•A combination of Paris Saponin I (PSI) and Camptothecin (CPT) was studied.•A combination of PSI and 10-hydroxycamptothecin (HCPT) was studied.•PSI enhanced the sensitivities of cancer cells to CPT/HCPT by inducing apoptosis.•PSI sensitized lung cancer cells to CPT and HCPT via MAPKs and Akt pathways.Paris Saponin I (PSI), a steroidal sponins isolated from plant, has been exhibited antitumor and many other biological activities. In this study, we investigated the role and underlying mechanisms of PSI in the synergistic regulation of antitumor activity of Camptothecin (CPT) and 10-hydroxycamptothecin (HCPT) in four types of lung cancer cells. The inhibitory evaluation showed that PSI could significantly reduce the CPT/HCPT-mediated cell proliferation and enhance the sensitivities of H1299, H460 and H446 lung cancer cells to CPT/HCPT. Mechanism study indicated that PSI improved the CPT/HCPT induced apoptosis in lung cancer cells through mitochondria pathway including cytochrome C release and activation of caspase-9 and -3 cascades. Furthermore, PSI plus CPT/HCPT also increased the up-regulation of Bax and down-regulation of Bcl-2 and Bcl-XL in H460 and H446 cells. Moreover, PSI enhanced CPT/HCPT-mediated inhibition of p38 MAPK and activation of phosphorylation of p38 MAPK in H1299 cells, and suppression of Akt and ERK pathways activation in H460 cells as well as in H446 cells. Collectively, our results demonstrated that PSI functions as a chemosensitizer by enhancing apoptosis through influencing p38 MAPK, ERK, and Akt pathways in lung cancer cells, and the combination with CPT/HCPT might be a promising strategy for the development of new therapeutic agents.

•Yam with hot air-drying at 60 °C had higher allantoin content.•Yam with hot air-drying at 40 °C and 80 °C had higher resistant starch.•Blanching (100 °C for 1min) was effective to inhibiting enzymatic browning of yam.•Flavonoid ingredients of yam may be mainly substrate of enzymatic browning reaction.The effects of blanching (in boiling water for 1min) and different hot air drying temperatures (40 °C, 60 °C and 80 °C) on the polyphenol oxidase (PPO), peroxidase (POD) and antioxidant activities, main bioactive components, as well as the starch-related physicochemical properties of yam flours were studied. The results of PPO and POD activities, and total flavone and total soluble polyphenol contents showed that blanching was effective to inhibiting enzymatic browning of yams, and the substrate of enzymatic browning reaction may be mainly flavonoid ingredients. The sample of H-40 had higher allantoin and total soluble polyphenol content, stronger DPPH scavenging activity and reducing power. From the results of scanning electron microscopy (SEM), X-ray diffraction (XRD), and Fourier transform infrared (FT-IR), the blanching yams was found contain partly gelatinized starch granules, and had lower crystallinity. The H-40 and H-80 samples had higher RS contents and lower GI values. Furthermore, the protein and soluble amylose contents, solubility and swelling power at 90 °C of the blanching yams were lower than those of the yams without blanching. We can effectively apply these flours in various products based on their characteristics.

•Twenty-nine metabolites were isolated from Dioscorea collettii.•Fourteen compounds were firstly isolated from the genus Dioscorea as well as the family Dioscoreaceae.•The chemotaxonomic significance of the isolated compounds was discussed.A chemical investigation of Dioscorea collettii led to the isolation of twenty-nine compounds, including six steroid saponins (1–6), thirteen monocyclic phenols (7–19), two flavonoids (20–21), three sterols (22–24), and five cyclodipeptides (25–29). The chemical structures of these compounds were elucidated using spectroscopic methods and by comparing their data to that reported in the literature. This study is the first report of compounds 2–4, 7, 14–17, 21, and 23–24 in D. collettii, while compounds 8–13, 18–20, and 25–29 were first isolated from the genus Dioscorea and the family Dioscoreaceae. The chemotaxonomic significance of the isolated compounds is discussed.

Prunella vulgaris L. is as a major plant in the Chinese traditional functional beverage Guangdong herbal tea for the treatment of fevers, diarrhea, and sore mouth. In this study, ethyl acetate parts of aqueous extracts from P. vulgaris L. (EtOAc-APV) were found to demonstrate potent acetylcholinesterase (AChE) inhibition in vitro. Therefore, this study was designed to further investigate the effects of EtOAc-APV on scopolamine (SCOP)-induced aging rats. Male Wistar rats were randomly divided into four groups (n = 12) and given orally by gavage EtOAc-APV (100 mg/kg) for 3 weeks. SCOP (1 mg/kg, ip) was administered to rats 30 min before starting behavioral tests consecutively for 3 days. EtOAc-APV could attenuate SCOP-induced brain senescence in rats by improving behavioral performance and decreasing brain cell damage, which was associated with a notable reduction in AChE activity and MDA level, as well as an increase in SOD and GPx activities. Additionally, EtOAc-APV administration could reduce the expression of NF-κB and GFAP, which showed an anti-neuroinflammatory effect on the SCOP-treated rat. Overall, the current study highlights P. vulgaris L. as an antidementia dietary supplement.Keywords: acetylcholinesterase inhibitor; chemical components; ethyl acetate parts of aqueous extracts from Prunella vulgaris L.; neuroprotection; Prunella vulgaris L.;

