Emodin elicits cytotoxicity in human lung adenocarcinoma A549 cells through inducing apoptosis

This study investigated the mechanism of the cytotoxic effect of emodin, an active anthraquinone, on human lung adenocarcinoma A549 cells. In vitro growth inhibition and suppression on colony forming were used to evaluate the effects of emodin on A549 cells. Emodin’s ability in changing the expressions of apoptosis-related genes was studied by real-time RT-PCR. Emodin could significantly inhibit the growth of A549 cells with IC₅₀ = 16.85 μg/ml (~60 μM). It also concentration dependently inhibited the colony-forming ability of A549 cells with IC₅₀ = 7.60 μg/ml (~30 μM). Hallmarks of apoptosis, such as single-strand DNA breakage and DNA fragmentation, were observed in A549 cells treated with emodin. Emodin (72 h) treatment could up-regulate the gene expression of FASL (p < 0.05) and down-regulate the gene expression of C-MYC (p < 0.01), but induce no significant changes in the gene expressions of MCL1, GAPDH, BAX and CCND1. These results suggest that emodin could induce growth inhibition and apoptosis in A549 cells through modifying the extrinsic apoptotic pathways and the induction of cell cycle arrest.     

中药大黄的生化学研究ⅩⅫ蒽醌衍生物对兔肾髓质Na+-K+-ATP酶活性的抑制和利尿作用

家兔实验表明:大黄素、大黄酸以30 mg/kg的剂量灌胃给药,2～4h后尿量、排Na⁺和K⁺量达最高峰,比对照组明显增多。而芦荟大黄素和大黄酚的作用较弱。大黄素、大黄酸和芦荟大黄素对免肾髓质Na⁺-K⁺-ATP酶活性有较强的竞争性抑制作用。     

Inhibitory effect of selected medicinal plants on the release of pro-inflammatory cytokines in lipopolysaccharide-stimulated human peripheral blood mononuclear cells

The inhibitory activities of the methanol extracts from 20 selected medicinal plants on the release of pro-inflammatory cytokines in human peripheral blood mononuclear cells (PBMCs) were evaluated. The major compound from the most active plant extract was also investigated. The inhibitory effect of the methanol extracts on the release of pro-inflammatory cytokines was tested by incubating PBMCs with the sample and then stimulating by lipopolysaccharide at 0.1 μg/ml. The level of cytokines was determined using enzyme-linked immunosorbent assay. Among the extracts tested, Andrographis paniculata extract demonstrated the strongest inhibition of interleukin (IL)-1β, IL-1α, and IL-6 release, with IC₅₀ values of 1.54, 1.06, and 0.74 μg/ml, respectively. The IC₅₀ value of A. paniculata extract was significantly higher than that of andrographolide on IL-1α, IL-1β, and IL-6 (p < 0.001) release. The IC₅₀ values of andrographolide for IL-1α, IL-1β, and IL-6 were significantly higher (p < 0.001) than that of dexamethasone. Cymbopogon citratus and Zingiber officinale strongly inhibited the release of IL-1β, with IC₅₀ values of 3.22 and 3.17 μg/ml, respectively. To our knowledge, this is the first report that A. paniculata extract and its major compound andrographolide strongly inhibited the release of IL-1α, whereas previous studies only showed their inhibitory effect on the release of another IL-1 family member, IL-1β. The results show that these extracts and this compound have potential effects as anti-inflammatory agents by inhibiting the release of pro-inflammatory cytokines.     

Protein tyrosine phosphatase 1B inhibitory activity of Indonesian herbal medicines and constituents of Cinnamomum burmannii and Zingiber aromaticum

