Cl Extract Research Articles

A randomised placebo-controlled clinical trial of curcuma longa extract for treating symptoms and effusion-synovitis of knee osteoarthritis

Purpose: Pharmacological therapies are limited, associated with off-target effects, are frequently contraindicated, and only modestly effective for pain in osteoarthritis (OA). Effusion and synovitis are common in OA and are associated with symptomatic and structural progression of OA. Curcuma longa (CL, or Turmeric) extract has anti-inflammatory effects and is gaining popularity in the treatment of OA despite the lack of high-quality evidence. The CurKOA trial aimed to compare the efficacy of CL extract versus placebo for treating knee pain and effusion-synovitis in an inflammatory phenotype of OA identified using ultrasound scan.

고구마껍질 주원료인 식물 혼합물의 RAW264.7 대식세포에서 면역활성 증진효과

This study aimed to investigate the immunostimulatory effect of a sweet potato peel-based plant mixture, including Platycodon grandiflorum, Codonopsis lanceolata and corn silk, on RAW264.7 macrophages. We tested the immunostimulatory effect of 12 plant extracts, individually, in terms of nitric oxide (NO) production in RAW264.7 macrophages. NO production of Platycodon grandiflorum, Codonopsis lanceolata, and corn silk extracts (PG, CL, CS) in RAW264.7 macrophages was significantly higher than that of other plant extracts (p<0.05). The cytotoxicity and production of NO and cytokines by PG, CL, CS, and weet potato peel extract (SP) in RAW264.7 macrophages were determined. The production of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 in PG, CL or CS-treated RAW264.7 macrophages was significantly higher than that of SP-treated ones (p<0.05). Immunostimulatory effect of the extract from plant mixture containing Platycodon grandiflorum, Codonopsis lanceolata, corn silk, and sweet potato peel in the ratio 1:1:0.5:3 (w/w) was significantly higher than that of SP extract alone, and was similar or higher than that of PG, CL, and CS, on RAW264.7 macrophages (p<0.05). Therefore, the extract from plant mixture may be considered as a potential candidate for the development of functional food materials for enhancing immune activity.

Indirect determination of chlorine and fluorine in eye shadow by ion chromatography after an eco-friendly sample preparation method based on combustion reaction

A powerful and efficient method for indirect determination of chlorine and fluorine in eye shadow is described in this work. The presence of these elements should be controlled in eye cosmetics because of its allergenic properties. The proposed method combines the analyte volatilization from eye shadow based on combustion reaction and the indirect determination of Cl and F by ion chromatography as chloride (Cl−) and fluoride (F−). To achieve better combustion conditions as well as to improve the volatilization of Cl and F from the sample matrix (which is mostly inorganic), microcrystalline cellulose was evaluated as a volatilization aid. The central composite rotatable design was used to optimize the sample mass and volatilization aid mass to be used in the microwave-induced combustion. Afterward, water or ammonium carbonate solutions (50, 100 or 150 mmol L−1) were evaluated for Cl and F absorption. Using the selected conditions (200 mg of eye shadow, 400 mg of microcrystalline cellulose, and water as absorbing solution) recoveries for Cl and F were 100 ± 8% and 106 ± 7%, respectively. Moreover, a mixture containing the certified reference material MESS-4 (marine sediment), microcrystalline cellulose and the sample was prepared by microwave-induced combustion, and no significant difference was observed between the result obtained for Cl (11,269 ± 325 mg kg−1) and the certified value (13,100 ± 4400 mg kg−1). The proposed method showed suitable trueness, precision (the repeatability and the intermediate precision was always lower than 7%) and limits of detection (LODs) for Cl (60 mg kg−1) and F (20 mg kg−1). Extraction of Cl and F from eye shadow assisted by ultrasound was also evaluated; however, the Cl and F recoveries were not quantitative and the LODs were considerably high. To the best of our knowledge, this is the first work demonstrating a reliable method for multielement determination in eye shadow, which is safe, presents low generation of laboratory effluents and may be considered an efficient approach for routine analysis in cosmetic industry.