Rheumatoid arthritis (RA) is a chronic inflammatory disease with a serious pre-vascular inflammatory phase, followed by significant increase in vessel growth. Inhibition of angiogenesis is a novel therapeutic strategy against RA. The Chinese herbal remedy Tripterygium wilfordii, Hook. f. (TwHf) has been reported to be therapeutically efficacious in the treatment of RA. Recent studies have revealed that treatment with TwHf extracts inhibit angiogenesis of RA, thereby elaborately attenuation RA symptom. This review mainly addresses the anti-angiogenesis effect of TwHf in treatment of RA.

Paris Saponin I (PSI), a steroidal saponin derivative extracted from a traditional Chinese herbal Paris polyphylla, has shown cytotoxic effects on several tumor cell lines. However, the mechanisms of its antitumor activity especially for lung cancers remain to be elucidated. In this present investigation, we continue to explore the efficacy and mechanisms underlying the cytotoxic effects of PSI in lung cancer cell lines. Three non-small cell lung cancer (NSCLC) cells (H1299, H520, H460) and one small cell lung cancer (SCLC) cell (H446) were treated with PSI for the first time. PSI significantly induced cell cycle arrest at the G2/M phase and mitochondrial-related apoptosis NSCLC cells but not SCLC cells. Additionally, PSI reduced phosphorylation of AKT in NSCLC and ERK in SCLC in general. Interestingly, we observed that PSI influenced different signaling pathways among the four kinds of lung cancer cells. After PSI treatment, p38 MAPK and ERK activation were observed in H1299, while p38 MAPK increased and JNK decreased in H520. On the contrary, we found JNK activation in H460 cells with PSI. However, PSI upregulated the AKT activity and inhibited the JNK expression in H446 cells. The results indicate that PSI exhibits the cytotoxicity in different pathways depending on the cancer types.

The aim of the study was to investigate the protective effects of costunolide (Co) and dehydrocostus (De) in 5-fluorouracil (5-FU)-induced intestinal mucositis (IM) as well as the potential mechanisms involved. Male Kunming mice were given 5-FU (60 mg kg−1 per day) by intraperitoneal injections for 5 consecutive days and IM was evaluated histochemically. Co (5, 20 mg kg−1) and De (5, 20 mg kg−1) were orally administered once daily for 8 days. Repeated 5-FU treatment caused severe IM including morphological damage, which was accompanied by feeding reduction, body weight loss and diarrhea. Daily intragastric administration of Co or De significantly relieved the severity of IM through promoting intestinal mucosal recovery, inhibiting reactive oxygen species and ameliorating the inflammatory responses. Accordingly, Co and De may be promising therapeutic candidates and clinically used for the prevention of IM during cancer chemotherapy.

•A new diarylheptanoid with 6/5/5 fused rings was isolated from D. collettii.•The structures were elucidated by spectroscopic analysis and ECD calculation.•The structure of new compound was confirmed by single-crystal X-ray diffraction.•The cytotoxic activities of the compounds were tested against NCL-H460.An unprecedented diarylheptanoid derivative with 6/5/5 fused rings, diocollettines A (1), together with five known compounds (2–6) were isolated from the rhizomes of Dioscorea collettii. The structures were elucidated by extensive NMR spectroscopic analysis, together with HR-ESI-MS techniques. The absolute configuration of compound 1 was unambiguously confirmed by comparison of experimental data with calculated electronic circular dichroism (ECD) spectra and single-crystal X-ray diffraction analysis. Compound 1 exhibited moderate cytotoxicity against NCL-H460.

