Antimicrobial substances from the rare actinomycete Nonomuraea rhodomycinica NR4-ASC07T

Nonomuraea rhodomycinica NR4-ASC07^T is a rare actinomycete isolated from soil in Sirindhorn peat swamp forest. The crude extract of its culture broth exhibited antimicrobial and anticancer against diverse human pathogens and cancer cells. The chemical investigation of the crude extract led to the isolation of two new metabolites named nonomuric acid (1) and 3-hydroxy deoxydaunorubicinol aglycone (2), along with two known bioactive compounds [ε-rhodomycinone (3) and 7-deoxy-13-dihydrocarminomycinone (4)]. Compounds 1 and 3 showed antimalarial activity with the half maximal inhibitory concentration (IC₅₀) of 8.00 and 8.88 μg mL^?1, respectively. Compound 4 inhibited growth of Mycobacterium tuberculosis and Bacillus cereus at the minimum inhibitory concentrations of 50.0 and 12.50 μg mL^?1, respectively. Every compound exhibited cytotoxicity against cancer cells tested at IC₅₀ ≥ 6.34 μg mL^?1. These finding are the first report of bioactive metabolites produced by strain NR4-ASC07^T, suggesting that rare actinomycetes are yet promising sources for novel drug discovery.     

In vitro biological activity of aromadendrin-4′-methyl ether isolated from root extract of Ventilago madraspatana Gaertn with relevance to anticandidal activity

In this study, antimicrobial and antioxidant activities of the hexane extract of the root of Ventilago madraspatana were evaluated. Based on the significant bioactivity of crude hexane extract, an active compound was purified from the root extract. The active compound was further purified and identified as aromodendrin-4′-methyl ether by the ¹H NMR spectrum. The isolated compound significantly inhibited Staphylococcus epidermidis with the lowest MIC and MBC at 78 μg/mL (P < 0.05). The compound also exhibited significant anticandidal activity with MIC and MBC values of 312 and 625 μg/mL, respectively. The radical scavenging activity of aromodendrin-4′-methyl ether was evident by its lower IC₅₀ values of 60 μg/mL for DPPH scavenging and 3.2 μg/mL for ABTS scavenging. The compound also exhibited ferrous ion chelation and H₂O₂ scavenging activities. The study is an attempt to increase the industrial utility of V. madrasapatana.     

Antioxidant,cholinesterase inhibition activities and essential oil analysis of Nelumbo nucifera seeds

Nelumbo nucifera seeds’ essential oil (EO), crude extract and subsequent fractions were evaluated for their DPPH, ABTS and superoxide anion-free radical scavenging and cholinesterase inhibitory activities. The ethyl acetate fraction and EO showed outstanding antioxidant activities with IC₅₀ values of 191, 450 μg/mL (DPPH), 123, 221 μg/mL (ABTS) and 69, 370 μg/mL (superoxide anion). The ethyl acetate fraction and EO also caused significant inhibition of acetylcholinesterase and butyrylcholinesterase with IC₅₀ values of 70 ± 0.6, 64 ± 0.8 and 75 ± 0.3, 58 ± 0.2, in dose-dependent manner. The first ever gas chromatography–mass spectrometry analysis of the EO obtained from N. nucifera seeds resulted in identification of 19 constituents, mainly comprised of oxygenated sesquiterpenes responsible for their promising bioactivity. The crude and fractions revealed the presence of saponins, flavonoids, steroids, alkaloids, terpenoids and cardiac glycosides in phytochemical investigation.     

GC/MS profiling,in vitro anti-leptospiral and haemolytic activities of Boesenbergia rotunda (L.) Mansf. used as a medicinal plant by Nicobarese of Andaman and Nicobar Islands

Leaves of the plant Boesenbergia rotunda are used by the Nicobarese tribe of Andaman and Nicobar Islands, India, to prepare traditional medicine for treating fever, headache and body ache. In the present investigation, methanol fraction of these leaves were analysed by GC/MS that revealed the presence of 25 compounds. The anti-leptospiral activity of methanol crude extract was determined by both microdilution and macrodilution methods. The MICs of the extract were tested against 24 pathogenic leptospiral strains and ranged between 62.5–125 μg/mL in both microdilution and macrodilution. The range of MBCs was 250 and 500 μg/mL in macrodilution and microdilution respectively. The crude extract was subjected to cytotoxic studies and found to have negligible or no haemolytic activity, exhibiting IC₅₀ values of greater than 4 mg/mL. Further in vivo studies are needed to investigate the pharmacological and toxicological properties of Boesenbergia rotunda, before it can be considered as a new anti-leptospiral agent.     

