Total Lactones Research Articles

The pharmacokinetics study of ginkgolide A, B and the effect of food on bioavailability after oral administration of ginkgolide extracts in beagle dogs.

Ginkgolides are the primarily active components in Ginkgo products that are popular worldwide. However, few studies have evaluated the bioavailability of ginkgolides and the effects of food on it after oral administration of ginkgolides. In this article, pharmacokinetics and absolute bioavailability of the primary components in ginkgolide extracts were evaluated in beagle dogs. For the first time, we showed that the fed dogs had significantly increased area under the concentration-time curve and peak concentration relative to the fasted dogs based on the data from both the prototype form and total lactones of ginkgolide A (GA) and ginkgolide B (GB). In terms of the free form of the prototype ginkgolides, the absolute bioavailabilities of GA and GB were 34.8 and 5.2% in the fasted dogs, respectively, which significantly increased to an average of 78.6 and 17.0%, respectively, in the fed dogs. In terms of acidified total lactones, the absolute bioavailabilities of GA and GB were 7.5 and 14.5% in the fed dogs, and the percentages declined to 4.1 and 3.7% in the fasted dogs, respectively. It was suggested that administration of ginkgolides after meals could promote the in vivo exposure and the bioavailability of GA and GB, and hence potentially enhance therapeutic outcomes.

Exploration of rapidly determining quality of traditional Chinese medicines by (NIR) spectroscopy based on internet sharing mode

Because of the numerous varieties of herbal species and active ingredients in the traditional Chinese medicine(TCM),the traditional methods employed could hardly satisfy the current determination requirements of TCM.The present work proposed an idea to realize rapid determination of the quality of TCM based on near infrared(NIR)spectroscopy and internet sharing mode. Low cost and portable multi-source composite spectrometer was invented by our group for in-site fast measurement of spectra of TCM samples. The database could be set up by sharing spectra and quality detection data of TCM samples among TCM enterprises based on the internet platform.A novel method called as keeping same relationship between X and Y space based on K nearest neighbors(KNN-KSR for short)was applied to predict the contents of effective compounds of the samples. In addition,a comparative study between KNN-KSR and partial least squares(PLS)was conducted. Two datasets were applied to validate above idea:one was about 58 Ginkgo Folium samples samples measured with four near-infrared spectroscopy instruments and two multi-source composite spectrometers,another one was about 80 corn samples available online measured with three NIR instruments. The results show that the KNN-KSR method could obtain more reliable outcomes without correcting spectrum.However transforming the PLS models to other instruments could hardly acquire better predictive results until spectral calibration is performed. Meanwhile,the similar analysis results of total flavonoids and total lactones of Ginkgo Folium samples are achieved on the multi-source composite spectrometers and near-infrared spectroscopy instruments,and the prediction results of KNN-KSR are better than PLS. The idea proposed in present study is in urgent need of more samples spectra, and then to be verified by more case studies.

Antidiabetic effect of ligustilide-rich total lactones derived from Shunaoxin dropping pills on mice with type 2 diabetes induced by a high-fat diet and streptozotocin

Shunaoxin dropping pill, a well-known Traditional Chinese Medicine formula, has been used to treat cerebrovascular diseases in China since 2005.

Quantitative and qualitative evaluation on tablets of Ginkgo biloba leaves using fingerprint and LC-MS analysis

A reasonable method for the quality control of tablets of Ginkgo biloba leaves was established in this paper. The total flavonol glycosides and terpene lactones of G. biloba tablets were quantified by HPLC. Totally, 16 batches of the commercially available tablets of G. biloba leaves were determined. Among of them, 2 batches were unqualified in the content of total flavonol glycosides, and 3 batches were unqualified in the content of terpene lactones. A validated HPLC fingerprint method was established to evaluate the commercially available tablets of G. biloba leaves with the assistance of LC-MS. Sixteen batches showed the similarity of 0.763-0.989. There were 31 fingerprint chromatogram peaks were identified as flavonoids compositions by LC-MS. This provides a research idea for the quality control of tablets of G. biloba leaves.

Evaluation of the anaphylactoid potential of Andrographis paniculata extracts using the popliteal lymph node assay and P815 cell degranulation in vitro

