Evaluation of disease severity and prediction of severe cases in children hospitalized with influenza A (H1N1) infection during the post-COVID-19 era: a multicenter retrospective study.

BACKGROUND: The rebound of influenza A (H1N1) infection in post-COVID-19 era recently attracted enormous attention due the rapidly increased number of pediatric hospitalizations and the changed characteristics compared to classical H1N1 infection in pre-COVID-19 era. This study aimed to evaluate the clinical characteristics and severity of children hospitalized with H1N1 infection during post-COVID-19 period, and to construct a novel prediction model for severe H1N1 infection. METHODS: A total of 757 pediatric H1N1 inpatients from nine tertiary public hospitals in Yunnan and Shanghai, China, were retrospectively included, of which 431 patients diagnosed between February 2023 and July 2023 were divided into post-COVID-19 group, while the remaining 326 patients diagnosed between November 2018 and April 2019 were divided into pre-COVID-19 group. A 1:1 propensity-score matching (PSM) was adopted to balance demographic differences between pre- and post-COVID-19 groups, and then compared the severity across these two groups based on clinical and laboratory indicators. Additionally, a subgroup analysis in the original post-COVID-19 group (without PSM) was performed to investigate the independent risk factors for severe H1N1 infection in post-COIVD-19 era. Specifically, Least Absolute Shrinkage and Selection Operator (LASSO) regression was applied to select candidate predictors, and logistic regression was used to further identify independent risk factors, thus establishing a prediction model. Receiver operating characteristic (ROC) curve and calibration curve were utilized to assess discriminative capability and accuracy of the model, while decision curve analysis (DCA) was used to determine the clinical usefulness of the model. RESULTS: After PSM, the post-COVID-19 group showed longer fever duration, higher fever peak, more frequent cough and seizures, as well as higher levels of C-reactive protein (CRP), interleukin 6 (IL-6), IL-10, creatine kinase-MB (CK-MB) and fibrinogen, higher mechanical ventilation rate, longer length of hospital stay (LOS), as well as higher proportion of severe H1N1 infection (all P < 0.05), compared to the pre-COVID-19 group. Moreover, age, BMI, fever duration, leucocyte count, lymphocyte proportion, proportion of CD3+ T cells, tumor necrosis factor α (TNF-α), and IL-10 were confirmed to be independently associated with severe H1N1 infection in post-COVID-19 era. A prediction model integrating these above eight variables was established, and this model had good discrimination, accuracy, and clinical practicability. CONCLUSIONS: Pediatric H1N1 infection during post-COVID-19 era showed a higher overall disease severity than the classical H1N1 infection in pre-COVID-19 period. Meanwhile, cough and seizures were more prominent in children with H1N1 infection during post-COVID-19 era. Clinicians should be aware of these changes in such patients in clinical work. Furthermore, a simple and practical prediction model was constructed and internally validated here, which showed a good performance for predicting severe H1N1 infection in post-COVID-19 era.

Qingfei Tongluo Mixture Attenuates Bleomycin-Induced Pulmonary Inflammation and Fibrosis through mTOR-Dependent Autophagy in Rats.

As an interstitial fibrosis disease characterized by diffuse alveolitis and structural alveolar disorders, idiopathic pulmonary fibrosis (IPF) has high lethality but lacks limited therapeutic drugs. A hospital preparation used for the treatment of viral pneumonia, Qingfei Tongluo mixture (QFTL), is rumored to have protective effects against inflammatory and respiratory disease. This study aims to confirm whether it has a therapeutic effect on bleomycin-induced IPF in rats and to elucidate its mechanism of action. Male SD rats were randomly divided into the following groups: control, model, CQ + QFTL (84 mg/kg chloroquine (CQ) + 3.64 g/kg QFTL), QFTL-L, M, H (3.64, 7.28, and 14.56 g/kg, respectively) and pirfenidone (PFD 420 mg/kg). After induction modeling and drug intervention, blood samples and lung tissue were collected for further detection. Body weight and lung coefficient were examined, combined with hematoxylin and eosin (H&E) and Masson staining to observe lung tissue lesions. The enzyme-linked immunosorbent assay (ELISA) and the hydroxyproline (HYP) assay kit were used to detect changes in proinflammatory factors (transforming growth factor-ß (TGF-ß), tumor necrosis factor-α (TNF-α), and interleukin-1ß (IL-1ß)) and HYP. Immunohistochemistry and Western blotting were performed to observe changes in proteins related to pulmonary fibrosis (α-smooth muscle actin (α-SMA) and matrix metalloproteinase 12 (MMP12)) and autophagy (P62 and mechanistic target of rapamycin (mTOR)). Treatment with QFTL significantly improved the adverse effects of bleomycin on body weight, lung coefficient, and pathological changes. Then, QFTL reduced bleomycin-induced increases in proinflammatory mediators and HYP. The expression changes of pulmonary fibrosis and autophagy marker proteins are attenuated by QFTL. Furthermore, the autophagy inhibitor CQ significantly reversed the downward trend in HYP levels and α-SMA protein expression, which QFTL improved in BLM-induced pulmonary fibrosis rats. In conclusion, QFTL could effectively attenuate bleomycin-induced inflammation and pulmonary fibrosis through mTOR-dependent autophagy in rats. Therefore, QFTL has the potential to be an alternative treatment for IPF in clinical practice.