Cerebralcare granule® (CG) is a preparation of Traditional Chinese Medicine that widely used in China. It was approved by the China State Food and Drug Administration for treatment of headache and dizziness associated with cerebrovascular diseases. In the present study, we aimed to investigate whether CG had protective effect against d-galactose (gal)-induced memory impairment and to explore the mechanism of its action. d-gal was administered (100 mg/kg, subcutaneously) once daily for 8 weeks to induced memory deficit and neurotoxicity in the brain of aging mouse and CG (7.5, 15, and 30 g/kg) were simultaneously administered orally. The present study demonstrates that CG can alleviate aging in the mouse brain induced by d-gal through improving behavioral performance and reducing brain cell damage in the hippocampus. CG prevents aging mainly via suppression of oxidative stress response, such as decreasing NO and MDA levels, renewing activities of SOD, CAT, and GPx, as well as decreasing AChE activity in the brain of d-gal-treated mice. In addition, CG prevents aging through inhibiting NF-κB-mediated inflammatory response and caspase-3-medicated neurodegeneration in the brain of d-gal treated mice. Taken together, these data clearly demonstrates that subcutaneous injection of d-gal produced memory deficit, meanwhile CG can protect neuron from d-gal insults and improve memory ability.

Suspended cells of Glycyrrhiza (CG) possessed a similar content of flavonoids and a lower content of triterpenes, when compared with its field cultivated equivalent (NG). Xylene-induced ear oedema and ovalbumin-induced mouse paw oedema were applied, to compare the effects of CG and NG on the acute inflammatory response. Extracts of the cell culture of Glycyrrhiza possessed a similar anti-inflammatory effect to those of NG, through the enhancement of the SOD activity of plasma and liver tissues. The use of a cell culture of liquorice instead of field cultivation would be potentially profitable.Highlights► Composition and activity comparison between field and cell-cultured Glycyrrhiza. ► Suspended cells of Glycyrrhiza are good for flavonoids accumulation. ► Cell-cultured Glycyrrhiza shows a good anti-inflammatory effect on mouse paw oedema.

In this study, callus and cell suspension were induced from seedlings of licorice (G. uralensis). In addition, it was revealed that the appropriate concentration of sucrose could promote the callus growth and increase the content of polysaccharide. The methyl jasmonate (MJ) and phenylalanine (PHE) could enhance the callus growth and content of flavonoids for G. uralensis. For producing more flavonoids and polysaccharide, two-stage cultivation was performed. In the first step, 30 g L−1 sucrose was fed into a 5-L balloon-type bubble bioreactor on 8th day of culture to enhance cell production and metabolite production. In a two-stage cultivation process, PHE (2 mM) and MJ (5 mg L−1) were added into a 5-L balloon-type bubble bioreactor after 10 days of culture. Using a fed-batch cultivation strategy (30 g L−1 sucrose was fed into a 5-L balloon-type bubble bioreactor on 8th day), polysaccharide production was enhanced to 1.19 g L−1, which was 2.12-fold greater than that in batch cultivation. The flavonoids yield (55.42 mg L−1) which was about 22 % higher than that in batch cultivation was obtained on 21st day. In a two-stage cultivation process, the polysaccharide content was increased by 1.14- and 2.12-fold compared with fed-batch cultivation and batch cultivation on 15th day. Meanwhile, total flavonoids yield (132.36 mg L−1) on 15th day, was increased by 2.26- and 2.67-fold compared with fed-batch cultivation and batch cultivation. In conclusion, two-stage cultivation process combined with the sucrose and elicitor treatment could promote both the callus growth and the secondary metabolites accumulation.

The contents of total phenolics, total flavonoids, total anthocyanins, and total triterpenes of eight pear samples were determined, and the monomeric compounds were identified and quantitated using high-performance liquid chromatography. The in vitro antioxidant and in vivo anti-inflammatory activities of the different pear cultivars were compared. Arbutin and catechin were the dominant polyphenol compounds in the eight pear varieties, followed by chlorogenic acid, quercetin, and rutin. In addition, Xuehua pear and Nanguo pear had significantly higher total phenolics and flavonoids contents, while Dangshansu pear had the largest total triterpenes value (209.2 mg/100 g). Xuehua pear and Nanguo pear also were the highest in total anthocyanins. The pears with high total phenolics and total flavonoids contents had significantly higher antioxidant and anti-inflammatory abilities than those of other species. Anthocyanins were correlated to antioxidant capacity in pears, whereas total triterpenoids were strongly correlated to anti-inflammatory activity.

Ten compounds (1–10) were isolated from the underground parts of Trillium tschonoskii Maxim.. Their structures were elucidated on the basis of spectroscopic evidence using 1D and 2D-NMR and chemical methods, and identified as two sterols (1–2), six spirostanols (3–8) and two furostanols (9–10). The results indicate a close relationship between the two genera Trillium and Paris, and the chemotaxonomic significance of these compounds was summarized.Highlights► Ten compounds were isolated from Trillium tschonoskii. ► Two sterols and two spirostanols were firstly obtained from Trillium. ► The complete NMR data of two furostanols has been reported. ► The research confirms that Trillium and Paris are closely related taxonomically. ► The study supports that the two genera can be independent from Liliaceae.

