[Progress in antitumor activity of diterpenoid alkaloids in plants of Aconitum].

Small-molecule compounds with rich sources have diverse structures and activities. The active ingredients in traditional Chinese medicine(TCM) provide new sources for the discovery of new antitumor drugs. Aconitum plants as Chinese medicinal plants have the effects of dispelling wind, removing dampness, warming meridian, and relieving pain. They are mainly used to treat inflammation, pain, rheumatism, and tumors, improve heart function, and dilate blood vessels in clinical practice. Diterpenoid alkaloids are the main active components of Aconitum plants, including C20-, C19-, C18-diterpenoid alkaloids and bis-diterpenoid alkaloids. Stu-dies have demonstrated that diterpenoid alkaloids can effectively treat lung cancer, liver cancer, breast cancer, colon cancer and other cancers. Diterpenoid alkaloids are considered as the most promising natural compounds against cancers. In this review, we summarized the chemical structures and antitumor activities of C20-, C19-, C18-diterpenoid alkaloids and bis-diterpenoid alkaloids extracted from plants of Aconitum, aiming to provide reference for further development of diterpenoid alkaloids from Aconitum as antitumor drugs.

High genetic diversity and low population differentiation of a medical plant Ficus hirta Vahl., uncovered by microsatellite loci: implications for conservation and breeding.

BACKGROUND: Wuzhimaotao (Radix Fici Hirtae) originates from the dry root of Ficus hirta (Moraceae), which is widely known as a medical and edible plant distributed in South China. As the increasing demand for Wuzhimaotao, the wild F. hirta has been extremely reduced during the past years. It is urgent to protect and rationally develop the wild resources of F. hirta for its sustainable utilization. However, a lack of genetic background of F. hirta makes it difficult to plan conservation and breeding strategies for this medical plant. In the present study, a total of 414 accessions of F. hirta from 7 provinces in southern China were evaluated for the population genetics using 9 polymorphic SSR markers. RESULTS: A mean of 17.1 alleles per locus was observed. The expected heterozygosity (He) varied from 0.142 to 0.861 (mean = 0.706) in nine SSR loci. High genetic diversity (He = 0.706, ranged from 0.613 to 0.755) and low genetic differentiation among populations (G'ST = 0.147) were revealed at population level. In addition, analysis of molecular variance (AMOVA) indicated that the principal molecular variance existed within populations (96.2%) was significantly higher than that among populations (3.8%). Meanwhile, the three kinds of clustering methods analysis (STRUCTURE, PCoA and UPGMA) suggested that the sampled populations were clustered into two main genetic groups (K = 2). Mantel test showed a significant correlation between geographic and genetic distance among populations (R2 = 0.281, P < 0.001). Pollen flow, seed flow and/or geographical barriers might be the main factors that formed the current genetic patterns of F. hirta populations. CONCLUSIONS: This is a comprehensive study of genetic diversity and population structure of F. hirta in southern China. We revealed the high genetic diversity and low population differentiation in this medicinal plant and clarified the causes of its current genetic patterns. Our study will provide novel insights into the exploitation and conservation strategies for F. hirta.

A holistic framework of water quality evaluation using water quality index (WQI) in the Yihe River (China).