EFFICACY AND SAFETY OF CURCUMA LONGA EXTRACT IN THE TREATMENT OF OSTEOARTHRITIS: A SYSTEMATIC REVIEW

Objective: Osteoarthritis (OA) is a chronic disease caused by inflammation of the tissue and bony structure of the joint, which affects more than 235 million people worldwide. Due to the adverse effects caused by the long-term use of standard treatment of OA, the attempt to find natural remedies to treat chronic diseases continues to rise. Curcuma longa is known to have anti-inflammatory effects, which may impact the pathophysiology of OA. While many randomized controlled trials show the efficacy of Curcuma longa extract in the treatment of OA, there has been no comprehensive review of this evidence.
 Methods: We systematically searched PubMed, Cochrane, Scopus, ProQuest, EBSCOhost, and ScienceDirect for randomized controlled trials that evaluated Curcuma longa extract (CE extract) vs. control (placebo or other therapy). Three trials were identified. Data were then extracted from the studies and summarized descriptively.
 Results: Across all trials, Curcuma longa therapy was proven to reduce Visual Analog Scale (VAS) and Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) scores significantly compared to the control group. Adverse effects were less likely to appear in patients treated with Curcuma longa extract compared to other groups.
 Conclusion: CL extract is beneficial as an alternative medication for OA treatment, shown by the reduced scores of the Visual Analog Scale (VAS) and WOMAC in all studies we reviewed.

New possibilities for pharmaceutical excipients analysis: Combustion combined with pyrohydrolysis system for further total chlorine determination by ICP-OES

An alternative method for the determination of total chlorine content in hydroxypropyl cellulose (HPC) was applied, combining a recently developed system based on a combustion step followed by pyrohydrolysis reaction. Using this approach it the determination of total chlorine by inductively coupled plasma optical emission spectrometry (ICP-OES) without interferences was feasible. It overcame the limitations of European Pharmacopoeia (EP) method for HPC analysis regarding to the inability to determine total chlorine in HPC, once some chlorine compounds (e.g., chloroform) that can not be identified by the official method (EP). The following parameters of combustion and pyrohydrolysis were evaluated: absorbing solution, sample mass, the use of powdered silica as retardant of combustion, oxygen flow rate and reaction time. Reference values for total chlorine were obtained after digestion using microwave-induced combustion and determination by ion chromatography (IC). Microwave-assisted extraction (MAE) was also investigated for Cl extraction. The accuracy of the proposed method was also evaluated by analyte recovery tests (agreement of 95–103%), as well as by the analysis of certified reference materials (CRMs). The agreement with the certified values was higher than 95% and the limit of quantification (LOQ) was 50 µg g−1. Up to 500 mg of sample were efficiently digested by the proposed method in 5 min (dissolved carbon in digests was below 50 mg L−1). Total chlorine content in samples of modified cellulose ranged from 284 to 576 µg g−1. Despite the relatively high chlorine content in all samples, the concentration was lower than the maximum limit allowed by the EP for HPC (0.5%).

Anti-inflammatory activity of Corylopsis coreana uyeki extracts and isolated compounds by inhibiting nitric oxide and cytokine production

Pharmacognosy Magazine ,2019,15,61,317-321.DOI:10.4103/pm.pm_144_18Published:March 2019Type:Original Article Authors:Jun Yin, HyeSoo Wang, and MinWon Lee Author(s) affiliations:Jun Yin, HyeSoo Wang, MinWon Lee Laboratory of Pharmacognosy and Natural Product Derived Medicine, College of Pharmacy, Chung-Ang University, Seoul, Republic of Korea Abstract:Context: Corylopsis coreana Uyeki (Korean winter hazel) belongs to the Hamamelidaceae family. It is cultivated as an ornamental plant in South Korea. In traditional folk medicine, C. coreana has been used to treat irritated skin and inflammatory diseases. Aims: To study the anti-inflammatory effects of C. coreana Uyeki leaf and bark extracts as well as their major active compounds, we evaluated in vitro levels of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and nitric oxide (NO) using RAW 264.7 macrophages. Materials and Methods: Production of TNF-α and IL-6 cytokines was measured by ELISA assay, and NO inhibitory activity was tested by Griess assay. Results: Extracts of leaves and barks, as well as isolated compounds from these extracts, showed remarkable anti-inflammatory activities by inhibiting NO, TNF-α, and IL-6 cytokine production. In particular, the leaf extract showed more potent inhibitory activities than that of barks. Conclusions: Ellagitannins and flavonoids were probably related to the anti-inflammatory activity of CL (leaves) extract, providing evidence of the anti-inflammatory property of CL. Keywords:Anti-inflammatory ability, Corylopsis coreana uyeki, cytokine production inhibition, interleukin-6, nitric oxide production inhibition, tumor necrosis factor-αView:PDF (1.08 MB)