Traditional Chinese medicines (TCMs) are generally considered complementary or alternative remedies in most Western countries. The constituents of TCMs are hard to define, and their efficacy is difficult to appraise. Thus, the development of suitable methods for evaluating the relationship between bioactivity and the chemical makeup of complex TCM mixtures remains a great challenge. In the present work, the bioactivity-integrated fingerprints of alkaloidal leaf extracts of Alstonia scholaris, a folk medicinal herb for chronic respiratory diseases, were established by ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q/TOF). This method was coupled with two dual-luciferase reporter assay systems to show nuclear factor-κB (NF-κB) inhibition and β2 adrenergic receptor (β2AR) activation. Using UPLC-Q/TOF, 18 potential candidates were identified according to unique mass spectrometric fragmentation. After in vitro biological evaluation, several indole alkaloids with anti-inflammatory and anti-asthmatic properties were found, including akuammidine, (E)-alstoscholarine, and (Z)-alstoscholarine. Compared with conventional fingerprints, the microfractionation based bioactivity-integrated fingerprints that contain both chemical and bioactivity details offer a more comprehensive understanding of the chemical makeup of plant materials. This strategy clearly demonstrated that dual bioactivity-integrated fingerprinting is a powerful tool for the improved screening and identification of potential dual-target lead compounds in complex herbal medicines.Highlights► A microfractionation bioactivity-based fingerprint of A. scholaris was established. ► This method was coupled with two dual-luciferase reporter assay systems. ► NF-κB inhibitors and β2AR agonists can be screened simultaneously in one process. ► Three dual-functional indole alkaloids with dual-target were found. ► The strategy is suitable for identifying dual-target compounds in complex systems.

Panax ginseng C. A. Meyer is one of the important nutraceutical and medicinal plants, which is used worldwide. Until now, ginseng has been reported to contain saponins, antioxidants, peptides, polysaccharides, fatty acids, vitamins, alkaloids, lignans, and flavonoids. The saponins, known as ginsenosides, are widely believed to be the major bioactive compounds of ginseng. In this article, ginsenoside biosynthesis pathway and key enzymes regulation are also described. This review provides a reference for improving ginsenoside contents through regulation of ginsenoside biosynthesis pathway.

Periploca sepium adventitious roots were cultured on 0.5 Murashige and Skoog solid media supplemented with exogenous hormones of different types and various concentrations, and with sucrose of different concentrations. Auxins (indole butyric acid (IBA) and naphthalene acetic acid (NAA)) and cytokinins (6-benzylaminopurine (BA) and kinetin (KT)) were selected as exogenous hormones for adventitious root proliferation. Compared with other hormones, IBA was the suitable auxin for adventitious root proliferation. Under this circumstance, every root explant generates 10–15 adventitious roots (1- to 2-cm long) after 30 days. However, nothing but callus was induced on the root explants when NAA was added into the medium and the same result was achieved when auxins (IBA or NAA) were added into the media together with cytokinins (BA or KT). The suitable concentration of IBA for adventitious root proliferation was 1–2 mg/l, when every root explant generated 10–20 adventitious roots (1- to 2-cm long). The optimum concentration of IBA for periplocin accumulation was 1 mg/l, when the periplocin content reached 95.46 μg/g. With regard to the investigation of sucrose concentration, 2–3% (w/v) sucrose was favorable for adventitious root proliferation as every root explant in this concentration generated 10–20 adventitious roots (1- to 2-cm long). The highest periplocin content (101.56 μg/g) was achieved at 5% (w/v) sucrose, whereas the periplocin content at 5% (w/v) sucrose did not show significant difference from the periplocin content (95.38 and 98.47 μg/g, respectively) at 3% (w/v) or 4% (w/v) sucrose.

A scale-up culture of adventitious roots of ginseng was established using a balloon-type bubble bioreactor (BTBB). Maximum growth rates of ~52-fold and ~50-fold in 3 and 5 L BTBBs were obtained, respectively after 40 days of inoculation, which was significantly higher than that in 0.5 L conical flask (~15-fold). Gradually scale-up culture of adventitious roots increased the root biomass, while the contents of ginsenoside and polysaccharides were not affected. This study also revealed that radical scavenging activity of dried adventitious roots on 1,1-diphenyl-2-picrylhydrazyl was higher than that of native roots at 20–100 mg L−1 methanolic extract.

The rhizomes growing from Licorice (Glycyrrhiza uralensis Fisch.) seeds carried by the Chinese recoverable satellite named “Shen Zhou” and from the parallel ground-based seeds were selected as the samples. Seeds were flown under the space condition for 18 days. Average radiation dose in the flight recovery module was 0.102 mGy/day and the distance from flight apogee to earth was 350 km and the gravity was 10−6 g. After returning to earth, the seeds carried by the satellite and the parallel ground control were cultivated to maturity under the same condition. In this paper, fingerprint was obtained and contents of the four main ingredients of the samples were investigated on a high performance liquid chromatography with diode-array detection. The differentiation between the 12 samples induced by cosmic factors was observed. Contents of the detected four components of space flight group were much higher than that of the control group. Areas of the 26 common peaks of the 12 samples were analyzed by principal component analysis and three components were extracted. The results demonstrated that extraterrestrial environment could affect the amount of its secondary metabolites. This report provided the scientific data for spaceflight breeding of a medicinal plant and indicated that extraterrestrial orbit is a possible way in accelerating the rate of breeding and select eximious germplasm resources.