Urease inhibitory profile of extracts and chemical constituents of Pistacia atlantica ssp. cabulica Stocks

The current study was designed to evaluate the urease inhibitory profile of extract and fractions of Pistacia atlantica ssp. cabulica Stocks followed by bioactivity-guided isolated compounds. The crude extract was found significantly active with urease inhibitor (95.40% at 0.2 mg/mL) with IC₅₀ values of 32.0 ± 0.28 μg/mL. Upon fractionation, ethyl acetate fraction displayed 100% urease inhibition with IC₅₀ values of 19.9 ± 0.51 μg/mL at 0.2 mg/mL. However, n-hexane and chloroform fractions exhibited insignificant urease inhibition. Similarly, the isolated compound, transilitin (1) and dihydro luteolin (2) demonstrated marked urease attenuation with 95 and 98% respectively, at 0.15 mg/mL. Both the isolated compounds showed marked potency with IC₅₀ values of 8.54 ± 0.54 and 9.58 ± 2.22 μg/mL, respectively. In short, both the extract and fractions and isolated compounds showed marked urease inhibition and thus a useful natural source of urease inhibition.     

Design,synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-β-lactam derivatives

This paper describes the synthesis of some new β-lactam derivatives containing the 1,2,3-triazole moiety. All the compounds were evaluated for their in vitro antimicrobial and antimalarial activities. Moderate to excellent antimalarial activities were encountered. The results showed that compounds 5a, 5c, 5f, 5i exhibited the most potent antimalarial activity with IC₅₀ values of 0.85, < 0.97, < 0.97, 1.81 µM against chloroquine-resistant P. falciparum K1 strain. A QSAR study highlights the structure–activity relationships that correlate the observed antimalarial activities with changes in the compounds’ structural features.     

Acanthus mollis L. leaves as source of anti-inflammatory and antioxidant phytoconstituents

This work expands the phytochemical composition knowledge of Acanthus mollis and evaluates antioxidant and anti-inflammatory activities which could be related with its traditional uses. Extracts from leaves, obtained by sequential extraction, were screened using TLC and HPLC-PDA. The ethanol extract was the most active on DPPH assay (IC₅₀ = 20.50 μg/mL) and inhibited nitric oxide (NO) production in RAW 264.7 macrophages (IC₅₀ = 48.31 μg/mL). Significant amounts of cyclic hydroxamic and phenolic acids derivatives were detected. A lower antioxidant effect was verified for a fraction enriched with DIBOA derivatives (IC₅₀ = 163.02 μg/mL), suggesting a higher contribution of phenolic compounds for this activity in ethanol extract. However, this fraction exhibited a higher inhibition of NO production (IC₅₀ = 32.32 μg/mL), with absence of cytotoxicity. These results support the ethnomedical uses of this plant for diseases based on inflammatory processes. To our knowledge, it is the first report to the anti-inflammatory activity for DIBOA derivatives.     

Chemical composition,antioxidant and antimicrobial activities of the edible medicinal Ononis natrix growing wild in Tunisia

Results showed that leaf methanolic extract of Ononis natrix has important total phenol (51 mg GAE/g DW) and flavonoid (14.76 CE/g DW) contents. The chemical composition of O. natrix leaf revealed the presence of quercitine (24.5%), amentoflavone (14.1%), flavones (11.3%) and kaempferol (10.5%). The leaf extract showed a high total antioxidant activity with 60.94 mg of GAE/g DW, displayed a high 2,2-diphenyl-1-picrylhydrazyl scavenging ability with low IC₅₀ value (29 μg/mL) and a great reducing power (EC₅₀ = 100 μg/mL). O. natrix leaf extract exhibited a significant broad spectrum activity against all tested microorganisms with bacterial inhibition zone sizes ranging from 8.5 to 17 mm in diameter.     