Acute and sub-chronic toxicity studies of the aqueous extract from leaves of Cistus ladaniferus L. in mice and rats

Ethnopharmacological relevanceCistus ladaniferus L. (C.ladaniferus) (Cistaceae) is an aromatic shrub native to the Mediterranean region. The leaves are widely used in traditional medicine throughout Morocco for the treatment of various diseases including, diabetes, diarrhea, inflammation, and skin ailments. However, to the best of our knowledge, no systematic study concerning its toxicity profile has been reported. Aim of the studyThe study carried out evaluates the potential toxicity of the aqueous extract from leaves of the C.ladaniferus (CL extract) shrub, through the method of acute and sub-chronic oral administration in mice and rats. Materials and methodsDuring the acute toxicity study, male and female mice were orally administrated with CL aqueous extract at single doses of 500, 1000, 2000, 3000 and 5000mg/kg (n = 5/group/sex). Abnormal behavior, toxic symptoms, weight, and death were observed for 14 consecutive days to assess the acute toxicity. During the sub-chronic toxicity study, the aqueous extract was administered orally at doses of 500, 700 and 1000mg/kg (n = 6/group) daily to Wistar rats of both sexes for 90 days. The general behavior of the rats was observed daily, and their body weight was recorded weekly. A urinalysis, biochemical analysis, hematological analysis, macroscopic examination and histopathological examination of several organs were conducted at the end of the treatment period. ResultsDuring the acute toxicity test, when mice were administered doses of 3000 and 5000mg/kg, the CL extract produced a 10–30% mortality rate, respectively, and induced signs of toxicity. However, no mortality or adverse effect was noted at the doses of 1000 and 2000mg/kg. The median lethal dose (LD50) of the extract was estimated to be more than 5000mg/kg. In the subchronic study, the CL extract induced no mortality or treatment-related adverse effects with regard to body weight, general behavior, relative organ weights, urine, hematological, and biochemical parameters. Histopathological examination of vital organs showed normal architecture suggesting no morphological alterations. Moreover, the CL extracts improved lipid profile and exhibited a significant hypoglycemic effect in all doses tested in rats. ConclusionThe results of the present study suggest that treatment with the CL extract for 13 weeks does not appear to produce significant toxicity, except at high dose. Therefore, the use of appropriate levels of the CL extract as a traditional medicine remedies should have a wide margin of safety for its therapeutic use.

Hepatic metabolic effects of Curcuma longa extract supplement in high-fructose and saturated fat fed rats

The metabolic effects of an oral supplementation with a Curcuma longa extract, at a dose nutritionally relevant with common human use, on hepatic metabolism in rats fed a high fructose and saturated fatty acid (HFS) diet was evaluated. High-resolution magic-angle spinning NMR and GC/MS in combination with multivariate analysis have been employed to characterize the NMR metabolite profiles and fatty acid composition of liver tissue respectively. The results showed a clear discrimination between HFS groups and controls involving metabolites such as glucose, glycogen, amino acids, acetate, choline, lysophosphatidylcholine, phosphatidylethanolamine, and β-hydroxybutyrate as well as an increase of MUFAs and a decrease of n-6 and n-3 PUFAs. Although the administration of CL did not counteract deleterious effects of the HFS diet, some metabolites, namely some n-6 PUFA and n-3 PUFA, and betaine were found to increase significantly in liver samples from rats having received extract of curcuma compared to those fed the HFS diet alone. This result suggests that curcuminoids may affect the transmethylation pathway and/or osmotic regulation. CL extract supplementation in rats appears to increase some of the natural defences preventing the development of fatty liver by acting on the choline metabolism to increase fat export from the liver.