Based on the results of carbon source consumption in cell suspension culture of Panax quinquefolium L., 30 g L−1 sucrose was fed into a 5-L stirred tank bioreactor on day 16 of culture to enhance cell density and metabolite production. Using a fed-batch cultivation strategy, polysaccharide production was enhanced to 1.608 g L−1, which was 1.96-fold greater than with batch cultivation. The maximum saponin yield (7.828 mg L−1) was obtained on day 24 and was about 36% higher than the yields obtained using batch cultivation. In a two-stage culture process, a combined treatment with sucrose, lactoalbumin hydrolysate, and methyl jasmonate caused a significant increase in total saponin yield (31.52 mg L−1) in cell cultures after 27 d. This value represents an increase of 4.03-fold compared with the total saponin yield in fed-batch cultivation. The two-stage culture mode provided the best method for the in vitro production of secondary metabolites from P. quinquefolium.

In this article, ginsenosides and polysaccharide contents in suspension cells and native roots of Panax quinquefolium L. were studied. In order to enhance the contents of ginsenosides and polysaccharide in P. quinquefolium suspension cells, we tested the effects of lactoalbumin hydrolysate on the growth of P. quinquefolium suspension cell, synthesis of ginsenosides and polysaccharide in flask and bioreactor. In flask culture, cells growth ratio was significantly enhanced by the addition of lower concentration of lactoalbumin hydrolysate. Addition of 100 mg L−1 lactoalbumin hydrolysate significantly enhanced the contents of total saponins (5.44 mg g−1 DW) and the contents were 3.89-fold over the control group. Addition of lactoalbumin hydrolysate significantly promoted the accumulation of polysaccharide, except 200 mg L−1 lactoalbumin hydrolysate. The highest total saponins yield (36.72 mg L−1 DW) and polysaccharide yield (0.83 g L−1 DW) were obtained at 100 mg L−1 lactoalbumin hydrolysate. In a 5-L stirred tank bioreactor, the highest contents of total saponins and TRb group ginsenosides were achieved on day 26, while the effect of lactoalbumin hydrolysate on the contents of TRg group ginsenosides were insignificant. This result suggests that lactoalbumin hydrolysate might have triggered the enzyme activities for the synthesis of TRb group ginsenosides. Overall, the highest total saponins yield (31.37 mg L−1 DW) and polysaccharide yield (1.618 g L−1 DW) were obtained on day 26 and day 24 respectively and the polysaccharide yield was 1.95-fold higher than the shake flask culture (0.83 g L−1 DW). These results provided theoretical reference for two-stage culture in suspension cells of P. quinquefolium in bioreactor.

A reliable and accurate liquid chromatography with evaporative light scattering detection (LC-ELSD) method was developed for simultaneous determination of five constituents in Xue-Fu-Zhu-Yu capsule, a widely used prescription of traditional Chinese medicine (TCM). The chromatographic separation was performed on a Symmetry C18 column (150 mm×4.6 mm, 5.0 μm) using gradient elution of acetonitrile and water (containing 1.0% acetic acid). The flow rate was 0.6 mL/min and the temperature of column was 30°C. A good linearity correlation was obtained over the investigated concentration ranges. Recoveries of the five components varied from 97.31% to 99.84% (RSD<4.0%). The validated method was successfully applied to the quality assessment of Xue-Fu-Zhu-Yu capsule.

High-performance liquid chromatographic (HPLC) with evaporative light scattering detection (ELSD) and HPLC with electrospray ionization multistage tandem mass spectrometry (HPLC–ESI-MSn) were used to identify and quantify steroid saponins in Paris and Trillium plants. The content of the known saponins such as Paris I, II, III, V, VI, VII, H, gracillin and protodioscin in Paris and Trillium plants was determined simultaneously using the developed HPLC-ELSD method. Furthermore, other 12 steroid saponins were identified by HPLC–ESI(+/−)-MSn detection. In the end, a developed analytical procedure was proved to be a reliable and rapid method for the quality control of Paris and Trillium plants. In addition, the alternative resources for Paris yunnanensis used as a traditional Chinese medicine were discovered according to the hierarchical clustering analysis of the saponin fraction of these plants.