Anti-hypertensive and composition as well as pharmacokinetics and tissues distribution of active ingredients from Alpinia zerumbet.

Alpinia zerumbet is a food flavor additive and a traditional medicine herb around the world. Several studies have reported that A. zerumbet has excellent effects on a variety of cardiovascular diseases, but its potential hypertensive applications, and pharmacokinetic features of main active substances have not been fully investigated. The mechanism of anti-hypertension with ethyl acetate extracts of A. zerumbet fruits (AZEAE) was evaluated by L-NNA-induced hypertensive rats and L-NAME-injured human umbilical vein endothelial cells (HUVECs). Blood pressure, echocardiographic cardiac index and H&E staining were used to preliminary evaluate the antihypertensive effect of AZEAE, the levels of TNF-α, IL-6, and IL-1ß were evaluated by ELISA, and the proteins expression of IL-1ß, IL-18, AGTR1, VCAM, iNOS, EDN1 and eNOS were also evaluated. In addition, isolation, identification, and activity screening of bioactive compounds were carried ou. Next, pharmacokinetics and tissues distribution of dihydro-5,6-dehydrokavain (DDK) in vivo were measured, and preliminary absorption mechanism was conducted with Caco-2 cell monolayers. AZEAE remarkably enhanced the state of hypertensive rats. Twelve compounds were isolated and identified, and five compounds were isolated from this plant for the first time. The isolated compounds also exhibited good resistance against injury of HUVECs. Moreover, pharmacokinetics and Caco-2 cell monolayers demonstrated AZEAE had better absorption capacity than DDK, and DDK exhibited differences in tissues distribution and gender difference. This study was the first to assess the potential hypertensive applications of A. zerumbet in vivo and vitro, and the first direct and concise study of the in vivo behavior of DDK and AZEAE.

Evaluation of febrile seizures in children infected with SARS-CoV-2 Omicron variant in Yunnan, China: a multi-center, retrospective observational study.

Background: The SARS-CoV-2 Omicron variant was reported to be linked to febrile seizures (FSs), but studies on FSs in children with Omicron infection remain relatively scarce, especially in the Chinese population. This study aimed to investigate the characteristics of children diagnosed with Omicron infection with FSs in Yunnan, China, and evaluate the potential association between FSs and Omicron infection. Methods: This study was conducted at four hospitals in Yunnan from December 8, 2022, to January 8, 2023, and consisted of 590 pediatric subjects. According to clinical characteristics, 85, 129 and 376 subjects were divided into the FS-only, Omicron-FS, and Omicron-only groups, respectively. Demographic, clinical and laboratory data were retrospectively collected for analysis. Results: The incidence of FSs in children with Omicron infection was 25.5% (129/505). Older age, stronger male predominance, as well as lower proportions of prior history and family history of seizures were observed in Omicron-FS and Omicron-only groups than in FS-only group, but there were no differences in these four above-mentioned events between these two Omicron-related groups. Compared to FS-only group, Omicron-FS group also had a shorter fever-to-seizure onset duration and more frequent seizures during a single course of fever. Moreover, higher levels of IL-6, TNF-α and ferritin as well as decreased counts of leukocytes and lymphocytes were confirmed in Omicron-FS group than in FS-only and Omicron-only groups. Regarding COVID-19 vaccination status, Omicron-FS group revealed a higher proportion of unvaccinated children and a lower proportion of three-dose vaccination than Omicron-only group. As for clinical outcomes, proportions of mechanical ventilation and intensive care unit admission observed in the two Omicron-related groups were notably higher than those in FS-only group. Meanwhile, Omicron-FS group showed the longest length of hospital stay, followed by Omicron-only group and FS-only group, in order. Finally, all patients but one who died of fulminant myocarditis had been successfully discharged. Conclusions: The incidence of FSs in children with Omicron infection was 25.5% in Yunnan. FSs might be a clinical sign deserving more attention in children with Omicron infection. Furthermore, COVID-19 vaccination is likely to provide effective protection against Omicron-related FSs in children.