Palladium(II) Weak-Link Approach Complexes Bearing Hemilabile N-Heterocyclic Carbene–Thioether Ligands

A new class of homoligated palladium(II) weak-link approach (WLA) complexes bearing hemilabile N-heterocyclic carbene (NHC)-thioether ligands is reported that, unlike previous tweezer-like WLA complexes, expand and contract in a linear fashion when switching between configurational states. These complexes can be chemically switched between a trans open state and a trans closed state via the addition or subsequent extraction of Cl-. These bis(NHC) complexes also display unusual isomerization behavior. For example, an NMR spectroscopic investigation into the solution-state configuration of the open complex reveals the presence of interconverting syn,trans and anti,trans isomers, and a kinetic study shows that the barrier is large enough to isolate, store, and study the anti,trans isomer at room temperature. Notably, the linker length between the NHC and thioether moieties can be tailored with additional -CH2- groups, which affords considerable control over the geometric changes imposed by switching. Therefore, this class of complexes may be useful in the construction of allosterically regulated supramolecular assemblies and materials.

Antimicrobial Activity and Phytochemical Analysis of Organic Extracts from Cleome spinosa Jaqc.

Due to the use of Cleome spinosa Jacq. (Cleomaceae) in traditional medicine against inflammatory and infectious processes, this study evaluated the in vitro antimicrobial potential and phytochemical composition of extracts from its roots and leaves. From leaves (L) and roots (R) of C. spinosa different extracts were obtained (cyclohexane: ChL and ChR; chloroform: CL and CR; ethyl acetate: EAL and EAR, methanol: ML and MR). The antimicrobial activity was evaluated by the broth microdilution method to obtain the minimum inhibitory (MIC) and microbicidal (MMC) concentrations against 17 species, including bacteria and yeasts. Additionally, antimicrobial and combinatory effects with oxacillin were assessed against eight clinical isolates of Staphylococcus aureus. All C. spinosa extracts showed a broad spectrum of antimicrobial activity, as they have inhibited all tested bacteria and yeasts. This activity seems to be related to the phytochemicals (flavonoid, terpenoids and saponins) detected into the extracts of C. spinosa. ChL and CL extracts were the most actives, with MIC less than 1 mg/mL against S. aureus, Bacillus subtilis, and Micrococcus luteus. It is important to note that these concentrations are much lower than their 50% hemolysis concentration (HC50) values. Strong correlations were found between the average MIC against S. aureus and their phenolic (r = −0.89) and flavonoid content (r = −0.87), reinforcing the possible role of these metabolite classes on the antimicrobial activity of C. spinosa derived extracts. Moreover, CL and CR showed the best inhibitory activity against S. aureus clinical isolates, they also showed synergistic action with oxacillin against all these strains (at least at one combined proportion). These results encourage the identification of active substances which could be used as lead(s) molecules in the development of new antimicrobial drugs.

Evaluating coagulant activity of locally available <i>Syzygium cumini</i>, <i>Artocarpus heterophyllus</i> and <i>Moringa oleifera</i> for treatment of community drinking water, Uganda

Most rural communities in Africa are without access to treated water and therefore use the readily available unsafe water sources exposing them to water borne diseases. This calls for the need for action to search for affordable and simple solutions. This research therefore examined the effectiveness of readily available natural coagulants Syzygium cumini (Javaplum), Artocarpus heterophyllus (Jackfruit) and Moringa oleifera (Moringa) using ‘Jar Test’. Water turbidity and coliforms removal from community drinking water by seeds extracts of natural coagulants was examined. Turbidity removal increased with coagulants concentration in (solvents extracts water and NaCl). Optimal turbidity removal occurred at 40 mg/l coagulant concentration with low and medium turbidity raw water for both solvents extracts and at 60 mg/l for Na Cl extract with high turbidity water. Compared to alum [KAl (SO 4 ) 2 .12(H 2 O)], the turbidity removal effectiveness was: alum> Moringa oleifera > Artocarpus heterophyllus > Syzygium cumini , except for 1MNaCl extract where it was: alum> Artocarpus heterophyllus > Moringa oleifera > Syzygium cumini .Optimal turbidity removal was: Moringa oleifera 97.7%, Artocarpus heterophyllus 95.8% and Syzygium cumini 94.1%. The seed extracts were also effective as water disinfectants (Moringa>Jackfruit>Java plum). The use of Jackfruit and Java plum and Moringa, for water treatment is recommended. © 2015 International Formulae Group. All rights reserved. Keywords: Coagulant activity, Artocarpus heterophyllus , Moringa oleifera , Syzygium cumini , community drinking water treatment, turbidity removal