In order to understand how the nutrient elements were taken up during the cell growth as well as the production of metabolites, it was quite necessary to identify the dynamic change of metabolites and nutrients in suspension cells of Panax quinquefolium in bioreactor. In this study, dynamic accumulation of biomass and ginsenosides Re, Rb1 and polysaccharide as well as major nutrients consumption in cell suspension culture of P. quinquefolium in a 5-L stirred tank bioreactor were investigated. The dry cell weight and the contents of ginsenosides Re, Rb1 and polysaccharide reached the maximum peak simultaneously on about 21 days and the results showed that cell growth and metabolites synthesis related to nutrients consumption. For this reason, we supposed that the contents of metabolites can be increased through added nutrient at the right moment. These results provided theory reference for two-stage or continuous perfusion culture in suspension cells of P. quinquefolium in bioreactor.

Though several naphthalimide derivatives have exhibited antitumor activity in clinical trials, some issues such as toxicity prompted further structural modifications on the naphthalimide backbone. A series of naphthalimides conjugated with polyamines were synthesized to harness the polyamine transporter (PAT) for drug delivery, which was beneficial for the tumor cell selectivity. Bioevaluation in human hepatoma HepG2 cells treated with α-difluoromethylornithine (DFMO) or spermidine (Spd), human hepatoma Bel-7402 and normal QSG-7701 hepatocyte confirmed the PAT recognition and cell selectivity. In addition, the novel naphthalimide polyamine conjugate kills cellsviaapoptosis, and the Akt/mTOR signal pathway was first identified as the upstream cellular target through the apoptotic mechanism research. The presence of DFMO or Spd only either elevated or attenuated the cell apoptosis, but did not change the signal pathway. Collectively, the proper polyamine recognition element (i.e., homospermidine) mediated effective drug delivery via the PAT, and helped the proper cytotoxic goods (i.e., diverse naphthalimides) exert antitumor properties.

Carboxymethyl starch (CMS) was obtained as a product of the reaction of starch and monochloroacetic acid (MCA) in the presence of sodium hydroxide. The influence of the molar ratio of NaOH/AGU, the molar ratio of MCA/AGU, the reaction time, reaction temperature, and the water content on the degree of substitution (DS) was studied. The optimal molar ratio of NaOH/AGU and MCA/AGU is 2.4 and 1.0, respectively. Increase of the ratio of NaOH/AGU or MCA/AGU leads to an increase in DS, but only to certain extent. The highest values of the DS were obtained when the carboxymethylation was performed at 60 °C for 2.5 h. The water content in the reaction media ethanol was optimal at 20% (v/v). The scanning electron micrographs (SEMs) revealed that the carboxymethylation affected the structural arrangement of the starch and caused granular disintegration. The particle size distribution (PSD) also displayed that the average particle diameter increased greatly after modification from 37.37 μm to 72.88 μm. Wide angle X-ray diffractometry (XRD) revealed that starch crystallinity was obviously reduced after carboxymethylation. The new bands at 1600 cm−1 and 1426 cm−1 in FT-IR indicated that the starch granules were substituted.

A new macrolide glycoside, cuneataside F was isolated from the n-butanol extract of the stem of Sargentodoxa cuneata. The structure was elucidated on the basis of extensive 1D and 2D NMR as well as HRESI-MS spectroscopic analysis.

Licorice (Glycyrrhiza uralensis Fisch.) seeds were flown on a recoverable satellite for 18 days(the average radiation dose in the flight recovery module was 0.102 mGy/d, the distance from flight apogee to earth was 350 km, gravity 10−6). After returning to earth, the seeds were germinated and grown to maturity. The parallel ground-based seeds were also planted under the same conditions. The leaves of licorice were used for inter-simple sequence repeat (ISSR) analysis and the two main secondary metabolites in one-year-old roots were analyzed by high performance liquid chromatography (HPLC). Among 22 random primers used in this experiment, 6 primers generated different DNA band types. Analysis of HPLC showed that the content of glycyrrhizic acid (GA) and liquiritin (LQ) in the roots from seeds flown in space was respectively 2.19, 1.18 times higher than that of the control group. The results demonstrated that the extraterrestrial environment induced mutagenic effects on licorice and affected its secondary metabolites. These changes indicated that extraterrestrial orbit is possible means of breeding of licorice so as to preserve this endangered medicinal plant.

Two novel mononaphthalimide homospermidine derivatives (2a, 2b) with three or four methylene unit as linkages were synthesized and evaluated for cytotoxicity against human leukemia K562, murine melanoma B16 and Chinese hamster ovary CHO cell lines. The presence of homospermidine motif could greatly elevate the potency of 1,8-naphthalimide. Conjugate 2b with longer spacer exhibited higher in vitro cytotoxicity than 2a. The DNA binding experiments indicated that conjugates 2b could bind to herring sperm DNA. The topoisomerase II poison trials revealed that 2b could inhibit the activity of top. II.

