Research progress on chemical constituents and pharmacological effects of Ajania plants / 中国中药杂志

Ajania belonging to the subtribe Artemisiinae of Anthemideae(Asteraceae) is a genus of semi-shrubs closely related to Chrysanthemum. There are 24 species of Ajania in northwestern China, most of which are folk herbal medicines with strong stress tolerance. Modern medical studies have demonstrated that the chemical constituents of Ajania mainly include terpenoids, flavonoids, phenylpropanoids, alkynes, and essential oils. These compounds endow the plants with antimicrobial, anti-inflammatory, antitumor, antimalarial, antioxidant, and insecticide effects. In this study, we reviewed the research progress in the chemical constituents and pharmacological activities of Ajania, aiming to provide reference for the further research and development of Ajania.

The pulmonary pharmacokinetics and anti-inflammatory effect of anemoside B4 after intratracheal and intravenous administration / 药学学报

Anemoside B4 (B4), a main triterpenoid saponin from a traditional Chinese medicine plant, Pulsatilla chinensis, is a novel anti-inflammatory agent for protection from acute lung injury. We investigated the pulmonary availability and anti-inflammatory efficacy of B4 after intratracheal and intravenous dosing with a view to evaluating the suitability of inhalation delivery. All animal studies were performed under the guidelines approved by the Animal Care and Use Committee of Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences (Approval No: SLXD-20181113046). In vitro evaluation of the aerodynamic characteristics and droplet size distribution showed that the aerosols generated by a commercially available nebulizer were well deposited in the respiratory tract. Following intratracheal administration, B4 underwent pulmonary absorption into the bloodstream, rendering an absolute bioavailability of 103%. Compared to intravenous delivery, intratracheal administration dramatically increased the drug availability in lung tissue of rats by more than 1 000-fold, leading to improved and prolonged concentrations of B4 in lung tissue up to 48 h. In addition, the intratracheal administration of B4 resulted in dose-dependent and prolonged anti-inflammatory efficacy in a lipopolysaccharide (LPS)-induced lung injury model in mice. The present results demonstrate that inhalation delivery of B4 is a promising approach to treat pulmonary inflammation with once-daily dosing.

The ethyl acetate extraction of Pileostegia tomentella (ZLTE) exerts anti-cancer effects on H1299 cells via ROS-induced canonical apoptosis / 中国天然药物

Lung cancer is the leading cause of cancer death and the most common malignant tumor, the long-term survival of which has stagnated in the past several decades. Pileostegia tomentella Hand. Mazz is a traditional Chinese medicine called "Zhongliuteng" (ZLT) in the pharmacopeia, which has been proved to possess a potent anti-tumor effect on various cancers. In this study, the effects of ZLT N-butanol extraction (ZLTN) and ZLT ethyl acetate extraction (ZLTE) on the viability of non-small cell lung cancer cell (NSCLC) lines H1299 and A549 were evaluated. Here, we firstly reported that ZLTE significantly inhibited H1299 cells growth without affecting the release of lactate dehydrogenase (LDH). In addition, ZLTE induced caspase-dependent apoptosis in a concentration-dependent manner and increased the expression cleaved-PARP and decreased pro-caspase-3, pro-caspase-7, pro-caspase-8, and pro-caspase-9. Moreover, ZLTE increased the level of cellular reactive oxygen species (ROS) in H1299 cells to lead to apoptosis, which was reversed by N-acetyl-cysteine (NAC). Taken together, our results revealed that ZLTE induced caspase-dependent apoptosis via ROS generation, suggesting that ZLTE is a promising herbal medicine for the treatment of NSCLC.

Application of metabolomics and related technologies in research and development field of traditional Chinese medicine / 中国中药杂志

Internal environment of metabolism of traditional Chinese medicine (TCM) is a dynamic process, which is in line with the "holistic-dynamic-comprehensive-analytic" characteristics of metabonomics, therefore metabonomics have a unique advantage to reveal the metabolic pattern of TCM. The application of metabonomics in TCM has great practical significance in understanding the pharmacodynamic/toxic effect material basis, mechanisms and guiding for determination of dosage and treatment course; At the same time, the scientific compatibility of TCM prescription, the germplasm resources of TCM and the preclinical safety/toxicity can be widely researched. At present, metabolomics has become a leading technology in many industries and fields including the research and development of TCM. The core of metabolomics is analytical technology, because comprehensive metabolite profiles or accurate identification of known metabolites can be obtained from complex biological samples only by appropriate analytical techniques. At the same time, a series of bioinformatics/chemical informatics/stoichiometry methods are needed to process the data, so as to obtain the potential law and information in the mass data. In this paper, the concept of metabolomics, relevant analytical techniques, data processing methods and applications were explained and analyzed clearly. In addition, the core problems and countermeasures of metabolomics were summarized, and the future development of metabolomics was prospected as well.

