Pharmacokinetic characteristics of emodin in polygoni Multiflori Radix Praeparata.

ETHNOPHARMACOLOGICAL RELEVANCE: Polygoni Multiflori Radix Praeparata (Zhiheshouwu) has been a Wudang Taoist medicine for tonifying the liver and kidney, resolving turbidity and reducing lipid. Emodin is one of the active anthraquinones in Zhiheshouwu. Our previous studies showed that emodin (EM) and the other anthraquinones in Zhiheshouwu extract (HSWE) exerted similar inhibitory effects on liver cancer cells in vitro. However, it is still unknown if the other anthraquinones enhance pharmacokinetics (PK) of EM in HSWE in vivo. AIM OF THE STUDY: In this study, we compared the PK characteristics of EM alone with that in Zhiheshouwu aiming to explore which anthraquinones in HSWE contribute to the changed PK of EM in rats. MATERIALS AND METHODS: Quality control of HSWE was determined using high performance liquid chromatography (HPLC). The ratios of emodin to other anthraquinones, physcion (PH), chrysophanol (CH), rhein (RH), aloe-emodin (AE), emodin-8-O-ß-D-glycoside (EMG), physcion-1-O-ß-D-glycoside (PHG) and chrysophanol-8-O-ß-D-glycoside (CHG) in HSWE were determined and analyzed using UPLC combined with tandem mass spectrometry (UPLC/MS). The PK parameters and intestinal tissue concentration of EM alone, EM in HSWE, or with other anthraquinones in SD rats were analyzed using UPLC/MS. RESULTS: The quality of the Zhiheshouwu samples met the quality standard of the Chinese Pharmacopoeia (Version 2020). The PK results showed that compared with EM alone, Cmax (239.90 ± 146.71 vs. 898.46 ± 291.62, P < 0.001), Tmax (0.26 ± 0.15 vs. 12.55 ± 1.33, P < 0.001), AUC0-t (1575.09 ± 570.46 vs. 12154.96 ± 5394.25, P < 0.001), and AUC0-∞ (4742.51 ± 1837.62 vs. 37131.34 ± 21647.39, P < 0.001) of EM in HSWE were decreased due to PH and EMG, while the values of Vd (380.75 ± 217.74 vs. 11.75 ± 7.35, P < 0.001), T1/2 (10.81 ± 1.99 vs. 6.65 ± 2.76, P < 0.05) and CL (19.30 ± 7.82 vs. 2.78 ± 1.88, P < 0.001) of EM in HSWE were increased due to PH and AE. In addition, the intestinal tissue concentration of emodin in HSWE was decreased compared with that of EM alone in 20 and 780 min (25.37 ± 5.98 vs. 43.29 ± 4.16 and 26.72 ± 4.03 vs. 43.40 ± 14.19, respectively. P < 0.05) dominantly due to RH and PH. CONCLUSION: In conclusion, compared with treatment of EM alone, the AUC0-t value of EM in HSWE was decreased with different ways in rats. PH shortened Tmax, and increased Vd and CL. While AE prolonged T1/2 of EM. This indicated that the other anthraquinones in HSWE changed the PK of EM in rats and participated in the complex effects of EM on liver cancer. Besides the other anthraquinones, other components (e.g., 2,3,5,4'-tetrahydroxystilbene-2-O-ß-D-glucoside) in Zhiheshouwu may contribute in the pharmacokinetic and pharmacodynamic interactions with EM for anti-liver cancer.

Quality control, preparation process optimizing and anti-inflammatory effects of Premna Puberula Pamp. Pectin.

Background: Premna Puberula Pamp. Pectin (PP) was a Wudang functional food in China. It has the effect of dispelling fire, clearing heat and detoxification in folk medicine. However, little studies have been reported for their preparation, quality control, effects and toxicity. Methods: The P. Puberula leaves were collected from different pharms and seasons. The compounds in PP were identified using UPLC-Q-TOF-MS/MS. UV-VIS spectrophotometry with phenol-sulfuric acid and sodium nitrite aluminum nitrate were conducted for analyzing the water-soluble sugars and total flavonoids, respectively. L9(34) orthogonal experimental method was used to optimize the preparation process of PP. For the pharmacological effects of PP, the swelling right hind paw of ICR mice was modeled using subcutaneous injection of carrageenan gum solution, and the local tissue inflammatory reactions of the model mice were investigated using vernier calipers and HE staining. The serum inflammatory factor expression was detected using ELISA. The acute toxicity experiments were carried out for safety assessment of PP in ICR mice. Results: Fifty-three compounds were initially identified in PP among which flavonoids were dominant (19 out of 53). The average values of water-soluble sugar content and total flavonoid content of PP were 13.366 and 4.970 mg/g, respectively. The best preparation process of PP was powder-liquid ratio 1: 20, temperature 90 °C, and stirring time 3 min. Data showed that PP reduced paw edema and decrease the serum level of IL-6, TNF-α and IL-1ß in the model mice. There was no toxic effect of PP on mice at a total dose of 6000 mg/kg/24h. Conclusion: In summary, by optimizing the preparation process, PP with stable quality can be obtained. PP has anti-inflammatory effects without toxicity.