The Yihe River is an important river in Shandong Province, China. It is a catchment river for the South-to-North Water Diversion Project (SNWDP-ER), providing a variety of benefits and ecosystem services, such as flood and drought regulation, fishery and aquaculture, drinking water sources, and biodiversity conservation. In order to objectively reflect the status and changing trend of water environmental quality of the Yihe River, reduce the cost of detection, and improve the efficiency of water quality evaluation, samples were collected at 8 sampling sites in the 220 km main stream of the Yihe River from 2009 to 2019. The spatiotemporal variations of 10 water quality indicators were analyzed, including pH, water temperature (WT), dissolved oxygen (DO), 5-day biochemical oxygen demand (BOD5), chemical oxygen demand (COD), total phosphorus (TP), ammonia nitrogen (NH3-N), nitrate (NO3-N), fluoride (F-), and sulphate (SO42-). The water quality index (WQI) was used to evaluate the spatiotemporal water quality changes, and the minimum WQI (WQImin) model consisting of five key indicators, i.e., NH3-N, BOD5, DO, SO42-, and WT, was built by using stepwise multiple linear regression analysis. The results indicated that the water quality indicators in the Yihe River showed significant spatiotemporal variations. With the exception of the COD and TP, the other water quality indicators conformed to the Class I or II standards of China, indicating that the water quality of the Yihe River was better than most natural water bodies. Seasonally, the WQI was better in the autumn and higher in the upstream area compared to the downstream. The water quality remained at the "good" level. The weighted WQImin model performed well in evaluating water quality, with coefficient of determination (R2), mean square error (MSE), and percentage error (PE) values of 0.903, 3.05, and 1.70%, respectively.

O2 distribution and dynamics in the rhizosphere of Phragmites australis, and implications for nutrient removal in sediments.

Root-triggered microscale variations in O2 distribution in the rhizosphere of young Phragmites australis are important for nutrient removal in sediments. In this study, the micro-scale O2 dynamics and the small-scale changes of soluble reactive phosphorus (SRP) and ammonium (NH4+) in the rhizosphere of P. australis were investigated using planar optodes and high-resolution dialysis (HR-Peeper), respectively. Results suggested that root O2 leakage has a highly variable distribution depending on the stage of root growth, the site of O2 leakage gradually shift from the entire emerging main roots to the main root tip and subsequently shifted the emerging lateral roots. The O2 concentration increased in the rhizosphere with increasing light intensity and O2 levels in the overlying water. Continuous O2 release from the lateral roots causes the formation of iron plaque on the surface of lateral roots, which reduce the mobility of P by adsorption of iron plaque in the rhizosphere. The oscillation of oxic-anoxic root zones improves nitrogen removal through the processes of anammox, heterotrophic denitrification and nitrification. This work from the micro-scale demonstrates that the O2 concentration is the spatio-temporal variations in the rhizosphere, and it presents an important role for nutrient removal in sediments.

Mechanisms driving phosphorus release during algal blooms based on hourly changes in iron and phosphorus concentrations in sediments.

Algal growth causes a drastic change in aquatic conditions over a diel cycle, which may induce sensitive feedback systems in sediments, causing P release. In this study, a microcosm experiment was performed using a suction sampler (Rhizon) to observe changes in soluble reactive phosphorus (SRP) and soluble Fe(II) concentrations in the top 20 mm sediment layer on a 3-h time interval, at different phases of harmful algal bloom (HAB) development. The results showed that the algal blooms prevailed up to 15 days after incubation, after which the process of bloom collapse proceeded until the 70th day. The concentrations of pore-water soluble Fe(II) and SRP increased throughout the incubation period. Compared to day 1, maximum increases of 214% in soluble Fe(II) and 387% in SRP were observed at night during the bloom and collapse periods, respectively. The diffusive fluxes of Fe and P at the sediment-water interface (SWI) generally corresponded to their changes in concentrations. Hourly fluctuation in soluble Fe(II) and SRP concentrations were observed with two distinct concentration peaks occurred at 21:00 p.m. and 06:00 a.m. (or 03:00 a.m.), respectively. These findings suggest that Fe-P coupling mechanisms are responsible for the release of P from sediments. During the collapse period, soluble Fe(II) concentrations were suppressed by the increase of labile S(-II) at night. Meanwhile, SRP concentrations were decoupled from Fe cycling with small fluctuations (<11% RSD) on an hourly timescale, and the decomposition of algae was a dominant source contributing to the release of P from sediments. These results significantly improved the understanding of processes and mechanisms behind the stimulated release of P from sediments during HABs.