In vivo metabolism of three coumarins from Chimonanthi Radix based on UHPLC-QTOF-MS/MS / 中国中药杂志

Scopolin (SC-1), scopoletin (SC-2) and isofraxidin (IS-1) are the main active constituents in Chimonanthi Radix. However, the in vivo metabolism of SC-1, SC-2 and IS-1 have not been comprehensively clarified. In this study, the in vivo metabolic profiles of these three coumarins in the rat plasma, urine and feces were analyzed. Ultra-high performance liquid chromatography-quadrupole time of flight mass spectrometry (UHPLC-QTOF-MS/MS) method was applied to characterize the prototypes and metabolites of SC-1, SC-2 and IS-1 in rat feces, urine, and plasma after intravenous administration. A total of 11 metabolites of the three parent compounds were tentatively identified. The main metabolic pathways were analyzed by identification of metabolites, and it was found that these three coumarins underwent multiple in vivo metabolic reactions including glucuronidation, sulfonation, isomerism and reduction. In this study, the analysis of metabolites of three coumarins basically demonstrated their in vivo metabolic process, providing basis for the further pharmacokinetics and pharmacological evaluations of SC-1, SC-2 and IS-1.

Three new triterpenoids isolated from the aerial parts of Ilex cornuta and protective effects against HO-induced myocardial cell injury / 中国天然药物

In the present study, three new triterpenoids, 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-α-L-arabinopyranoside (1), 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (2), and urs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (3), and a known triterpenoid, 3β-hydroxy-urs-2, 18-dien-28-oic acid (4, randialic acid B), were isolated from the aerial parts of Ilex cornuta. Their structures were identified by the spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, and 1D and 2D NMR) and chemical reactions. Compound 4 showed significant cell-protective effects against HO-induced H9c2 cardiomyocyte injury. Compounds 1-4 did not show any significant DPPH radical scavenging activity.

Antioxidant and cardioprotective effects of Ilex cornuta on myocardial ischemia injury / 中国天然药物

Previous studies have indicated that the Ilex genus exhibits antioxidant, neuroprotective, hepatoprotective, and anti-inflammatory activities. However, the pharmacologic action and mechanisms of Ilex cornuta against cardiac diseases have not yet been explored. The present study was designed to investigate the antioxidant and cardioprotective effects of Ilex cornuta root with in vitro and in vivo models. The anti-oxidative effects of the extract of Ilex cornuta root (ICR) were measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging and MTT assays as well as immunoassay. Furthermore, a rat model of myocardial ischemia was established to investigate the cardioprotective effect of ICR in vivo. Eight compounds were isolated and identified from ICR and exhibited DPPH free-radical scavenging activities. They also could increase cell viability and inhibit morphological changes induced by HO or NaSO in H9c2 cardiomyocytes, followed by increasing the SOD activities and decreasing the MDA and ROS levels. In addition, it could suppress the apoptosis of cardiomyocytes. In the rat model of myocardial ischemia, ICR decreased myocardial infarct size and suppressed the activities of LDH and CK. Furthermore, ICR attenuated histopathological alterations of heart tissues and the MDA levels, while increasing SOD activities in serum. In conclusion, these results suggest that ICR has cardioprotective activity and could be developed as a new food supplement for the prevention of ischemic heart disease.

Dissolution difference of ginsenosides from ultrafine granular powder and common powder traditional pieces of Panacis Quinquefolii Radix in vitro / 中国中药杂志