Mg-Fe-Al-O spinel: Preparation and application as a heterogeneous photo-Fenton catalyst for degrading Rhodamine B.

It is an urgent need to develop new environmentally friendly spinel ferrites with high catalytic efficiency. In this work, a series of Mg-Fe-Al-O spinels with different ratios of Mg/Al were successfully synthesized by the reaction sintering method and were used as a heterogeneous photo-Fenton catalyst for degradation of Rhodamine B (RhB). The effect of different ratios of Mg/Al on the properties of Mg-Fe-Al-O spinel was characterized and analyzed through a range of advanced characterization techniques and DFT calculations. The influence factors on the photo-Fenton reaction catalyzed by Mg-Fe-Al-O spinels were systematically investigated. The results showed that the prepared Mg-Fe-Al-O spinels had larger lattice parameters, wider bandgap, and stronger magnetism, with the Mg content increased. Among them, Mg-9 (Mg0.88Fe1.88Al0.23O4) had the best catalytic performance in the photo-Fenton reaction. The degradation efficiency of RhB reached 98.45%, and the TOC removal efficiency was 83.47%. The elemental valence and PDOS of Mg-9 (Mg0.88Fe1.88Al0.23O4) spinels were closer to MgFe2O4. The photo-generated holes could directly oxidize water and hydroxyl to generate reactive oxygen species ·OH, improving the catalytic activity.

[Characteristics and treatment outcomes in 822 adult patients with acute myeloid leukemia:a single center experience].

OBJECTIVE: To investigate the characteristics and the short- or long-term treatment outcomes of the adult patients with acute myeloid leukemia (AML) in China. METHODS: From 1999 to 2010, 822 adult cases with AML were enrolled, diagnosed and classified by the FAB and WHO criteria, respectively. The treatment outcomes and prognostic factors were analyzed retrospectively. RESULTS: In all patients with a median age of 38.5(15-83) years, acute monoblastic and monocytic leukemia (M5), AML with t(15;17)/PML-RARα (APL) and AML with t(8;21)/AML1-ETO(M2b) were the most common subtypes, accounting for 29.7%, 20.9% and 14.6% respectively. In APL patients, CR was achieved in 95.2%, with an early death (ED) rate of 4.8%. And the estimated overall survival (OS) and disease-free survival (DFS) at 5 year was 87.5% and 88.8%, respectively. Patients with other AML subtype (Non-APL) revealed a CR rate of 82.0%, ED of 4.3%, and estimated 5-year OS and DFS both of 48.8%. The OS rate of Non-APL patients at 3-year varied significantly (P<0.01) among three prognostic groups by cytogenetic risk stratification:favorable, 69.5%; intermediate, 52.8%; unfavorable, 29.8%. The prognostic factors for OS among Non-APL included age, cytogenetic abnormalities, courses of the median/high-dose cytarabine and allogeneic hematopoietic stem cell transplantation. CONCLUSION: When compared with the previous reports, the AML patients in our study were younger and showed a different subtype distribution. Treatment outcomes of APL and Non-APL were just the same as those in international leukemia centers. Chemotherapy by risk stratification, after diagnosis and classification according to the WHO criteria, is a key point to improve the outcomes in AML.

[Sorafenib in combination with chemotherapy in the induction therapy for FLT3-ITD positive acute monocytic leukemia: a case report and literature review].

OBJECTIVE: To explore the safety and efficacy of sorafenib in combination with chemotherapy for the treatment of FLT3 positive acute myeloid leukemia (AML), to highlight the impact of FLT3 mutations and targeting therapy on response of AML. METHODS: The clinical and laboratory features and the treatment response, especially the safety profile of sorafenib in an acute monocytic leukemia patient with FLT-ITD were reported. RESULTS: The patient achieved clinical and molecular CR after sorafenib was added to the second course of combination chemotherapy. The side effects of sorafenib were mild and tolerable. CONCLUSION: The patient responded well to the combination of sorafenib and standard chemotherapy of AML without significant adverse effects.