This study was carried out to understand and establish the changes in physicochemical properties of starch extracted from Chinese yam (Dioscorea opposita Thunb.) after acetylation. Yam starch acetates with different degrees of substitution (DS) were prepared by the reaction of yam starch with glacial acetic acid/acetic anhydride using sulfuric acid as the catalyst. Their formation was confirmed by the presence of the carbonyl signal around 1750 cm−1 in the Fourier transform infrared (FT-IR) spectra. The thermal behavior of the native starch and starch acetate were investigated using thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The results reveal that the starch acetates are more thermally stable than the native starch. The starch esters showed 50% weight loss at temperatures from 328°C to 372°C, while the native starch underwent 50% weight loss at 325°C. The glass transition temperature (Tg) of the starch decreased from 273°C to 226°c. The X-ray diffraction (XRD) patterns could be classified as typical of the C-type for yam starch. X-ray diffraction also showed the loss of the ordered C-type starch crystalline structure and the degree of crystallinity of starch decreased from 36.10% to 10.96% with the increasing DS. The scanning electron microscopy (SEM) suggested that the most of the starch granules disintegrated with many visible fragments with the increasing DS.

Cyclophosphamide (CTX), as a common use of chemotherapeutic agent, has some side effects in clinical treatment. In our experiments, we studied CTX-treated T739 mice using histopathology, immunohistochemistry, reverse transcription polymerase chain reaction and Western blot for markers of proliferation, angiogenesis, tumor progression and distant metastasis. As a result, CTX increased the number and area of metastases and tumor embolus in lungs by effecting on the expression of matrix metalloproteinase-2, intercellular adhesion molecule-1 and tissue inhibitor of metalloproteinase-2. Taken together, it indicated that CTX enhanced the process of pulmonary metastasis by the synergistic effect of matrix-degrading proteases and adhesion proteins.

A novel phenylpropanoid glycosides 1, named parispolyside F, and a novel derivation of phenolic glycoside 2, named parispolyside G, as well as two known flavonoid glycosides were isolated from the rhizome of Paris polyphylla var. yunnanensis. Their structures were elucidated by spectroscopic methods.

A novel phenanthro [2,3-b] furan 1, named (3-hydroxy-9-(4′-hydroxy-3′-methoxyphenyl)-11-methoxy-5,6,9,10-tetrahydrophenanthro [2,3-b] furan-10-yl) methyl acetate, and two known phenolic compounds were isolated from the tubers of Pleione bulbocodioides (Franch.) Rolfe. Their structures were elucidated by spectroscopic methods.

Two new α,β-unsaturated butyrolactone derivatives, 4-(4″-hydroxybenzyl)-3-(3′-hydroxy-phenethyl)furan-2(5H)-one (1) and 3-(3′-hydroxyphenethyl)furan-2(5H)-one (2), together with one known phenolic compound (3), were isolated from the tubers of Pleione bulbocodioides (Franch.) Rolfe. Their structures were elucidated by analysis of spectroscopic data.

A novel alkenoic acid ester, (E)-4-hydroxy-dodec-2-enedioic acid-12-O-methyl ester and a new benzophenone, ethyl (S)-3-[2-(3,4-dihydroxybenzoyl)-4,5-dihydroxyphenyl]-2-hydroxypropanoate, together with a known compound, (E)-4-hydroxy-dodec-2-enedioic acids were isolated from the roots of Ranunculus ternatus. Their structures were elucidated by spectroscopic methods.

Rhizoma Paridis saponins (RPS) have been found to show strong antitumor activity. However, few studies have yet investigated its role on pulmonary metastasis treated with this herb. To investigate the molecular mechanisms related to metastasis, we studied RPS-treated T739 mice using histopathology, immunohistochemistry and reverse transcription polymerase chain reaction. Apoptosis was measured by TUNEL assay. As a result, RPS inhibited tumor growth by inducing apoptosis and upregulated the expression of TIMP-2 and down-regulated the level of MMP-2 and MMP-9. In conclusion, RPS is a potent anticancer agent that elicits programmed cell death and inhibits metastases in murine lung adenocarcinoma in vivo.