The dissolution of Panacis Quinquefolii Radix ultrafine granular powder and common powder, traditional pieces in water and simulated gastric juice in vitro was compared, and the effect of particles size of Panacis Quinquefolii Radix on the dissolution was studied. HPLC method was used for determination of five ginsenosides including Rg1, Re, Rb1, Rc and Rd from ultrafine granular powder and common powder, traditional pieces of Panacis Quinquefolii Radix at different points in time, furthermore, the dissolution curves of Panacis Quinquefolii Radix ultrafine granular powder and common powder, traditional pieces were obtained. The dissolution characteristics of the three Panacis Quinquefolii Radix forms were also compared in this study. According to the results, the dissolution rates of ginsenosides from ultrafine granular powder exceeded 90% of the total content with 5 min, significantly higher than that of the other two forms in water in vitro. At the same time, the dissolved amount of the ultrafine granular powder was fourteen percent higher than that of the traditional pieces and eight percent higher than that of the common powder. Under the condition of simulated gastric juice in vitro, the dissolution rates of ginsenosides from ultrafine granular powder were little lower than that of the other two, but the maximum dissolved amount of the former was fourteen percent higher than that of the common powder and five percent higher than that of the extracts. Therefore the conclusion is that micronization of Panacis Quinquefolii Radix contributed to dissolution of effective components.

Effects of ultrahigh pressure extraction on yield and antioxidant activity of chlorogenic acid and cynaroside extracted from flower buds of Lonicera japonica / 中国天然药物

The present study was designed to establish and optimize a new method for extracting chlorogenic acid and cynaroside from Lonicera japonica Thunb. through orthogonal experimental designl. A new ultrahigh pressure extraction (UPE) technology was applied to extract chlorogenic acid and cynaroside from L. japonica. The influential factors, including solvent type, ethanol concentration, extraction pressure, time, and temperature, and the solid/liquid ratio, have been studied to optimize the extraction process. The optimal conditions for the UPE were developed by quantitative analysis of the extraction products by HPLC-DAD in comparison with standard samples. In addition, the microstructures of the medicinal materials before and after extraction were studied by scanning electron microscopy (SEM). Furthermore, the extraction efficiency of different extraction methods and the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities of the extracts were investigated. The optimal conditions for extracting chlorogenic acid and cynaroside were as follows: ethanol concentration, 60%; extraction pressure, 400 MPa; extraction time, 2 min; extraction temperature, 30 °C; and the solid/liquid ratio, 1 : 50. Under these conditions, the yields of chlorogenic acid and cynaroside were raised to 4.863% and 0.080%, respectively. Compared with other extraction methods, such as heat reflux extraction (HRE), ultrasonic extraction (UE), and Sohxlet extraction (SE), the UPE method showed several advantages, including higher extraction yield, shorter extraction time, lower energy consumption, and higher purity of the extracts. This study could help better utilize L. japonica flower buds as a readily accessible source of natural antioxidants in food and pharmaceutical industries.

Identification and characterization of two new xanthones from Cudrania fruticosa / 中国天然药物

The present study was designed to investigate the chemical constituents of the roots of Cudrania fruticosa Wight. Compounds were isolated by various column chromatographic methods including silica gel, polyamide, sephadex LH-20, and semi-preparative HPLC. Their structures were elucidated by a combination of 1D and 2D NMR techniques, mass spectrometry, and chemical methods. Two new xanthones, Cudraxanthone T and U (1-2), along with four known compounds (3-6) were isolated from the roots of Cudrania fruticosa Wight.

A high-performance liquid chromatography with circular dichroism detector for determination of stereochemistry of 6, 9-oxygen bridge dibenzocyclooctadiene lignans from kadsura coccinea / 中国天然药物

The stereochemistry of two 6, 9-oxygen bridge dibenzocyclooctadiene lignans from Kadsura coccinea, are difficult to separate and very unstable. The present study was designed to develop a high-performance liquid chromatography using circular dichroism detection for the analysis of the stereochemistry. A new 6, 9-oxygen bridge dibenzocyclooctadiene lignans named Kadsulignan Q was firstly found with an S-biphenyl configuration. The other compound was identified as Kadsulignan L with an R- biphenyl configuration. In order to obtain kinetic data on their reversible interconversion, the stability was measured at different deuterated solvents such as deuterated methanol, deuterated chloroform and deuterated dimethylsulfoxide. The lignans were more unstable and converted more easily in deuterated methanol than in deuterated chloroform and deuterated dimethylsulfoxide.