Efficacy of Curcuma longa in osteoarthritis: Association of IL-1β, IL-10 and MMP-9 with severity of disease

Abstract Osteoarthritis (OA) is a progressively debilitating immune mediated inflammatory disorder in which various biomarkers have been reportedly increased. This study was carried out to establish a correlation between IL-1β, IL-10 and MMP-9 in various grades of OA of knee and to observe the effect of Curcuma longa (CL-an indigenous drug) in such patients through a randomized, placebo controlled, double blind trial. After obtaining clearance from Institutional Ethics Committee, 160 patients of either sex aged between 40 to 80 years, meeting the inclusion and exclusion criteria, were enrolled and randomly divided in two groups. The grading of the disease was done according to Kellgren-Lawrence (KL) grading scale. Placebo and extract of CL were given along with the standard treatment to the two groups in blind manner. The assessment of the patients was done after two and four months. On day 0 the level of IL-1β, MMP-9 and IL-10 was found to be significantly higher in grade 3 and 4 patients as compared to grade 1 and 2 patients. After oral administration of CL extract there was significant clinical improvement (as compared to placebo) in all grades of patients as adjudged by WOMAC score and VAS. There was also significant decrease in levels of IL-1β and MMP-9 in parallel with the clinical improvement. Moreover, decline in the level of IL-10, after treatment with CL was not significant. It is concluded that IL-1β, MMP-9 and IL-10 have strong parallel association with severity of OA. Further, CL produced significant relief in the patients of OA of knee, when given along with standard treatment.

Comparative evaluation of five plant extracts and juices for nanoiron synthesis and application for hexavalent chromium reduction

The effectiveness of five plant extracts and juices, i.e. extracts of Camellia sinensis (green tea, GT), Syzygium aromaticum (clove, CL), Mentha spicata (spearmint, SM), Punica granatum juice (pomegranate, PG) and Red Wine (RW), for the production of nanoiron suspensions and their application for Cr(VI) reduction was investigated. Polyphenols contained in extracts act as reducing agents for iron ions in aqueous solutions, forming thus iron nanoparticles, and stabilize the nanoparticles produced from further oxidation and agglomeration. The maximum amount of polyphenols extracted per g of herbs was obtained at herb mass to water volume ratio varying from 10 to 20g/L. Suspensions of nanoparticles with sizes below 60nm were produced by mixing iron chloride solution with the plant extracts and juices investigated. The maximum concentration of nanoiron in suspensions was estimated to 22mM, obtained using RW and PG at a mixing ratio of iron solution to extract equal to 2. Lower concentrations, up to 18mM, were achieved using GT and CL extracts. Therefore, PG juice and RW were considered as more effective for nanoiron production, and, together with GT extracts, they were selected for the production of nanoiron suspensions, which have been proven effective for Cr(VI) reduction, reaching removal capacity as high as 500mg Cr(VI) per g of iron in nanoparticles.

On a snow cover composition in the vicinity of the Verkhnekamsky Salt Deposit

The snow cover chemical composition was investigated on the territory of the Verkhnekamskiy potash-magnesium salt deposit in the zone of influence of atmospheric emissions of Berezniki Potash Mining Complex (Perm Region). The object of researches was the snow in this area. Features of specific pollutants contained in the emissions of these mine groups and their relationship with the air intake and following atmospheric deposition were examined. With regard for specific character of pollutants in the emissions, studies of melt water included determination of the following chemical components – SO42-, Cl-, NO3-, NO2-, НCO3-, Ca2+, Mg2+, Na+, K+, of the pH value as well as suspended solid substances, and total mineralization. An analysis of snow composition was performed on two sites from which one was the surrounding background territory, while another area was the urban territory of city Berezniki, i.e. area of operating mine group. To assess the results the indicator of specific stock macro component was used. Increased specific stock relative to the background snowpack is clearly indicative of components directly related to the extraction and processing of salts Cl-, Na+, K+. The revealed anomalies have a local character and, as a rule, do not extend beyond boundaries of sanitary protection zones of the enterprises. Maps of distribution of values of the specific reserves for the analyzed list of components in the melt water were constructed. Our results obtained for the Verkhnekamskiy Deposit area were compared with similar published data on the territories of cities in the zone influenced by motor roads, reserves, and coastal zones of the Russian Arctic seas.