•RPS and cyclophosphamide both exhibited anti-cancer effect alone.•CYP2B6 and CYP3A4-mediated herb-drug interactions between RPS and other drugs.•RPS inhibited transference of cyclophosphamide into active and inactive compounds.Rhizoma Paridis Saponins (RPS), which is the effective part of Rhizoma Paridis, showed strong activity against lung cancer and hepatocarcinoma. In this research, a combination of RPS with cyclophosphamide (CTX) was used to treat hepatocarcinoma in mice. Although no active enhancement of activity was observed, some attenuation of the toxicity of RPS in combination with CTX occurred. In order to explain this phenomenon, we carried out research on the effects of Rhizoma Paridis Saponins on the activities of cytochrome p450 enzymes CYP1A2, CYP2A6, CYP2B6, CYP2C9, CYP2E1 and CYP3A4. The results indicated that RPS significantly influenced the activity of CYP2B6 and CYP3A4 through the inhibition of protein expression. However, RPS did not affect the activity of CYP1A2, CYP2A6, CYP2C9 and CYP2E1 in rats in vivo. These results suggested that RPS inhibited the conversion of cyclophosphamide into active metabolites and inactive byproducts through the reduced activities of CYP2B6 and CYP3A4. Therefore, it’s essential to pay attention to CYP2B6- and CYP3A4-mediated herb–drug interactions between RPS and other drugs.Download full-size image

Ethnopharmacological relevanceWei-Chang-An pill (WCA pill), a traditional Chinese pharmaceutical preparation, possessed potential anti-inflammatory advantages and noteworthy gastrointestinal regulations in digestive diseases, which might represent a promising candidate for the treatment of intestinal mucositis (IM) induced by 5-fluorouracil (5-FU).Aim of the studyTo analyze the bioactive constituents and investigate the effect of methanol extraction from WCA pill (WCA ext) on 5-FU induced IM with underlying mechanisms.Materials and methodsThe analysis of serum bioactive constituents after WCA ext administration in rats was carried out by UHPLC-Quadrupole-Time of Flight-Mass Spectrometry. In mice, IM was induced by 5-FU and physical manifestations were measured during the period of drug delivery. Half of mice were assessed with histology, expression of inflammatory cytokines in ileum and plasma via hematoxylin and eosin staining, immunohistochemical staining as well as cytokine enzyme-linked immunosorbent assay test, respectively. Besides, gastric emptying (GE) and gastrointestinal transit (GIT) were further tested in the other half of 5-FU induced mice.ResultsTwenty-two compounds were identified or tentatively characterized. IM induced by 5-FU was improved significantly after treatment with WCA ext through reducing the body weight loss, relieving the severe diarrhea, and inhibiting the GE as well as GIT. Further assessments validated that WCA ext promoted the recovery of intestinal mucosa, evaluated the activity of enterocyte proliferation, maintained the integrity of tight junction, and ameliorated the inflammatory disturbances.ConclusionsThese results suggested that WCA ext promoted the restoration of intestinal function in 5-FU-induced IM via regulating multiple sites of actions in intestinal homeostasis. Accordingly, WCA pill might be a promising therapeutic candidate for the prevention of IM during cancer chemotherapy.Download high-res image (319KB)Download full-size image

•The starch granules of microwave dried yam flour was gelatinization.•Freeze dried yam can as a source of hypoglycemic and lipid-lowering functional foods.•Hot air dried can be considered as an alternative method for sulphur fumigation dried.The effects of five different drying processes, air drying (AD), sulphur fumigation drying (SFD), hot air drying (HAD), freeze drying (FD) and microwave drying (MWD) for yams in terms of starch-related properties and antioxidant activity were studied. From the results of scanning electron microscopy (SEM), polarized optical microscopy (POM), X-ray diffraction (XRD), and Fourier transform infrared (FT-IR), the MWD sample was found to contain gelatinized starch granules. The FD yam had more slow digestible (SDS) and resistant starches (RS) compared with those processed with other modern drying methods. The bioactive components and the reducing power of the dried yams, were lower than those of fresh yam. When five dried samples were compared by principal component analysis, the HAD and SFD samples were observed to have the highest comprehensive principal component values. Based on our results, HAD would be a better method for yam drying than the more traditional SFD.

Though several naphthalimide derivatives have exhibited antitumor activity in clinical trials, some issues such as toxicity prompted further structural modifications on the naphthalimide backbone. A series of naphthalimides conjugated with polyamines were synthesized to harness the polyamine transporter (PAT) for drug delivery, which was beneficial for the tumor cell selectivity. Bioevaluation in human hepatoma HepG2 cells treated with α-difluoromethylornithine (DFMO) or spermidine (Spd), human hepatoma Bel-7402 and normal QSG-7701 hepatocyte confirmed the PAT recognition and cell selectivity. In addition, the novel naphthalimide polyamine conjugate kills cellsviaapoptosis, and the Akt/mTOR signal pathway was first identified as the upstream cellular target through the apoptotic mechanism research. The presence of DFMO or Spd only either elevated or attenuated the cell apoptosis, but did not change the signal pathway. Collectively, the proper polyamine recognition element (i.e., homospermidine) mediated effective drug delivery via the PAT, and helped the proper cytotoxic goods (i.e., diverse naphthalimides) exert antitumor properties.