BackgroundThe anaphylactoid reactions induced by andrographis injection have repeatedly been reported. The aim of our study was to evaluate the immuno-sensitizing potential of extracts from Andrographis paniculata Nees and to screen for the constituent that is responsible for inducing the anaphylactoid reaction.MethodsIn the direct popliteal lymph node assay (D-PLNA), female BALB/c mice were randomly divided into several groups with ten mice per group according to the experiment design, the right hind footpads of mice received a single subcutaneous injection of Andrographis paniculata (50 μl), and the left hind footpads received the same volume of vehicle. Seven days later, the mice were sacrificed by cervical dislocation, and the popliteal lymph nodes from both the left and right sides were removed. The weight (WI) and cellularity indices (CI) of the popliteal lymph nodes (PLNs) were then calculated, and the pathological changes of the PLNs were measured. In addition, P815 mast cells were collected for the in vitro cell degranulation experiment. The level of histamine, the percentage of cell degranulation and the ratio of ammonia glycosidase released were measured to further evaluate the potential allergenicity.ResultsAlcohol extract (AEE), ethyl acetate extract (EAE) and n-butanol extract (NBE) significantly increased the weight (WI > 2) and cell number (CI > 5) of PLNs (P < 0.05, P < 0.01). Additionally, all the three monomers of andrographis, namely NAD, AND, and DDA, significantly increased the weight (WI > 2) and cell number (CI > 5) of the PLNs (P < 0.05, P < 0.01). In the cell model, all of the different extract fractions (AEE, EAE and NBE) and the three monomers of andrographis markedly elevated the level of histamine, the percentage of cell degranulation and the ratio of ammonia glycosidase released.ConclusionThe diterpene lactone compounds of Andrographis paniculata Nees (total lactones of andrographolide) may have a potential sensitizing capacity in andrographis injection.

Preparation of hydrophilic matrix sustained release tablets of total lactones from Andrographis paniculata and study on its in vitro release mechanism

In this study, hydrophilic matrix sustained release tablets of total lactones from Andrographis paniculata were prepared and the in vitro release behavior were also evaluated. The optimal prescription was achieved by studying the main factor of the type and amount of hydroxypropyl methylcellulose (HPMC) using single factor test and evaluating through cumulative release of three lactones. No burst drug release from the obtained matrix tablets was observed. Drug release sustained to 14 h. The release mechanism of three lactones from A. paniculata was accessed by zero-order, first-order, Higuchi and Peppas equation. The release behavior of total lactones from A. paniculata was better agreed with Higuchi model and the drug release from the tablets was controlled by degradation of the matrix. The preparation of hydrophilic matrix sustained release tablets of total lactones from A. paniculata with good performance of drug release was simple.

Ultrasonic-Assisted Extraction of Total Flavonoids and Lactones from Ginkgo Biloba Powder

This article aims to study the extraction conditions of the total flavonoids and lactones from the ginkgo biloba powder. First, the influencing factors and levels for the extraction were determined by the single factor method, and then the optimum extraction conditions were optimized by orthogonal experimental design. The results showed that the optimal conditions for ultrasonic extraction of the total flavonoids were as follows: 2mg cellulase and 0.1g raw material (ginkgo biloba powder) were dissolved in 10ml water solution. The pH of the solvent was 4.5 adjusted with hydrochloric acid. The materials were extracted in ultrasound bath at 55°C for 40min. The optimal conditions for ultrasonic extraction of the total lactones were as follows: 7mg cellulase and 0.1g raw material were dissolved in 10ml water solution with pH 4.9. The raw materials were extracted at 50°C for 35min. Under the optimum conditions, the peak area contents were nearly 90% and 58% for total flavonoids and lactones, respectively.

A Validated Fourier Transform Infrared Spectroscopy Method for Quantification of Total Lactones in Inula racemosa and Andrographis paniculata

Fourier transform infrared (FT-IR) spectroscopy is a technique widely used for detection and quantification of various chemical moieties. This paper describes the use of the FT-IR spectroscopy technique for the quantification of total lactones present in Inula racemosa and Andrographis paniculata. To validate the FT-IR spectroscopy method for quantification of total lactones in I. racemosa and A. paniculata. Dried and powdered I. racemosa roots and A. paniculata plant were extracted with ethanol and dried to remove ethanol completely. The ethanol extract was analysed in a KBr pellet by FT-IR spectroscopy. The FT-IR spectroscopy method was validated and compared with a known spectrophotometric method for quantification of lactones in A. paniculata. By FT-IR spectroscopy, the amount of total lactones was found to be 2.12 ± 0.47% (n = 3) in I. racemosa and 8.65 ± 0.51% (n = 3) in A. paniculata. The method showed comparable results with a known spectrophotometric method used for quantification of such lactones: 8.42 ± 0.36% (n = 3) in A. paniculata. Limits of detection and quantification for isoallantolactone were 1 µg and 10 µg respectively; for andrographolide they were 1.5 µg and 15 µg respectively. Recoveries were over 98%, with good intra- and interday repeatability: RSD ≤ 2%. The FT-IR spectroscopy method proved linear, accurate, precise and specific, with low limits of detection and quantification, for estimation of total lactones, and is less tedious than the UV spectrophotometric method for the compounds tested. This validated FT-IR spectroscopy method is readily applicable for the quality control of I. racemosa and A. paniculata.