We screened water and methanol extracts of 28 Indonesian medicinal plants for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Nine water extracts, i.e., Alstonia scholaris leaf, Blumea balsamifera, Cinnamomum burmannii, Cymbopogon nardus, Melaleuca leucadendra, Phyllanthus niruri, Piper nigrum, Syzygium aromaticum, and Sy. polyanthum, exhibited ≥70 % inhibition at 25 μg/mL, whereas 11 methanol extracts, i.e., Als. scholaris, Andrographis paniculata, B. balsamifera, Ci. burmannii, Curcuma heyneana, Glycyrrhiza glabra, M. leucadendra, Punica granatum, Rheum palmatum, Sy. polyanthum, and Z. aromaticum, exhibited ≥70 % inhibition at 25 μg/mL. Water extracts of B. balsamifera (IC₅₀, 2.26 μg/mL) and M. leucadendra (IC₅₀, 2.05 μg/mL), and methanol extracts of Ci. burmannii (IC₅₀, 2.47 μg/mL), Pu. granatum (IC₅₀, 2.40 μg/mL), and Sy. polyanthum (IC₅₀, 1.03 μg/mL) exhibited strong inhibitory activity, which was comparable with that of the positive control, RK-682 (IC₅₀, 2.05 μg/mL). The PTP1B inhibitory activity of the constituents of Ci. burmannii and Z. aromaticum was then evaluated. 5′-Hydroxy-5-hydroxymethyl-4″,5″-methylenedioxy-1,2,3,4-dibenzo-1,3,5-cycloheptatriene (2; IC₅₀, 29.7 μM) and trans-cinnamaldehyde (5; IC₅₀, 57.6 μM) were the active constituents of Ci. burmannii, while humulatrien-5-ol-8-one (21; IC₅₀, 27.7 μM), kaempferol-3,4′-di-O-methyl ether (32; IC₅₀, 17.5 μM), and (S)-6-gingerol (33; IC₅₀, 28.1 μM) were those of Z. aromaticum. These results suggest that these medicinal plants may contribute to the treatment and/or prevention of type II diabetes and/or obesity through PTP1B inhibition.     

In vitro and in vivo antioxidant activity of Symplocos cochinchinensis S. Moore leaves containing phenolic compounds

Methanol extract of Symplocos cochinchinensis S. Moore leaves was evaluated for its in vitro and in vivo antioxidant activity. The total phenolic content of the extract was 230 mg of gallic acid equivalents/g extract. The extract showed very good scavenging activity on 2,2-diphenyl-picrylhydrazyl (DPPH) (IC₅₀ 620.30 ± 0.14 μg/ml), hydroxyl (IC₅₀ 730.21 ± 1.05 μg/ml), nitric oxide (IC₅₀ 870.31 ± 0.19 μg/ml) radicals, as well as high reducing power. The extract also showed strong suppressive effect on lipid peroxidation. In in vivo study CCl₄ induced oxidative stress produced significant increase in SGOT, SGPT and LDH levels along with reduction in liver SOD, CAT, GSH and GPx levels. Pre-treatment of rats with the extract (250 and 500 mg/kg) for 7 days showed significant reduction in the levels of SGOT, SGPT and LDH compared to CCl₄ treated rats. SOD, CAT, GSH and GPx levels were increased significantly due to treatment with the extract. The activity of the extract was comparable to the standard drug, silymarin (25 mg/kg). The results suggest that the leaves of S. cochinchinensis are a source of natural antioxidants.     

Chemical constituents from the roots of Feroniella lucida

A new furanocoumarin named lucidafuranocoumarin A (7) together with 13 known coumarins (1–6, 8–14) and four known alkaloids (15–18) was isolated from the roots of Feroniella lucida. Their structures were elucidated on the basis of spectroscopic analysis. Some of the isolates were evaluated for their biological activities, and compound 18 showed strong cytotoxicity against KB (IC₅₀ = 0.637 μg/ml) and NCI-H187 (IC₅₀ = 0.094 μg/ml) human cancer cell lines, antimalarial activity against Plasmodium falciparum (IC₅₀ = 0.336 μg/ml), and antituberculosis activity against Mycobacterium tuberculosis (MIC = 6.25 μg/ml).     

Simultaneous analysis and peroxynitrite-scavenging activity of galloylated flavonoid glycosides and ellagic acid in Euphorbia supina

The herbs of Euphorbia supina (Euphorbiaceae) have been used to treat hemorrhage, chronic bronchitis, hepatitis, jaundice, diarrhea, gastritis, and hemorrhoids as a medicinal herb. This work is aimed to qualitatively and quantitatively analyze the polyphenols with peroxynitrite-scavenging activities. The eight compounds: gallic acid, methyl gallate, avicularin, astragalin, juglanin, isoquercitrin 6″-gallate, astragalin 6″-gallate, and ellagic acid, were isolated from E. supina and used for HPLC analysis and peroxynitrite (ONOO^?)-scavenging assay. Simultaneous analysis of the eight compounds was performed on MeOH extract and its fractions. The contents in MeOH extract and peroxynitrite-scavenging activities of the dimer of gallic acid, ellagic acid (15.64 mg/g; IC₅₀ 0.89 μM), and two galloylated flavonoid glycosides, astragalin 6″-gallate (13.72 mg/g; IC₅₀ 1.43 μM) and isoquercitrin 6″-gallate (16.99 mg/g; IC₅₀ 1.75 μM), were high, compared to other compounds. The legendary uses of E. supina could be attributed to the high content of polyphenols, particularly ellagic acid, isoquercitrin 6″-gallate, and astragalin 6″-gallate as active principles.     