Optimization of Extraction and Separation Process of Notoginsenoside Fc from Panax notoginseng Leaves.

Response surface methodology (RSM) was used to determine the optimal conditions for ultrasound-assisted extraction (UAE) of Notoginsenoside Fc (Fc) from panax notoginseng leaves. The experiment utilized a Box-Behnken design (BBD) and separation conditions were optimized. The optimum extraction conditions were as follows: extraction time = 1.5 h, ethanol concentration = 86%, liquid-to-solid ratio = 19:1. The experimentally obtained values were in accordance with the values predicted by the RSM model. We determined that the RSM model was able to successfully simulate the optimal extraction of Fc from the leaves. Further, Fc was enriched from Panax notoginseng through nine macroporous resins, and HPD-100 macroporous resins were selected for preliminary enrichment of Fc due to its economic costs and benefits. Subsequently, octadecyl silane (ODS) column chromatography was used to improve the purity of Fc to over 90% after separation by ODS column chromatography. Fc with a purity greater than 95% can be obtained by recrystallization. This is the first study that has focused on the extraction and enrichment of Fc from Panax notoginseng leaves using macroporous resin combined with ODS column chromatography, which provides the possibility for further application of Fc.

Bioactive substances inhibiting COX-2 and cancer cells isolated from the fibrous roots of Alangium chinense (Lour.) Harms.

Alangium chinense has been used as a traditional folk medicine for centuries to treat rheumatism, skin diseases, and diabetes by the people of Southeast Asia. However, the bioactive constituents inhibiting COX-2 and cancer cells (HepG2, Caco-2, HeLa) remain unclear. In this study one new (14) along with twenty-four known compounds (1-13, 15-25) were isolated from the fibrous roots of Alangium chinense by chromatographic methods, and identified by NMR, and Gaussian and CD calculation. Compounds 1, 2, 13, 16, 17, 19, 20, 23, and 24 were isolated from this plant for the first time. Their inhibition effects on COX-2 enzyme and cancer cells were evaluated by MTT assay. Compounds 1-4, 13-14, and 16-18 can be used as good inhibitors against COX-2 enzyme, and compounds 1, 13, 14, and 17 were stronger than the positive control (celecoxib). In addition, molecular docking suggested that compounds 13, 17, and 18 belong to ellagic acids and have good inhibition against COX-2 enzyme. While compounds 1, 5, 13 and 21 showed cytotoxicity against HepG2 cells, compounds 2 and 21 showed cytotoxicity against Caco-2 cells, and compound 20 showed cytotoxicity against HeLa cells.

Terpenoids as anti-inflammatory substances inhibiting COX-2 isolated from the fibrous roots of Alangium chinense (Lour.) Harms.

A new sesquiterpene, 1-carbonyl-2,8-dihydroxy-11-oxabicyclo [4,4,1] germacra- 2(3),4(5),6(7),8(9)-tetraene (1) and four known compounds (3E, 23E)-3-caffeoyl-23-coumaroylhederagenin (2), (3E, 23E)-dicoumaroylhederagenin (3), morettinone (4), 24-ehylcholesta-3,6-dione (5) were isolated from the ethyl acetate layer of the fibrous root of Alangium chinense (Lour.) Harms. The structure of compound 1 was characterized by its 1H-NMR, 13C-NMR, DEPT, HMBC, HSQC spectrums, and the structures of the known compounds were determined by comparison of their spectroscopic data with those reported by the literatures. The obtained compounds were evaluated for their anti-inflammatory against cyclooxygenase (COX-2). Compound 1 has a good inhibitory effect against COX-2 with IC50 20.43 ± 4.72 µM. The compounds 2-5 have inhibitory effect against COX-2 with IC50 49.19 ± 0.76, 23.29 ± 0.99, 47.78 ± 1.33, and 44.44 ± 0.12 µM, respectively.