Activity of compounds from Taxillus sutchuenensis as inhibitors of HCV NS3 serine protease.

This study aimed to isolate active compounds from traditional Chinese medicinal Taxillus sutchuenensis to inhibit hepatitis C virus (HCV) NS3 protease activity. Under the guidance of bioassay, 10 compounds were isolated from the EtOAc extract fraction, which were identified as inhibitors of HCV NS3 protease. IC50 values of these compounds were obtained, and a broad degree of anti-HCV activity was observed. The most active compounds were kaempferol-3,7-bisrhamnoside (19.4 µM) and (3S)-3-hydroxy-1,7-bis(4-hydroxy-phenyl)-6E-hepten-5-one (28.7 µM). In conclusion, flavonoids and diarylheptanoids were responsible for the anti-HCV constitution of Taxilli Herba. These inhibitors of HCV NS3 protease might serve as potential candidate of anti-HCV agents.

H1-A, a compound isolated from Fusarium oxysporum inhibits hepatitis C virus (HCV) NS3 serine protease.

The present study was aimed to isolate the active compounds from the fermentation products of Fusarium oxysporum, which had hepatitis C virus (HCV) NS3 protease inhibitory activity. A bioactive compound was isolated by reverse-phase silica-gel column chromatography, silica-gel column chromatography, semi-preparative reverse-phase High Performance Liquid Chromatography (HPLC), and then its molecular structure was elucidated based on the spectrosopic analysis. As a result, the compound (H1-A, 1) Ergosta-5, 8 (14), 22-trien-7-one, 3-hydroxy-,(3ß, 22E) was isolated and identified. To the best of our knowledge, this was the first report on the isolation of H1-A from microorganisms with the inhibitory activity of NS3 protease.

[Evaluation for impacts of gut wall metabolism of multiple components in Chuanxiong Rhizoma during intestinal absorption with S9 incubation].

The information of drug deposition in the intestine is required in the study for the drug absorption in biopharmaceutics classification system (BCS). To illustrate the impacts of gut wall metabolism on the absorption, metabolism of multiple components in Chuanxiong Rhizoma in gut wall was tested by rat S9 incubation in vitro. The chemical fingerprint technology was used in this study to simultaneously detect multiple components in Chuanxiong, and peak areas before and after S9 incubation were compared. The results showed that senkyunolide I and several constituents were metabolized by gut wall, and one new metabolite was founded. However, ferulic acid and other compounds remained unchanged after incubation. Therefore, the subsequent intestinal permeability of multiple components in Chuanxiong that were not metabolized in the intestine was suggested to be detected directly by in situ single-pass intestinal perfusion (SPIP).Nonetheless, the intestinal permeability of the constituents that were metabolized in the intestine shall be explored by appropriate approaches.

Aptamer-based surface-enhanced Raman scattering-microfluidic sensor for sensitive and selective polychlorinated biphenyls detection.

A surface-enhanced Raman scattering (SERS) measurement of 3,3',4,4'-tetrachlorobiphenyl (PCB77) with aptamer capturing in a microfluidic device was demonstrated. To construct the microfluidic chip, an ordered Ag nanocrown array was fabricated over a patterned polydimethylsiloxane (PDMS) that was achieved by replicating an anodic aluminum oxide (AAO) template. The patterned PDMS sheet was covered with another PDMS sheet having two input channel grooves to form a close chip. The Ag nanocrown array was used for the SERS enhancement area and the detection zone. PCB 77 aptamers were injected into one channel and the other allows for analytes (PCBs). The mercapto aptamers captured the targets in the mixed zone and were immobilized to the SERS detection zone via S-Ag bonds so as to further improve both the SERS sensitivity and selectivity of PCB77. Such an aptamer-based microfluidic chip realized a rapid SERS detection. The lowest detectable concentration of 1.0 × 10(-8) M was achieved for PCB77. This work demonstrates that the aptamer-modified SERS microfluidic sensor can be utilized for selective detections of organic pollutants in the environment.