Histological studies of neuroprotective effects of Curcuma longa Linn. on neuronal loss induced by dexamethasone treatment in the rat hippocampus

Long term exposure to dexamethasone (Dx) is associated with brain damage especially in the hippocampus via the oxidative stress pathway. Previously, an ethanolic extract from Curcuma longa Linn. (CL) containing the curcumin constituent has been reported to produce antioxidant effects. However, its neuroprotective property on brain histology has remained unexplored. This study has examined the effects of a CL extract on the densities of cresyl violet positive neurons and glial fibrillary acidic protein immunoreactive (GFAP-ir) astrocytes in the hippocampus of Dx treated male rats. It showed that 21days of Dx treatment (0.5mg/kg, i.p. once daily) significantly reduced the densities of cresyl violet positive neurons in the sub-areas CA1, CA3 and the dentate gyrus, but not in the CA2 area. However, CL pretreatment (100mg/kg, p.o.) was found to significantly restore neuronal densities in the CA1 and dentate gyrus. In addition, Dx treatment also significantly decreased the densities of the GFAP-ir astrocytes in the sub-areas CA1, CA3 and the dentate gyrus. However, CL pretreatment (100mg/kg, p.o.) failed to protect the loss of astrocytes in these sub-areas. These findings confirm the neuroprotective effects of the CL extract and indicate that the cause of astrocyte loss might be partially reduced by a non-oxidative mechanism. Moreover, the detection of neuronal and glial densities was suitable method to study brain damage and the effects of treatment.

Quantifying chloride binding and salt extraction with poly(methyl methacrylate) copolymers bearing aryl-triazoles as anion receptor side chains.

Copolymers of methyl methacrylate and aryl-triazole based anion receptors were quantitatively analyzed. Transfer of structural features (1 : 1 and 2 : 1 complexes) and Cl(-) affinities from the parent receptors was demonstrated. Cl(-)-induced cross-linking changed the polymer's hydrodynamic radius. Extraction of tetrapropylammonium Cl(-) from water to dichloromethane was enhanced over PMMA.

Production of reactive oxygen species in decoupled, Ca2+-depleted PSII and their use in assigning a function to chloride on both sides of PSII

Extraction of Ca(2+) from the oxygen-evolving complex of photosystem II (PSII) in the absence of a chelator inhibits O2 evolution without significant inhibition of the light-dependent reduction of the exogenous electron acceptor, 2,6-dichlorophenolindophenol (DCPIP) on the reducing side of PSII. The phenomenon is known as "the decoupling effect" (Semin et al. Photosynth Res 98:235-249, 2008). Extraction of Cl(-) from Ca(2+)-depleted membranes (PSII[-Ca]) suppresses the reduction of DCPIP. In the current study we investigated the nature of the oxidized substrate and the nature of the product(s) of the substrate oxidation. After elimination of all other possible donors, water was identified as the substrate. Generation of reactive oxygen species HO, H2O2, and O 2 (·-) , as possible products of water oxidation in PSII(-Ca) membranes was examined. During the investigation of O 2 (·-) production in PSII(-Ca) samples, we found that (i) O 2 (·-) is formed on the acceptor side of PSII due to the reduction of O2; (ii) depletion of Cl(-) does not inhibit water oxidation, but (iii) Cl(-) depletion does decrease the efficiency of the reduction of exogenous electron acceptors. In the absence of Cl(-) under aerobic conditions, electron transport is diverted from reducing exogenous acceptors to reducing O2, thereby increasing the rate of O 2 (·-) generation. From these observations we conclude that the product of water oxidation is H2O2 and that Cl(-) anions are not involved in the oxidation of water to H2O2 in decoupled PSII(-Ca) membranes. These results also indicate that Cl(-) anions are not directly involved in water oxidation by the Mn cluster in the native PSII membranes, but possibly provide access for H2O molecules to the Mn4CaO5 cluster and/or facilitate the release of H(+) ions into the lumenal space.