Chemical composition and in vitro anticancer,antimicrobial and antioxidant activities of essential oil and methanol extract from Rumex nervosus

Chemical composition, antioxidant, anticancer, and antimacrobial activities of essential oil obtained from leaves of Rumex nervosus has been evaluated here for the first time. GC/MS analysis reveals the presence of Palmitoleic Acid (28.35%) and Palmitic acid, (25. 37%) as their methyl ester as major components. The essential oil showed significant DPPH radical scavenging activity (94.907 ± 0.1089% and 94.003 ± 0.0749%) at concentration (100 and 80) μg/mL respectively. The oil showed promising activity against staph aureus, while showed weak activity against (Hela and 3T3) cell lines. The crude extract / fractions of R. nervosus (leaves) showed significant antioxidant activity at dose (100 and 80) μg/mL. Futhermore the crude showed significant activity against (MCF-7 and MDA-MB-231) cell lines with IC₅₀ (20.5138 ± 0.933 and 25.1728 ± 0.9176) μg/mL respectively, and chloroform fraction showed good activity against (MCF-7 and MDA-MB-231) cell lines with IC₅₀ (31.154 ± 0.965 and 42.269 ± 2.1045) μg/mL.     

In vitro antimicrobial activity of extracts and compounds isolated from Cladonia uncialis

Heptane (Hep), diethyl ether (Et₂O), acetone (Me₂CO) and methanolic (MeOH) extracts, as well as ( ? )-usnic acid and squamatic acid, were obtained from thallus of Cladonia uncialis (Cladoniaceae). The antimicrobial activities of these extracts, ( ? )-usnic acid and squamatic acid, were tested against reference strains: Staphylococcus aureus, Escherichia coli and Candida albicans. In addition, Me₂CO extract was analysed against 10 strains of Methicillin-resistant S. aureus (MRSA) isolated from patients. All extracts exerted antibacterial activity against the reference strain S. aureus, comparably to chloramphenicol [minimum inhibitory concentration (MIC) = 5.0 μg/mL]. The Me₂CO extract exhibited the strongest activity against S. aureus (MIC = 0.5 μg/mL), higher than ( ? )-usnic acid, whereas squamatic acid proved inactive. The Me₂CO extract showed potent antimicrobial activity against MRSA (MIC 2.5–7.5 μg/mL). Also no activity of C. uncialis extracts against E. coli and C. albicans was observed.     

Preparative isolation of paclitaxel and related taxanes from cell cultures of Taxus chinensis using reversed-phase flash chromatography

In this study, paclitaxel, baccatin III, taxuyunnanine C and sinenxane C were successfully separated by reversed-phase flash chromatography on a manually packed C₁₈ column from Taxus chinensis cell culture extract. The crude cell culture extract was first treated with Al₂O₃ column chromatography and then divided into two parts: fraction 1 and fraction 2. Ten milligrams of baccatin III and 19 mg of paclitaxel were obtained from 100 mg dried fraction 1. Fifty-two milligrams of taxuyunnanine C and 11 mg sinenxane C were obtained from 100 mg dried fraction 2. The purities of the four compounds were 98.02%, 98.53%, 98.93% and 98.76%, respectively. Their structures were characterised by using UV, MS and NMR. These results indicate that paclitaxel and related taxanes including baccatin III can be obtained from cell culture in a highly pure state using reversed-phase flash chromatography.     

Bioactivity and chemical characterisation of Lophostemon suaveolens – an endemic Australian Aboriginal traditional medicinal plant

Lophostemon suaveolens is a relatively unexplored endemic medicinal plant of Australia. Extracts of fresh leaves of L. suaveolens obtained from sequential extraction with n-hexane and dichloromethane exhibited antibacterial activity in the disc diffusion and MTT microdilution assays against Streptococcus pyogenes and methicillin sensitive and resistant strains of Staphylococcus aureus (minimum bactericidal concentration < 63 μg/mL). The dichloromethane extract and chromatographic fractions therein inhibited nitric oxide in RAW264.7 murine macrophages (IC₅₀ 3.7–11.6 μg/mL) and also PGE₂ in 3T3 murine fibroblasts (IC₅₀ 2.8–19.7 μg/mL). The crude n-hexane, dichloromethane and water extracts of the leaves and chromatographic fractions from the dichloromethane extract also showed modest antioxidant activity in the ORAC assay. GC–MS analysis of the n-hexane fraction showed the presence of the antibacterial compounds aromadendrene, spathulenol, β-caryophyllene, α-humulene and α-pinene and the anti-inflammatory compounds β-caryophyllene and spathulenol. Fractionation of the dichloromethane extract led to the isolation of eucalyptin and the known anti-inflammatory compound betulinic acid.     