Determination of equilibrium solubility and n-octanol/water partition coefficient of pulchinenosiden D by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To determine the equilibrium solubility of pulchinenosiden D in different solvents and its n-octanol/water partition coefficients.</p><p><b>METHOD</b>Combining shaking flask method and high performance liquid chromatography (HPLC) to detect the n-octanol/water partition coefficients of pulchinenosiden D, the equilibrium solubility of pulchinenosiden D in six organic solvents and different pH buffer solution were determined by HPLC analysis.</p><p><b>RESULT</b>n-Octanol/water partition coefficients of pulchinenosiden D in different pH were greater than zero, the equilibrium solubility of pulchinenosiden D was increased with increase the pH of the buffer solution. The maximum equilibrium solubility of pulchinenosiden D was 255.89 g x L(-1) in methanol, and minimum equilibrium solubility of pulchinenosiden D was 0.20 g x L(-1) in acetonitrile.</p><p><b>CONCLUSION</b>Under gastrointestinal physiological conditions, pulchinenosiden D exists in molecular state and it has good absorption but poor water-solubility, so increasing the dissolution rate of pulchinenosiden D may enhance its bioavailability.</p>

Chemical constituents from roots of Psammosilene tunicoides / 中国中药杂志

Three compounds, including a new one (1), were isolated from the roots of Psammosilene tunicoides. Based on analysis of NMR data as well as their physical and chemical properties, their structures were elucidated as 3,3'-(4,5-dimethoxynaphthalene-2,7-diyl) bis (1-nitropropan-1-one) (1), alpha-spinasterol-3-O-beta-D-glucopyranoside (2) and alpha-spinasteryl-3-O-beta-D-glucoside-6'-O-palmitate(3). Compounds 2 and 3 were isolated from this genus for the first time.

Study on intestinal absorption of formononetin in Millettia nitita var. hirsutissima in rats / 中国中药杂志

To use the single-pass intestine perfusion (SPIP) model and HPLC to determine the concentration of formononetin, the effect of quality concentrations of formononetin, different intestinal segments and P-glycoprotein inhibitor on intestinal absorption of formononetin, in order to observe the intestinal absorption mechanism of formononetin from Millettia nitita var. hirsutissima in rats. The experimental results showed that the qulaity concentration of formononetin in the perfusate had no significant effect on the absorption rate constant (K(a)) and the apparent absorption coefficient (P(app)); K(a) and P(app) of formononetin in duodenum, jejunum and ileum showed no significant difference. However, K(a) was significantly higher than that in colon (P < 0.05), with significant difference between that in intestinum tenue and colon. P-glycoprotein inhibitor verapamil showed significant difference in K(a) and P(app) in intestinal segments (P < 0.05). This indicated that the absorption mechanism of formononein in rat intestinal tracts passive diffusion, without any saturated absorption. Formononein is absorbed well in all intestines. Their absorption windows were mainly concentrated in the intestinum tenue, without specific absorption sites. Formononein may be the substrate of P-glycoprotein.

Chemical constituents of Psammosilene tunicoides and bacteriostatic activity / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents and bacteriostatic activity of Psammosilene tunicoides.</p><p><b>METHOD</b>Such methods as silica gel column chromatography and gel column chromatography were adotped separate and purify the compounds, and their structures were indentified on the basis of their spectral data and physicochemical properties.</p><p><b>RESULT</b>Ten compounds were separated from ethanol extracts and identified as methyl-4-hydroxybenzoate (1), N-methylsaccharin (2), 3-hydroxy-4-methoxybenzoic acid (3), germanicol (4), tricosanoic acid (5), octacosane (6), amber acid (7), succinic acid (8), stellarine A (9), and oleanane-12-ene-3alpha, 16alpha-two hydroxy-23,28-acid (10).</p><p><b>CONCLUSION</b>All compounds except compound 10 were separated from P. tunicoides for the first time. Compounds 8 and 9 showed the bacteriostatic activity to a certain extent.</p>

Two new phenolic glycosides from the stems of Clematis parviloba / 药学学报

To study the chemical constituents of the stems of Clematis parviloba, six compounds were isolated from a 95% ethanol extract by using a combination of various chromatographic techniques including column chromatography over silica gel, ODS, Sephadex LH-20, and semi-preparative HPLC. Two new phenolic glycosides, 2-((E)-3-carboxybut-2-en-yl)-4-hydroxy-3-methyl-phenyl-O-beta-D-glucopyranoside (1) and 4'-hydroxy-phenol-beta-D-[6-O-(4"-hydroxy-3", 5"-dimethoxy-benzoate)] glucopyranoside (2) were isolated, together with a known phenolic glycoside, 4'-hydroxy-3'-methoxy-phenol-beta-D-[6-O-(4"-hydroxy-3", 5"-dimethoxy-benzoate)] glucopyranoside (3) as well as three known megastigmane glycosides, linarionoside A (4), linarionoside C (5), and staphylionoside K (6). Their structures were determined on the basis of spectroscopic analysis and chemical evidence. Among them, compounds 1 and 2 were named as clemaparvilosides A (1) and B (2), respectively, and compounds 3-6 were obtained from Clematis genus for the first time.