Near Infrared Spectroscopic Examination of Charred Pine Wood, Bark, Cellulose and Lignin: Implications for the Quantitative Determination of Charcoal in Soils

The objective of this research was to investigate the effect of charring on near infrared spectra of materials likely to be present in forest fires in order to determine the feasibility of determining charred carbon in soils. Four materials (cellulose, lignin, pine bark and pine wood) and char from these materials created by charring for various durations (1 to 168 h) and at various temperatures (200 to 450°C) were studied. Near infrared spectra and measures of acidity (total acids, carboxylic acids, lactones and phenols as determined by titration) were available for 56 different samples (Not all samples charred at all temperatures/durations). Results showed spectral changes that varied with the material, temperature and duration of charring. Examination of spectra and correlation plots indicated that changes in the constituents of the materials in question, such as loss of OH groups in carbohydrates, rather than direct determination of typical products produced by charring, such as carboxylic acids, lactones and phenols, were the basis for the spectral changes. Finally, while the spectral changes resulting from charring appeared to be relatively unique to each material, PLS calibrations for total acids, carboxylic acids, lactones and phenols were successfully created (with R2 of 0.991, 0.943, 0.931 and 0.944, respectively) indicating that there is a sufficient commonality in the changes to develop calibrations without the need for unique calibrations for each specific set of charring conditions (i.e. material, temperature and time of heating).

Effects of cold storage on aroma compounds of white- and yellow-fleshed peaches

The stir bar sorptive extraction (SBSE) technique was used to determine volatile constituents in two peach cultivars, one yellow-fleshed (cv. Spring Lady) and one white-fleshed (cv. Regina Bianca). For both cultivars four distinct experimental samples were considered, each formed by fruits obtained with four different cultivation practices. In order to investigate the effects of cold storage on the volatile profile, on all peach experimental samples changes in aroma compounds after 1 and 2 weeks of storage at 1°C, plus 1 day at ambient temperature, were monitored; moreover, only on the four experimental samples from cv. Regina Bianca, the effect of a prestorage hot water treatment (46°C for 25 min) was also evaluated. On the isolate obtained by SBSE, 24 compounds were identified and quantified by GC-MS: saturated and unsaturated lactones, aldehydes, C13 norisoprenoids, monoterpenes, alcohols and esters. The profile of the white-fleshed cultivar was characterised by a higher level of C13 norisoprenoids, and, in particular, of 8,9-dehydrotheaspirone. In all experimental samples after 1 week of storage, plus 1 day at ambient temperature, a marked increase (on average by 89%) in total lactones was observed. This increase was due to a noticeable accumulation of saturated lactones with longer side chains (γ- and δ-decalactone) and unsaturated lactones ((Z)-dec-7-en-5-olide and γ-jasmolactone). Peaches analysed after 2 weeks of storage showed total lactone levels close to those detected in the samples at harvest, suggesting that increasing storage times reduced fruit ability to accumulate these character impact compounds of peach aroma. A similar effect of cold storage, although less marked, was also observed on C13 norisoprenoid fraction, but only on cv. Regina Bianca. On the other hand, we did not find univocal effects of cold storage on C6 aldehydes, whereas linalool, detected only in samples of cv. Spring Lady at harvest, disappeared quickly during the first days of storage. In samples of cv. Regina Bianca peaches subjected to hot water treatment, after 1 week of storage, lactone level was significantly reduced in comparison with untreated fruits, denoting a possible inhibition effect on lactone accumulation and on aroma development.

LC-UV and LC-MS analysis of food and drink products containing kava

A method for the determination of six kava lactones, methysticin, dihydromethysticin, kawain, dihydrokawain, yangonin and desmethoxyyangonin, in solid foods and beverages has been developed. Solid samples were prepared using methanol extraction, while beverages were extracted using a separate solid phase extraction (SPE) method. After sample preparation, the extracts were analysed using LC-UV or atmospheric pressure photoionization (APPI) LC-MS in the positive mode. Using the method, 10 beverage products, two chocolate products, three unbrewed tea products, three dietary supplements and a drink mix product were analysed. The results obtained using the LC-UV were comparable to those obtained using APPI-LC-MS for most products. Using the SPE method in conjunction with LC-MS, individual kava lactones were detected in drink products at ppb concentrations. Concentrations of total kava lactones ranged between 135–0.035 mg per serving in the food and beverage products tested and between 40–61 mg per serving for the dietary supplement products tested. Results of these analyses as well as extraction efficiency and reproducibility data are reported.

Analysis of terpenelactones in Ginkgo biloba by high performance liquid chromatography and evaporative light scattering detection.

A reversed phase HPLC method permitting the determination of 5 terpenelactones in Ginkgo biloba, without the need of any sample preparation is presented in this paper. The compounds were successfully separated within 25 min by using a C-12 column, an evaporative light scattering (ELS) detector and a mobile phase comprising of ammonium acetate buffer, methanol and isobutanol. All terpenelactones were detectable at concentrations as low as 20.3 microg/ml. The analysis of G. biloba market products showed remarkable variations in the lactone content, and more than 2 fold differences in the suggested daily doses of the total lactones, from 8.84 mg to 18.28 mg, respectively.

Structure of isobadkhysin. The stereochemistry of badkhysin and isobadkhysin

1. By chromatography of the total lactones obtained from the sodium carbonate treatment of the resin of the roots ofFerula oopoda (Boiss. et Buhse) Boiss. we isolated a previously unstudied sesquiterpene lactone C20H24O5, mp 189–190° C, which we called isobadkhysin.