Synergistic effect of poly(ionic liquid) and phosphoramide on flame retardancy and crystallization of poly(lactic acid).

Crystallinity and flame retardancy are two key properties for poly(lactic acid)(PLA) in applications. In this paper, a quaternary phosphonium salt poly(ionic liquid) (PIL) and a phosphamide (POFA) were prepared. The PIL, POFA and their blend were used to regulate the flame retardancy and crystallization behaviors of PLA using the limiting oxygen index, UL-94 vertical burning, and thermogravimetric analysis, and differential scanning calorimetry etc. The results showed that a synergistic effect exists between PIL and POFA on flame retardancy. When 6 wt% PIL/POFA (2/1) was added into PLA, its LOI value is 28.0 vol%, and achieves the UL-94 V-0 rating while the PLA composites containing 6 wt% PIL or POFA just achieve the UL-94 V2. The PIL/POFA improves the flame retardancy of PLA by melting-away mode. In addition, the crystallization rate of PLA containing PIL/POFA is faster than that of PLA/PIL and PLA/POFA. The degradation of PLA induced by PIL/POFA produces some small molecular oligomers, which enhances the molecular chain mobility and rearrangement, thus contributes to better flame retardancy and faster crystallization.

Interfacial silicon­nitrogen aerogel raise flame retardancy of bamboo fiber reinforced polylactic acid composites.

A triazine derivative containing nitrogen and silicon (SiN) was synthesized and the SiN hybrid aerogel was covered on the surface of bamboo fiber (BF). The modified BF was identified as MBF. The MBF and ammonium polyphosphate (APP) were used to regulate the flame retardancy and mechanical properties of polylactic acid (PLA). The PLA/BF composites were investigated using limiting oxygen index (LOI), UL-94 vertical combustion, cone calorimetry, thermogravimetric analysis linked with infrared spectra (TG-IR) etc. The char residue of MBF at 800 °C is as high as 43.5 % which is 200 % more than that of BF. Incorporating 9 wt% APP generates a PLA9 which displays the UL-94 V2 rating and a LOI value of 28.0 vol%. PLA9/MBF composites display the UL-94 V0 rating and increased LOI values while PLA9/BF composites obtain the UL-94 V2 rating and decreased LOI. The MBF reduces the release of flammable gases during combustion, enhances charring ability and decreases the thermal conductivity of composites. Besides, the tensile and impact strength of PLA9/20MBF is 20 % and 37 % more than that of PLA9/20BF due to stronger interfacial adhesion. This work provides a good method to regulate the flame retardancy and mechanical properties of PLA/BF composites.

Roles of phosphoramide derivatives in flame retardancy, thermal degradation and crystallization behaviors of polylactic acid.

Two kinds of phosphoramide derivatives containing one (POFA) or two (BPOFA) phosphoramide bonds were synthesized using diphenylphosphinic chloride, phenylphosphonic dichloride and furfurylamine, respectively. The flame retardancy, thermal degradation and crystallization behaviors of polylactic acid (PLA)/POFA and PLA/BPOFA blends were investigated using the limiting oxygen index (LOI), UL-94 vertical burning tests, cone calorimeter tests, thermogravimetric analysis and differential scanning calorimetry. A small amount of 1.0 wt% BPOFA increases the LOI of PLA from 20.4 vol% to 28.0 vol% and achieves the UL-94 V0 rating, while 7.0 wt% POFA is needed to achieve the UL-94 V0 rating indicating that the PLA/BPOFA has better flame retardancy than that of PLA/POFA. Both POFA and BPOFA decrease the amount of flammable gaseous compounds and play positive roles in transesterification of PLA. More importantly, BPOFA is easier to catalyze the degradation of PLA and improve UL-94 rating by melting-away mode. Moreover, the BPOFA accelerates the crystallization rate and thus improves the crystallinity of PLA, while POFA does not show a positive effect on crystallization behaviors of PLA.