Studies on lignan constituents of Clematis parviloba / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of the stems of Clematis parviloba.</p><p><b>METHOD</b>The compounds were isolated and purified by repeated column chromatography with silica gel, Sephadex LH-20 and HPLC. Their structures were identified by spectroscopic data together with physical and chemical property.</p><p><b>RESULT</b>Ten compounds have been isolated from the stems of C. parviloba, and identified as: (+) pinoresionol (1), (+) pinoresionol-4'-O-p-D-glucopyranoside (2), ( +) pinoresionol4, 4'-O-bis-beta-D-glucopyranoside (3), (-) syringaresinol (4), (+) syringaresinol-4'-O-beta-D-glucopyranoside (5), (-)episyringaresinol (6), (+) medioresinol-4'-O-beta-D-glucopyranoside (7), (+) lariciresinol-4-O-beta-D-glucopyranoside (8), (+) lariciresinol-4'-O-beta-D-glucopyranoside (9), (+) lariciresinol-4, 4'-O-bis-beta-D-glucopyranoside (10), respectively.</p><p><b>CONCLUSION</b>Compounds 6, 7 were isolated from this genus for the first time, and the other ones were isolated from this plant for the first time.</p>

Amides from the stems of Uvaria kweichowensis / 药学学报

Uvaria kweichowensis is a folk nongovernmental herb used to treat cure inflammation and tumour in the Southwest area of China. During the course of our investigation for antitumour agents from the stems of Uvaria kweichowensis, six amides were obtained by means of solvent extraction, chromatography on silica gel and Sephadex LH-20 repeatedly. And their structures were identified as uvariadiamide (1), cepharanone (2), aristololactam A II (3), enterocarpam II (4), aristololactam A Ia (5), and 4,5-dioxodehydroasimilobine (6) on the basis of chemical methods and spectral analyses (EI-MS, 1H NMR, 13C NMR). Among them, compound 1 is a new compound; the other compounds were obtained from this plant for the first time.

A new glycoside from Alpinia officinarum / 药学学报

<p><b>AIM</b>To investigate the glycosidic constituents in the rhizomes of Alpinia officinarum Hance.</p><p><b>METHODS</b>The isolation and purification of glycosides were done with column chromatography on macro porous resin, polyamides and Sephadex LH-20, whilst the structure elucidation was done by HRCI-MS and NMR (1D and 2D) methods.</p><p><b>RESULTS</b>A glycosidic ester identified as 4'-hydroxy-2'-methoxyphenol-beta-D-{6-0-[4"-hydroxy-3", 5"-dimethoxy (benzoate)]}-glucopyranoside (I), along with a known compound n-butyl-beta-D-fructopyranoside (II), were isolated and characterized.</p><p><b>CONCLUSION</b>I was found to be a new compound, named as alpinoside A, whilst II was isolated from the genus Alpinia for the first time.</p>

Study on HPLC fingerprint of different growing areas on fructus aurantii fried with bran / 中国中药杂志

<p><b>OBJECTIVE</b>To establish a method for HPLC fingerprint determination of different growing areas on Fructus Aurantii fried with bran.</p><p><b>METHOD</b>HPLC chromatographic experiment was carried out by ultrasonic distilment of acetacetic ester, gradient elution mode and the detection wavelength of 320 nm. The column temperature was set at 30 degrees C, and flow rate is 1.0 mL x min(-1). Naringin served as the reference standard. Ten batches of Fructus Aurantii fried with bran in the different places were analyzed. Similarity evaluation system for chromatographic fingerprint of TCM proceeded the evaluation, The correlation coefficients between ten batches were used to define the similarity.</p><p><b>RESULT</b>There were eleven characteristic peaks in Fructus Aurantii fried with bran by HPLC fingerprint which constituted fingerprint characters. Both the reproducibility and stability on HPLC fingerprint were proper.</p><p><b>CONCLUSION</b>The method was accurate and simple. It can be applied to the analysis on Fructus Aurantii fried with bran. The fingerprint spectrum can be used to distinguish Fructus Aurantii fried with bran and to be its quality control.</p>