Chemical composition and larvicidal activity of Zanthoxylum armatum against diamondback moth,Plutella xylostella

The diamondback moth, Plutella xylostella (L.) (Lepidoptera: Yponomeutidae) is the most serious pest of cruciferous crops grown in the world causing economic yield loss. Several synthetic insecticides have been used against P. xylostella but satisfactory control was not achieved due to development of resistance to insecticides. Therefore, the present study was carried out to screen different fractions of Zanthoxylum armatum for their insecticidal activities against second instar larvae of P. xylostella. Results indicate, all the fractions showed activity to P. xylostella. However, n-hexane fraction of Z. armatum showed maximum larvicidal activity with minimum LC₅₀ value of 2988.6 ppm followed by ethanol (LC₅₀ = 12779.7 ppm) and methanol fraction (LC₅₀ = 12908.8 ppm) whereas chloroform fraction was least toxic (LC₅₀ = 16750.6 ppm). The GC–MS analysis of n-hexane fraction of leaf extract showed maximum larvicidal activity, which may be due to two major compounds i.e. 2-undecanone (19.75%) and 2-tridecanone (11.76%).     

Phytochemical profiles and antioxidant capacity of the crude extracts,aqueous- and saponin-enriched butanol fractions of <Emphasis Type="Italic">Helicteres hirsuta</Emphasis> Lour. leaves and stems

This study aimed to compare phytochemical profiles and antioxidant capacity of various extracts including crude extracts, aqueous- and saponin-enriched butanol fractions prepared from the stems and leaves of Helicteres hirsuta Lour. The results revealed that all the three powdered extracts from the leaves and the stems possessed high levels of phenolics (177.07–241.03 mg GAE g^?1), flavonoids (158.03–280.06 mg CE g^?1) and saponins (165.77–1035.33 mg ESE g^?1) and exhibited strong antioxidant capacity. HPLC analysis identified nine major compounds in the leaf powder crude extract; however, the leaf aqueous fraction had three extra compounds; whereas, the saponin-enriched butanol leaf fraction had seven extra compounds. For the stems, twelve main compounds were evident in either the powdered crude extract or the aqueous fraction, and five new compounds were revealed in the saponin-enriched butanol fraction. The findings revealed that the powdered aqueous fractions and saponin-enriched butanol fractions are potential sources of biologically active compounds for further investigation and industrial utilisation.     

Anti-hydroxyl radical activity,redox potential and anti-AChE activity of Amanita strobiliformis polysaccharide extract

This study outlines antioxidant and anti-AChE activities of the polysaccharide (PSH) extract from the mushroom species Amanita strobiliformis. Both the presence of α and ß glucans within the aforementioned extract was recorded. PSH extract displayed a profound scavenging activity of OH radicals (IC₅₀ value, 11.86 ± 0.59 μg/mL) and high potential for reduction of Fe³⁺ ions (174.11 ± 8.70 mg eq. AA/g d.w.) being almost 48- and 5-fold more effective than mannitol and butylated hydroxytoluene used as a positive control, respectively. Compared with galanthamine (0.001 μg), the same extract exhibited a moderate anti-AChE activity (10 μg) in solid. Since purified PSH extract exhibited higher bioactivity (IC₅₀ value 7.27 ± 0.31 μg/mL, 197.68 ± 9.47 mg eq. AA/g d.w. and 0.1 μg, respectively), it can be predominantly ascribed to the polysaccharide compounds. A. strobiliformis PSH extract may be considered as a promising resource of potent bioactive polysaccharides of natural origin successfully addressing both oxidative stress and lack of acetylcholine.     

Chemical constituents of essential oil of endemic Rhanterium suaveolens Desf. growing in Algerian Sahara with antibiofilm,antioxidant and anticholinesterase activities

Twenty compounds were detected in the essential oil of Rhanterium suaveolens representing 98.01% of the total oil content. Perillaldehyde (45.79%), caryophyllene oxide (24.82%) and β-cadinol (5.61%) were identified as the main constituents. In β-carotene–linoleic acid assay, both the oil and the methanol extract exhibited good lipid peroxidation inhibition activity, with IC₅₀ values of 17.97 ± 5.40 and 11.55 ± 3.39 μg/mL, respectively. In DPPH and CUPRAC assays, however, the methanol extract exhibited a good antioxidant activity. The highest antibiofilm activity has been found 50.30% against Staphylococcus epidermidis (MU 30) at 20 μg/mL for essential oil and 58.34% against Micrococcus luteus (NRRL B-4375) at 25 mg/mL concentration for methanol extract. The in vitro anticholinesterase activity of methanol extract showed a moderate acetylcholinesterase inhibitory (IC₅₀ = 168.76 ± 0.62 μg/mL) and good butyrylcholinesterase inhibitory (IC₅₀ = 54.79 ± 1.89 μg/mL) activities. The essential oil was inactive against both enzymes.     