Effects of an isopropanolic-aqueous black cohosh extract on central body temperature of ovariectomized rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Black cohosh (Cimicifuga racemosa) is widely used in menopause symptoms strategy. AIM OF THE STUDY: The aim of this study was to examine the effect of isopropanolic black cohosh extract (iCR) on the central body temperature (CBT) of ovariectomized rats (OVX) and elaborate its possible effects in alleviating menopause related hot flushes. MATERIALS AND METHODS: 64 female Sprague-Dawley rats, weighing 230 ± 10g and aged 6-8 weeks, were divided into four groups: ovariectomy (OVX), sham, ovariectomy plus estradiol valerate (OVX+E), and ovariectomy plus iCR (OVX+ICR). The sham group underwent a sham surgery without ovariectomies, while the other three groups underwent bilateral ovariectomies under sterile conditions and a temperature implant was embedded in the abdominal cavity of all four groups. After 2-week recovery period, the temperature of all animals was monitored for 6 weeks. RESULTS: CBT of four groups maintained a normal circadian rhythm, with a low day CBT and a high night CBT. CBTs of the sham group were lower than that of the other three groups. The day CBTs of the (OVX+E) group and (OVX+ICR) group were lower than that of the OVX group from day 2 and day 22 respectively. For the difference between day and night CBT, the sham group was smallest, while (OVX+E) and (OVX+ICR) groups were higher than that of OVX group. The amplitude of day and night CBT, CBT fluctuation frequency at 5 min intervals, were higher for the OVX group than the sham group; the amplitude of day and night CBT of (OVX+E) group and the amplitude of night CBT of (OVX+ICR) group were higher than those of OVX group; while the amplitude of day CBT of (OVX+ICR) group was lower than that of OVX group; CBT fluctuation frequency at 5 min intervals was higher for the (OVX+E) and (OVX+ICR) groups than the OVX group. CONCLUSIONS: Ovariectomized rats had abnormal thermoregulation, demonstrating an increase in day and night CBT, greater difference between day and night CBT, higher amplitude of day and night CBT, and more CBT fluctuation frequency. For the herbal extract iCR, the onset of affecting abnormal thermoregulation took longer than that of estradiol valerate. ICR had a significant effect on day CBT but was only little effective on night CBT of ovariectomized rats.

[Studies on chemical constituents from stem bark of Trewia nudiflora].

OBJECTIVE: To study the chemical constituents from the stem bark of Trewia nudiflora. METHOD: The chemical constituents were isolated by silica gel and sephadex LH - 20 column chromatography, and the structures were elucidated by means of spectral analysis. RESULT: Ten compounds were obtained from EtOAc fraction of EtOH extract and identified as stigmast-4-en-6beta-ol-3-one (1), stigmast-4-en-6alpha-ol-3-one (2), 7beta-hydroxysitosterol (3), 7alpha-hydroxysitosterol (4), schleicheol 2 (5), taraxerone (6), abbeokutone (7), beta-hydroxypropiovanillone (8), o-vanillyl alcohol (9), glycerol monopalmitate (10). CONCLUSION: Compounds 1-5 and 7-9 were isolated from this plant for the first time.

A new ellagic acid glycoside from Paeonia delavayi.

A new ellagic acid glycoside, 4'-O-methylellagic acid 4-O-beta-D-glucopyranoside (1), was isolated from the root cortex of Paeonia delavayi. The structure was elucidated on the basis of spectroscopic methods.

Monoterpene glycosides from Paeonia delavayi.

A new monoterpene glycoside, 4-O-methyl-4''-hydroxy-3''-methoxy-paeoniflorin (1), was isolated from the root cortex of Paeonia delavayi along with the known paeoniflorin, oxypaeoniflorin, benzoylpaeoniflorin, benzoyloxypaeoniflorin, albiflorin and a paeonilactone-A.