Emodin inhibits ATP-induced IL-1β secretion,ROS production and phagocytosis attenuation in rat peritoneal macrophages via antagonizing P2X7 receptor

Context: Previous in vitro studies have demonstrated that emodin (1,3,8-trihydroxy-6-methyl-anthraquinone), an anthraquinone derivative from the rhizome of Rheum palmatum L., can inhibit the activation of P2X₇ receptors (P2X₇R) as a potential antagonist. However, the effects of emodin on P2X₇R-related inflammatory processes remain unclear.

Objective: This study aimed to investigate the effects of emodin on different inflammation responses of macrophages induced by ATP, the natural ligand of P2X₇R.

Materials and methods: Rat peritoneal macrophages were treated with millimolar ATP and emodin (0.1, 0.3,?1,?3,?10?µM) or brilliant blue G (BBG, 0.1,?1,?10?µM). Cytosolic Ca²⁺ concentration ([Ca²⁺]_c) was detected by fluorescent Ca²⁺ imaging. Interleukin-1β (IL-1β) release was measured by rat IL-1β ELISA kits. Reactive oxygen species (ROS) generation was examined by dihydroethidium (DHE) fluorescent staining. Phagocytic activity was tested by neutral red uptake assay.

Results: We found that the [Ca²⁺]_c increase evoked by ATP (5?mM) was inhibited by emodin, in a dose-dependent manner with IC₅₀ of 0.5?μM. Furthermore, emodin reduced the IL-1β release induced by ATP (2?mM) in lipopolysaccharide (LPS)-activated macrophages, with an IC₅₀ of 1.6?μM. Emodin also strongly suppressed the ROS production and phagocytosis attenuation triggered by ATP (1?mM), with IC₅₀ values of 1?μM and 0.7?μM, respectively. Besides, BBG, a specific antagonist of P2X₇R, exhibited similar suppressive effects on these inflammation responses.

Conclusion: These results showed the inhibitory effects of emodin on ATP-induced [Ca²⁺]_c increase, IL-1β release, ROS production and phagocytosis attenuation in rat peritoneal macrophages, by inhibiting the activation of P2X₇R.     

Antioxidant activity and total phenolic content of ethanolic extract of Caesalpinia bonducella seeds

The aim of this study was to assess the in vitro potential of ethanolic extract of Caesalpinia bonducella seeds as a natural antioxidant. The DPPH activity of the extract (20, 40, 50, 100 and 200 μg/ml) was increased in a dose dependent manner, which was found in the range of 38.93–74.77% as compared to ascorbic acid (64.26–82.58%). The IC₅₀ values of ethanolic extract and ascorbic acid in DPPH radical scavenging assay were obtained to be 74.73 and 26.68 μg/ml, respectively. The ethanolic extract was also found to scavenge the superoxide generated by EDTA/NBT system. Measurement of total phenolic content of the ethanolic extract of C. bonducella was achieved using Folin–Ciocalteau reagent containing 62.50 mg/g of phenolic content, which was found significantly higher when compared to reference standard gallic acid. The ethanolic extract also inhibited the hydroxyl radical, nitric oxide, superoxide anions with IC₅₀ values of 109.85, 102.65 and 89.84 μg/ml, respectively. However, the IC₅₀ values for the standard ascorbic acid were noted to be 70.79, 65.98 and 36.68 μg/ml respectively. The results obtained in this study clearly indicate that C. bonducella has a significant potential to use as a natural antioxidant agent.     

Bioactive triterpenoids from Atriplex lasiantha

Chromatographic purification of the ethyl acetate soluble fraction from the methanolic extract of Atriplex lasiantha yielded a new triterpenoid, 7β,15α,16β-trihydroxyolean-12-ene-28,30-dioic acid-3-O-β-d-xylopyranoside (1), along with two known triterpenoids, rotundifolioside I (2) and corchorusin B (3). Structures of the compounds 1–3 were elucidated through sophisticated NMR studies and high resolution mass spectrometry. The three isolates (1–3) were evaluated for antibacterial, antioxidant, and antiurease activities. Compound 2 exhibited the best antibacterial activity against Escherichiacoli with IC₅₀ value of 66.25 μg/ml, whereas, all the tested compounds exhibited antioxidant (IC₅₀ values of 68.7–75.4 μg/ml) and antiurease (IC₅₀ values of 25.5–49.3 μg/ml) activities, respectively.     