Antioxidant potential assessment of phenolic and flavonoid rich fractions of Clematis orientalis and Clematis ispahanica (Ranunculaceae)

The antioxidant activities of crude extract fractions using Hexane, Chloroform, Ethyl Acetate, Butanol and Water of Clematis orientalis and Clematis ispahanica were investigated. 1,1-diphenyl-2-picryl-hydrazyl (DPPH) assay and the ferric reducing/antioxidant potential (FRAP) were used to evaluate the antioxidant capacity. The total phenolics were found to be 4.37–9.38 and 1.32–11.37 mg gallic acid equivalents (GAE)/g in different fractions for C. orientalis and C. ispahanica, respectively. The ethyl acetate fraction of C. orientalis and chloroform fraction of C. ispahanica showed the highest DPPH and FRAP activities at a concentration of 300 μg/mL. The predominant phenolic compounds identified by HPLC in C. orientalis were Resorcinol (603.5 μg/g DW) in chloroform fraction and Ellagic acid (811.7 μg/g DW) in chloroform fraction of C. ispahanica.     

Antioxidant and α-glucosidase inhibitory ingredients identified from Jerusalem artichoke flowers

Jerusalem artichoke (JA, Helianthus tuberosus L.) has been researched extensively due to its wide range of uses, but there are limited studies on its flowers. In this study, we report the first detailed phytochemical study on JA flowers, which yielded 21 compounds. Compound 4 was identified as a major water-soluble yellow pigment of JA flowers. In addition, the methanol extract of JA flowers and the isolates were evaluated for their antioxidant and α-glucosidase inhibitory activities. Among the tested compounds, compound 13 showed the strongest ABTS⁺ free radical scavenging activity with SC₅₀ value of 2.30 ± 0.13 μg/mL, and compound 6 showed most potent α-glucosidase inhibitory activity with inhibition rate of 60.0% ± 10.3% at a concentration of 250 μg/mL. Results showed that methanol extract of JA flowers exhibited antioxidant and α-glucosidase inhibitory activities which could be attributed to its phenolic ingredients including chlorogenic acid derivatives, flavonoids and phenols.     

Antibacterial activity of extract and fractions from branches of Protium spruceanum and cytotoxicity on fibroblasts

The crude ethanol extract (CEE) and fractions from branches of Protium spruceanum were subjected to antibacterial and cytotoxicity assays. Compounds of the most active fraction were identified by GC-MS and LC-MS. CEE was active against 19 bacteria and the ethyl acetate fraction (EAF) showed the lowest minimum bactericidal concentration (MBC 0.3–80.0 mg/mL). Through time-kill assay was observed that EAF induced rapid bactericidal effect against Staphylococcus saprophyticus. The cytotoxicity tests against L929 fibroblasts showed great potential of EAF on the treatment of infections caused by five bacteria (MBC < IC₅₀). The results provide in vitro scientific support to the possible application of branches of P. spruceanum as antimicrobial agent that may contribute for treatment of infections.     

A new fatty acid ester from an edible mushroom Rhizopogon luteolus

Phytochemical investigation of the Rhizopogon luteolus Fr. led to the isolation of one new fatty acid ester, 3-hydroxy-2,4-dimethylheptacosyl acetate (1) together with two known compounds tetracosanoic acid (2) and ergosterol (3). 1D and 2D NMR, and MS techniques were used for structural elucidation. Phenolic and fatty acid compositions were identified using HPLC–DAD and GC–MSD, respectively. Fumaric acid was the major phenolic acid, whereas linoleic, stearic and oleic acids were the most abundant fatty acids. Antioxidant and anticholinesterase activities of the extracts and compounds (1–3) were tested spectrophotometrically. Among the extracts, hexane extract showed the highest activity in all tests, particularly in β-carotene-linoleic acid assay (IC₅₀: 16.65 ± 1.12 μg/mL). Furthermore, compound 3 exhibited higher antioxidant and anticholinesterase activities. The study indicates that R. luteolus can be used in food, cosmetic and pharmaceutical industries.