Introduction of cation vacancies and iron doping into TiO2 enabling efficient uranium photoreduction.

The reduction of U(VI) to U(IV) in wastewater by semiconductor photocatalysis has become a new highly efficient and low-cost method for U(VI) removal. However, due to the weak absorption of visible light led by wide band gap and low carrier utilization rate resulted from the severe electron-holes recombination, the photoreduction performance of U(VI) is limited. Herein, the Ti vacancies and doped Fe atoms were simultaneously introduced into TiO2 nanosheet (labeled as 4%Fe-Ti1-xO2) as a highly active and stable catalysis for U(VI) photoreduction. Without adding any hole sacrifice agent, 4%Fe-Ti1-xO2 nanosheets achieved 99.7% removal efficiency for U(VI) within 120 min. And the 92.1% removal efficiency of U(VI) via 4%Fe-Ti1-xO2 nanosheets was still maintained after 5 cycles. Moreover, 4%Fe-Ti1-xO2 exhibited dramatic removal rate, 81.6% U(VI) in the solution was removed in 10 min. Further study on the mechanism showed that simultaneously introducing the Ti vacancies and doped Fe atoms in 4%Fe-Ti1-xO2 nanosheets improved the visible light utilization and decreased the recombination of photogenerated electron-hole pairs, contributing to the highly efficiency removal of U(VI).

Fabrication and Mechanism Study of Cerium-Based P, N-Containing Complexes for Reducing Fire Hazards of Polycarbonate with Superior Thermostability and Toughness.

A superior comprehensive performance is essential for the extensive utilization of polymers. Current flame-retardant strategies for polycarbonates (PCs) usually realize satisfied fire resistance at the cost of thermostability, toughness, and/or mechanical robustness. Thus, we report a rare-earth-based P, N-containing complex with a lamellar aggregated structure [Ce(DPA)3] by a coordination reaction between a tailored ligand and cerium(III) nitrate. The results indicate that incorporating 3 wt % Ce(DPA)3 enables the resultant PC composite to achieve UL-94 V-0 rating, with a 55% reduction in the peak heat release rate. Besides, the initial (T5) and maximum (Tmax1 and Tmax2) decomposition temperatures are significantly increased by 21, 19, and 27 °C, respectively, in an air atmosphere. Moreover, the impact strength and elongation at break of the PC composite containing 3 wt % Ce(DPA)3 are greatly increased by 20 and 59%, respectively, relative to pristine PC, while its tensile strength (57 MPa) is still close to that of bulk PC (60 MPa). Notably, this work provides a novel methodology for revealing the evolution mechanisms of chemical structures of vapor and residual products during thermal decomposition, which is conducive to guiding fire and heat resistance modification of PC in the future.

Multiple Roles of Black Raspberry Anthocyanins Protecting against Alcoholic Liver Disease.

This study aimed to investigate the protective effect of black raspberry anthocyanins (BRAs) against acute and subacute alcoholic liver disease (ALD). Network analysis and docking study were carried out to understand the potential mechanism. Thereafter, the serum biochemical parameters and liver indexes were measured, the histopathological changes of the liver were analyzed in vivo. The results showed that all tested parameters were ameliorated after the administration of BRAs with alcohol. Meanwhile, there was increased protein expression of NF-κB and TGF-ß in extracted livers, which was associated with hepatitis and hepatic fibrosis. Furthermore, BRAs and cyanidin-3-O-rutinoside exhibited cytotoxic effects on t-HSC/Cl-6, HepG2, and Hep3B and induced the apoptosis of HepG2 cells; downregulated the protein expression level of Bcl-2; upregulated the level of Bax; and promoted the release of cytochrome C, cleaved caspase-9, cleaved caspase-3, and cleaved PARP in HepG2 cells. In addition, the antioxidant activity of BRAs was tested, and the chemical components were analyzed by FT-ICR MS. The results proved that BRAs exert preventive effect on ALD through the antioxidant and apoptosis pathways.

Investigation of Anti-Fatigue Effect and Simultaneous Determination of Eight Nucleosides in Different Parts of Velvet Antler in Red Deer and Sika Deer.