In vitro cytotoxicity, α-glucosidase inhibition,antioxidant, and free radical scavenging activities of Illicium griffithii Hook. f. & Thoms fruits

Illicium griffithii is a medicinal tree species of the temperate broad-leaved forests of North East India; its fruits are used in the pharmaceutical and spice industries. The fruits are used medicinally to treat cough, sinusitis, toothache, regurgitating, dyspepsia, abdominal pain, and food poisoning and are considered carminative, stomachic, and glactagogic. The present study was aimed to evaluate the cytotoxicity, α-glucosidase inhibitory potential, antioxidant, and free radical scavenging activities of hexane, ethyl acetate, and methanol extracts of I. griffithii fruits. Ethyl acetate extract (EAE) exhibited 78.7 % toxicity at the dose of 500 μg/ml with IC₅₀ value of 300 μg/ml against A549 human adenocarcinoma lung cancer cell line, 50 % α-glucosidase inhibition at 810.32 ± 1.28 μg/ml concentration, and potent scavenging activity at 1,000 μg/ml on DPPH (91.12 % ± 2.08), CUPRAC (2.384 ± 0.03), reducing power (0.847 ± 0.02), lipid peroxidation (55.52 % ± 1.56), hydroxyl (75.83 % ± 1.47), and DMPD (76.12 % ± 1.35). It additionally showed maximum activity at 300 μg/ml on total antioxidant activity (0.290 ± 0.04 GAE mg/g) and FRAP (2.150 ± 0.23 mM Fe²⁺/g). The results demonstrated that EAE possessed marked activity in all the tested biological parameters. On further fractionation, EAE gave an active fraction F3. Two phenolic compounds were isolated and identified (3,4-dihydroxybenzoic acid and 3,4,5-trihydroxybenzoic acid) from this fraction for the first time. I. griffithii showed promising cytotoxic and antioxidant activities.     

Essential oil composition and antioxidant activities of Curcuma aromatica Salisb.

The chemical composition of the hydro-distilled essential oil from leaves of Curcuma aromatica Salisb. was analysed by GC–MS. Twenty-three compounds representing 94.29% of the total oil were identified. The antioxidant activities of the oil and various extracts of C. aromatica were evaluated by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radical-scavenging assays. The oil and methanol extract showed potent DPPH radical-scavenging activities (IC₅₀ = 14.45 and 16.58 μg/ml, respectively), which were higher than butylated hydroxyanisole (IC₅₀ = 18.27 μg/ml). The extracts also exhibited remarkable superoxide radical-scavenging activities (IC₅₀ = 22.6–45.27 μg/ml) and the activity in the methanol extract was superior to all other extracts (IC₅₀ = 22.6 μg/ml). Furthermore, the amount of total phenolic compounds was determined and its content in ethyl acetate extract was the highest as compared to other extracts. The results indicate that the oil and extracts of C. aromatica could serve as an important bio-resource of antioxidants for using in the food industries.     

Antiproliferative activity of Solanum lycocarpum alkaloidic extract and their constituents, solamargine and solasonine, in tumor cell lines

Natural products are some of the important sources of new anticancer drugs. The Brazilian flora is considered one of the most diverse in the word, although not many large-scale pharmacological and phytochemical studies have been conducted to date. With this in mind, in the present study we evaluated the antiproliferative activity of Solanum lycocarpum fruit glycoalkaloid extract (SL) and its major compounds, solamargine (SM) and solasonine (SS), against different tumor cell lines: murine melanoma (B16F10), human colon carcinoma (HT29), human breast adenocarcinoma (MCF-7), human cervical adenocarcinoma (HeLa), human hepatocellular liver carcinoma (HepG2) and human glioblastoma (MO59J, U343 and U251). The antiproliferative activity was evaluated using XTT assay and results were expressed as IC₅₀. The most pronounced antiproliferative activity was observed for SM, with IC₅₀ values ranging from 4.58 to 18.23 μg/mL. The lowest IC₅₀ values were observed against HepG2, being 9.60 μg/mL for SL, 4.58 μg/mL for SM and 6.01 μg/mL for SS. Thus, SL, SM and SS demonstrated antiproliferative activity against the tumor cell lines tested, and were most effective against the HepG2 cell line.     