Extracts of Crinum latifolium inhibit the cell viability of mouse lymph oma cell line EL4 and induce activation of anti-tumour activity of macrophages in vitro

Ethnopharmacological relevanceCrinum latifolium L. (CL) leaf extracts have been traditionally used in Vietnam and are now used all over the world for the treatment of prostate cancer. However, the precise cellular mechanisms of the action of CL extracts remain unclear. Aim of the studyTo examine the effects of CL samples on the anti-tumour activity of peritoneal murine macrophages. Materials and methodsThe properties of three extracts (aqueous, flavonoid, alkaloid), one fraction (alkaloid), and one pure compound (6-hydroxycrinamidine) obtained from CL, were studied (i) for redox capacities (DPPH and bleaching beta-carotene assays), (ii) on murine peritoneal macrophages (MTT assay) and on lymphoma EL4-luc2 cells (luciferine assay) for cytotoxicity, (iii) on macrophage polarization (production of ROS and gene expression by PCR), and (iv) on the tumoricidal functions of murine peritoneal macrophages (lymphoma cytotoxicity by co-culture with syngeneic macrophages). ResultsThe total flavonoid extract with a high antioxidant activity (IC50=107.36mg/L, DPPH assay) showed an inhibitory action on cancer cells. Alkaloid extracts inhibited the proliferation of lymphoma cells either by directly acting on tumour cells or by activating of the tumoricidal functions of syngeneic macrophages. The aqueous extract induced mRNA expression of tumour necrosis factor-α (TNF-α), interleukin-1β (IL-1β) and interleukin 6 (IL-6) indicating differentiation of macrophages into pro-inflammatory M1 polarized macrophages. The total flavonoid, alkaloid extracts and an alkaloid fraction induced the expression of the formyl peptide receptor (FPR) on the surface of the polarized macrophages that could lead to the activation of macrophages towards the M1 phenotype. Aqueous and flavonoid extracts enhanced NADPH quinine oxido-reductase 1 (NQO1) mRNA expression in polarized macrophages which could play an important role in cancer chemoprevention. All the samples studied were non-toxic to normal living cells and the pure alkaloid tested, 6-hydroxycrinamidine, was not active in any of the models investigated. ConclusionsOur results indicate that CL extracts and alkaloid fraction (but not pure 6-hydroxycrinamidine) inhibit the proliferation of lymphoma cells in multiple pathways. Our results are in accordance with traditional usage and encourage further studies and in vivo assays.

Echinocystic acid, a metabolite of lancemaside A, inhibits TNBS-induced colitis in mice

The rhizome of Codonopsis lanceolata (CL, family Campanulaceae), of which the main constituent is lancemaside A, has been used for cough and bronchitis in traditional Chinese medicine. To evaluate anti-colitic effect of CL, we examined anti-inflammatory effect of CL extracts, lancemaside A and its metabolites in lipopolysaccharide (LPS)-stimulated peritoneal macrophages and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitic mice. Among CL extracts, CL BuOH extract inhibited LPS-induced IL-1β, IL-6 and TNF-α expression, as well as NF-κB activation most potently. CL BuOH extract also inhibited colon shortening and myeloperoxidase activity in TNBS-induced colitic mice. Among lancemaside A, a main constituent of CL BuOH extract, and its metabolites (lancemaside X, echinocystic acid-3-O-β-d-glucopyranoside and echinocystic acid), echinocystic acid inhibited the expression of the pro-inflammatory cytokines, IL-1β, IL-6, and TNF-α, as well as the phosphorylation of IKKβ and p65 in LPS-stimulated peritoneal macrophages most potently. Echinocystic acid also potently inhibited the binding of LPS to TLR4 on peritoneal macrophages. Lancemaside A and its metabolite, echinocystic acid, inhibited TNBS-induced colonic inflammation, including colon shortening, increased myeloperoxidase activity and pro-inflammatory cytokine expression, and NF-κB activation in mice. The anti-colitic effect of echinocystic acid was superior to that of lancemaside A. Based on these findings, orally administered lancemaside A may be metabolized to echinocystic acid, which may express anti-colitic effect by inhibiting the binding of LPS to TLR4 on the macrophages.

Reversible Photodynamic Chloride-Selective Sensor Based on Photochromic Spiropyran

We report here for the first time on a reversible photodynamic bulk optode sensor based on the photoswitching of a spiropyran derivative (Sp). The photoswitching of Sp induces a large basicity increase in the polymeric phase, which triggers the extraction of Cl– and H+. Cl– is stabilized by a lipophilic chloride-selective ionophore inside the membrane, while H+ binds with the open form of Sp and induces a spectral change, hence providing the sensor signal. The system was studied with spectroscopic and electrochemical methods.