Velvet antler (VA) is crucial and precious nourishment in China and some countries in Southeast Asia and has excellent anti-fatigue effect. The incidence of fatigue syndrome has increased gradually. VA can be a potential source of anti-fatigue products. Therefore, we investigated the anti-fatigue activity of different sections (upper, middle, and basal section) of VA from different species (red deer and sika deer) via loading swimming test in mice. Furthermore, nucleosides are one kind of active components in VA which could considerably reduce fatigue in mice. In order to explore whether the nucleosides are correlated with anti-fatigue effect, the contents of eight nucleosides (uracil, cytidine, hypoxanthine, xanthine, thymine, inosine, guanosine, and adenosine) were determined simultaneously using high-performance liquid chromatography. The results indicated that the swimming time in mice was increased from basal to upper section, which was consistent with the change trend of the total contents of eight nucleosides of VA. Therefore, we speculated that the contents of nucleosides in VA may affect its anti-fatigue effect. Furthermore, the contents of nucleosides were also used as a reference for evaluating the quality of different parts of VA obtained from red and sika deer.

Enrichment of total flavones and licochalcone A from licorice residues and its hypoglycemic activity.

Industrial processing of glycyrrhizic leads to a lot of residues which are usually threw away randomly or used as feed. Therefore, the purpose of this study was to study licorice residues as a source of bioactive compounds with potentially applications. In this study, the enrichment and purification of total flavones from the licorice residues was achieved by using macroporous resins. The performances and separation characteristics of four selected macroporous resins with different chemical and physical properties were investigated. HPD-100 resin was the most effective, the content of total flavones increased from 50.94% in the original extract to 82.98% in the 80% ethanol fraction (a 1.63-fold increase). Further purification treatment by polyamide resin, licochalcone A with a purity of 80.28% was obtained in a 45% ethanol fraction, and a higher purity (>85%) of licochalcone A can be obtained by single crystallization operation. And hypoglycemic effect of the total flavones from licorice residues on high fat diet and STZ induced diabetic c57 mice was preliminary investigated. The results showed: the fasting blood glucose of mice in the low and medium dose total flavones group decreased significantly. The proposed technique is uncomplicated, easily managed, cost-effective, and environmentally friendly and is proper for both large-scale licorice residues application and waste management.

Identification of Anthocyanins from Four Kinds of Berries and Their Inhibition Activity to α-Glycosidase and Protein Tyrosine Phosphatase 1B by HPLC-FT-ICR MS/MS.

The polyphenolic profiles of four berries (blueberry, bilberry, mulberry, and cranberry) in China were investigated using Fourier transform-ion cyclotron resonance mass spectrometry (FT-ICR MS). Thirty-nine polyphenols including 26 anthocyanins, 9 flavonoids, and 4 phenolic acids were identified accurately. Cyanidin aglycones are common in four berries, and malvidin aglycones are the main compounds found in bilberry and cranberry. The anthocyanin level in blueberry are the highest with 739.6 ± 17.14 mg/g DW and presented the strongest antioxidant capacity in DPPH, ABTS, FRAP, and ORAC assay. In α-glycosidase, the inhibition activity was in the following order: mulberry > bilberry > blueberry > cranberry. For the PTP1B inhibition assay, blueberry demonstrated the highest inhibitory effect with IC50 3.06 ± 0.02 µg/mL, followed by bilberry, mulberry, and cranberry. Molecular docking results showed that cyanidin aglycones had the highest inhibition activity to PTP1B.

Depside derivatives with anti-hepatic fibrosis and anti-diabetic activities from Impatiens balsamina L. flowers.

