND: The bi-directional solid fermentation product extract of Trametes robiniophila Murr (Huaier) with Radix Isatidis (TIF) has been shown to have good anti-tumor activity. However, the mechanisms of this activity are still unknown. In the present study, we aimed to investigate its inhibitory effect on both SK-BR-3 and MDA-MB-231 cells, and explore the possible mechanisms of its anti-cancer effect in vitro. METHODS: The experiment comprised a control group, Radix Isatidis group, Huaier group, and TIF group. The cell viability was measured by MTT and the distribution of cell cycle and apoptosis levels were analyzed by flow cytometry. Cell scratch, Transwell, and adhesion assays were used to measure the effects of the test compounds on the migration, invasion, and adhesion capability of SK-BR-3 and MDA-MB-231 cells. The effects of TIF on the mRNA and protein expression related to apoptosis and migration were measured by using semi-quantitative RT-PCR and western blotting. RESULTS: TIF strongly inhibited the cell proliferation of the SK-BR-3 and MDA-MB-231 cells in a time-dependent manner and induced G2/M arrest and apoptosis. Furthermore, TIF significantly inhibited the proliferation, migration, invasion, and adhesion capabilities of SK-BR-3 and MDA-MB-231 cells. Compared with other treatments, the anticancer effect of TIF were stronger in MDA-MB-231 cells. Semi-quantitative RT-PCR suggested that TIF may upregulate the expression of p53 and caspase-3 to inhibit cell proliferation, and downregulate the expression of MMP-9/Snail and MMP-9/MMP-2 to inhibit the migration, invasion, and adhesion capabilities of SK-BR-3 and MDA-MB-231 cells. Western blotting results showed that TIF increased the expression of p53 protein and decreased the expression of MMP-9 protein in SK-BR-3 and MDA-MB-231 cells. CONCLUSION: The results indicated that the bi-directional solid fermentation may enhance the efficacy of Huaier in MDA-MB-231 cells and that TIF may be an effective complementary medicine for cancer treatment.