Phyllanthus emblica (Amla) methanolic extract regulates multiple checkpoints in 15-lipoxygenase mediated inflammopathies: Computational simulation and in vitro evidence

Amla (Phyllanthus emblica) has long been used in traditional folk medicine to prevent and cure a variety of inflammatory diseases. In this study, the antioxidant activity (DPPH scavenging and reducing power), anti-inflammatory activity (RBC Membrane Stabilization and 15-LOX inhibition), and anticoagulation activity (Serin protease inhibition and Prothrombin Time assays) of the methanolic extract of amla were conducted. Amla exhibited a substantial amount of phenolic content (TPC: 663.53 mg GAE/g) and flavonoid content (TFC: 418.89 mg GAE/g). A strong DPPH scavenging effect was observed with an IC₅₀ of 311.31 µg/ml as compared to standard ascorbic acid with an IC₅₀ of 130.53 µg/ml. In reducing power assay, the EC₅₀ value of the extract was found to be 196.20 µg/ml compared to standard ascorbic acid (EC₅₀ = 33.83 µg/ml). The IC₅₀ value of the RBC membrane stabilization and 15-LOX assays was observed as 101.08 µg/ml (IC₅₀ of 58.62 µg/ml for standard aspirin) and 195.98 µg/ml (IC₅₀ of 19.62 µg/ml for standard quercetin), respectively. The extract also strongly inhibited serine protease (trypsin) activity with an IC₅₀ of 505.81 µg/ml (IC₅₀ of 295.44 µg/ml for standard quercetin). The blood coagulation time (PTT) was found to be 11.91 min for amla extract and 24.11 min for standard Warfarin. Thus, the findings of an in vitro study revealed that the methanolic extract of amla contains significant antioxidant, anti-inflammatory, and anticoagulation activity. Furthermore, in silico docking and simulation of reported phytochemicals of amla with human 15-LOXA and 15-LOXB were carried out to validate the anti-inflammatory activity of amla. In this analysis, epicatechin and catechin showed greater molecular interaction and were considerably stable throughout the 100 ns simulation with 15-lipoxygenase A (15-LOXA) and 15-lipoxygenase B (15-LOXB) respectively.     

中药大黄的生化学研究.ⅪⅩ.蒽醌衍生物对线粒体呼吸链的抑制部位

本实验结果表明:大黄素、大黄酸和芦荟大黄素是线粒体呼吸链电子传递的抑制剂。(1)三药对NADH脱氢酶有不同程度的抑制作用,(2)大黄素对琥珀酸脱氢酶有较强的抑制作用,而大黄酸和芦荟大黄素对此酶仅有轻微的抑制作用;(3)三药对辅酶Q-细胞色素C还原酶及细胞色素C氧化酶也仅有轻微的抑制作用;(4)动力学观察表明:三药对NADH脱氢酶的抑制均为竞争性的。     

Anti-inflammatory,antioxidant and anti-acetylcholinesterase activities of <Emphasis Type="Italic">Bouvardia ternifolia</Emphasis>: potential implications in Alzheimer’s disease

Bouvardia ternifolia has been used medicinally to treat inflammation. In the present study, we investigate the anti-Alzheimer’s potential effect of the hydroalcoholic extract of B. ternifolia through evaluation of anti-inflammatory and antioxidant activities, quantification of the percentage inhibition of acetylcholinesterase activity, protection effect against β-amyloid fibrillar-induce neurotoxicity, and the identification of the main constituents. Our results show that B. ternifolia extract and ethyl acetate fraction induced anti-inflammatory effects by reducing inflammation by >70 %, while antioxidant test revealed significant IC₅₀ values for flavonoid content fraction (30.67 ± 2.09 μg/ml) and ethyl acetate fraction (42.66 ± 0.93 μg/ml). The maximum inhibition of acetylcholinesterase was exhibited by scopoletin content fraction (38.43 ± 3.94 %), while ethyl acetate fraction exerted neuroprotective effect against β-amyloid peptide (83.97 ± 5.03 %). Phytochemical analysis, showed the presence of 3-O-quercetin glucopyranoside (415 mg/g), rutin (229.9 mg/g), ursolic and oleanolic acid (54 and 20.8 mg/g respectively), 3-O-quercetin rhamnopyranoside (12.8 mg/g), chlorogenic acid (9.5 mg/g), and scopoletin (1.38 mg/g). Our findings support the use of B. ternifolia since the extract induced significant neuroprotection against β-amyloid peptide, anti-inflammatory, antioxidant and anti-acetylcholinesterase effects that could be attributed to its contents of polyphenols, coumarins, and triterpenes, and encourage further studies for development of this extract as therapeutic agent in treatment of Alzheimer’s disease.     