Eighteen compounds (1-18), seven new (3-9) and eleven previously reported (1, 2, and 10-18), were isolated from the flowers of Impatiens balsamina (Linn). The structures of the isolated compounds were elucidated using different spectroscopic methods, including NMR (1D and 2D), UV, IR, and HR-ESI-MS. Analysis of the bioassay results showed the compounds had notable anti-hepatic fibrosis activity against murine Hepatic Stellate Cells (t-HSC/Cl-6) and anti-diabetics activity against α-glucosidase. Specifically, new compounds 7, 8, 9 showed significant inhibitory activity on t-HSC/Cl-6 cells with IC50 values of 42.12, 109.2, and 34.04 µg/mL respectively, while the IC50 values of positive control Silymarin and Fufang Biejia Ruangan Pian were 202.34 and 231.56 µg/mL, respectively. In addition, compounds 2, 4, 7, 8, 10, 11, 17, and 18 exhibited excellent α-glucosidase inhibitory activity. Among these compounds, 7 exhibited the highest activity with an IC50 value of 0.72 µg/mL, while the IC50 value of the positive control acarbose was 3.36 µg/mL. This is the first study evaluating the anti-hepatic fibrosis and anti-diabetic activities of compounds isolated from the flowers of I. balsamina.

Dammarane triterpenoids for pharmaceutical use: a patent review (2005 - 2014).

INTRODUCTION: Dammarane triterpenoids, the main secondary metabolites of Panax ginseng, are very important natural compounds with remarkable biological activity. They could be isolated from the plants of Panax or other genus, as well as through the modifications of certain natural products. This review is a collection of a number of patents (2005 - 2014) that describe the dammarane triterpenoids for therapeutic or preventive uses on numerous common diseases. AREAS COVERED: In this review, patents from 2005 to 2014 on chemical structures and treatment of different diseases by dammarane triterpenoids have been summarized. The SciFinder and the World Intellectual Property Organisation databases have been used as main sources for the search. EXPERT OPINION: In the last decade, over 90 patents concerning dammarane derivatives for pharmaceutical have been published. These types of compounds could be used as agents for prevention and treatment of various kinds of diseases, such as cancer, diabetes mellitus and metabolic syndrome, hyperlipidemia, cardiovascular and cerebrovascular disease, aging, neurodegenerative disease, bone disease, liver disease, kidney disease, gastrointestinal disease, depression-type mental illness and skin aging. Rare plants, except for Panax genus, which contain dammarane triterpenoids should be studied extensively. In addition, more dammarane triterpenoids with good biological activity, especially the aglycones possessing novel side chain, should be prepared using chemical modification. Finally, pharmacological effects of dammarane triterpenoids should be further studied.

In vitro metabolism of 20(R)-25-methoxyl-dammarane-3, 12, 20-triol from Panax notoginseng in human, monkey, dog, rat, and mouse liver microsomes.

The present study characterized in vitro metabolites of 20(R)-25-methoxyl-dammarane-3ß, 12ß, 20-triol (20(R)-25-OCH3-PPD) in mouse, rat, dog, monkey and human liver microsomes. 20(R)-25-OCH3-PPD was incubated with liver microsomes in the presence of NADPH. The reaction mixtures and the metabolites were identified on the basis of their mass profiles using LC-Q/TOF and were quantified using triple quadrupole instrument by multiple reaction monitoring. A total of 7 metabolites (M1-M7) of the phase I metabolites were detected in all species. 25(R)-OCH3-PPD was metabolized by hydroxylation, dehydrogenation, and O-demethylation. Enzyme kinetic of 20(R)-25-OCH3-PPD metabolism was evaluated in rat and human hepatic microsomes. Incubations studies with selective chemical inhibitors demonstrated that the metabolism of 20(R)-25-OCH3-PPD was primarily mediated by CYP3A4. We conclude that 20(R)-25-OCH3-PPD was metabolized extensively in mammalian species of mouse, rat, dog, monkey, and human. CYP3A4-catalyzed oxygenation metabolism played an important role in the disposition of 25(R)-OCH3-PPD, especially at the C-20 hydroxyl group.

New inhibitors of α-glucosidase in Salacia hainanensis Chun et How.

The methanol extract from roots of Salacia hainanensis Chun et How afforded three new compounds, 24,26-dihydroxy-25-methoxy-tirucall-9-en-3-one (1), 2ß,3ß,22α-trihydroxy-lup-20(29)-ene (2) and 3ß-hydroxy-2-carbonyl-lupan-29-oic acid (3), along with six known triterpenoids (4-9). Their structures were established on the basis of spectral analysis, in particular according to the data obtained by two-dimensional-NMR and high-resolution mass spectra experiments. Some of them showed much stronger inhibitory activity towards α-glucosidase than the positive control (acarbose, IC50 10.2 µM).