Chemical compositions,antifungal and antioxidant activities of essential oil and various extracts of Melodorum fruticosum L. flowers

This research presents the chemical composition antifungal and antioxidant activities of essential oils and various extracts from Melodorum fruticosum flowers. The essential oil composition of M. fruticosum flowers were investigated by GC–MS with 88 identified volatile constituents. Phenyl butanone, linalool, benzyl alcohol, α-cadinol, globulol and viridiflorol were found to be the major components, respectively. The dichloromethane extract played a major role as a remarkable fungicide according to their inhibition action against all tested pathogens followed by hexane extract, essential oil and methanol extract, respectively, along with their respective MIC values ranging from 125 to 1000 μg/ml. The dichloromethane extracts were also evaluated to be superior to all extracts tested with an IC₅₀ value of 87.6 μg/ml whereas other extracts showed their IC₅₀ values ranging from 100.13 to 194.50 μg/ml.     

Antimalarial and free radical scavenging activities of rhizomes of Polygonatum verticillatum supported by isolated metabolites

Antimalarial activity of the crude extract of Polygonatum verticillatum rhizomes and its sequentially partitioned fractions were investigated against Plasmodium falciparum. The crude extract possessed notable activity (IC₅₀: 21.67?μg/mL) that enhanced reasonably upon fractionation. The antiparasitic potency of the n-hexane fraction was maximum (IC₅₀: 2.33?μg/mL) followed by chloroform (IC₅₀: 4.62?μg/mL). However, the remaining fractions showed insignificant activity in the assay. The extracts of the plant showed marked scavenging activity on stable free radical, DDPH. The most potent antioxidant was the chloroform fraction (IC₅₀: 90?μg/mL) followed by ethyl acetate (IC₅₀: 93?μg/mL) and n-butanol (IC₅₀: 95?μg/mL) fractions. In the brine shrimps lethality test, the extracts were found nontoxic with the exception of ethyl acetate fraction (LD₅₀: 492.846?μg/mL). The bioactivity-guided isolation resulted into 5-hydroxymethyl-2-furaldehyde (HMF) and diosgenin which strongly supports the present experimental findings.     

Two New Flavonoid Glycosides from Viscum album ssp. album

Rheum ribes Linn (Polygonaceae) root is used traditionally to treat diabetes, hemorrhoids, ulcers, and diarrhea. Here, the hypoglycemic effect of R. ribes root extract in healthy mice was investigated. Fasted mice were given a single dose of 50?mg/kg of three extracts of different polarity from R. ribes by gastric feeding and the blood glucose was measured 0, 1, 2, 4, and 24?h later. The aqueous extract showed a significant hypoglycemic effect. In vitro, the aqueous extract stimulated insulin release from INS-1E cells at both stimulatory (20?mM) and non-stimulatory (1?mM) glucose concentrations, thus suggesting a mechanism for the in vivo effect. The hypoglycemic active fraction was found to contain anthraquinone glycosides of aloe emodin, emodin, physcion, and chrysophanol derivatives.     

New cyclomyrsinol diterpenes from Euphorbia aellenii with their immunomodulatory effects

Chloroform–acetone extract of the aerial parts of Euphorbia aellenii Rech. f. (Euphorbiaceae) was investigated for its diterpenoidal constituents. This led to the isolation of two new and one known cyclomyrsinol-type diterpenes 1–3. The structures were elucidated on the basis of 1D and 2D ¹H and ¹³C NMR techniques, and in vitro immunomodulatory activity was evaluated by standard proliferation of human peripheral blood lymphocytes. Results showed that all the three compounds were found to inhibit lymphocyte proliferation significantly (p < 0.05) at 50 μg/ml concentration. Among them, compound 2 showed more activity against phytohemagglutinin-activated T-cell proliferation with an IC₅₀ of 40.4 ± 9.35 μg/ml.