In Vitro Antimicrobial, Antioxidant Activities and Phytochemical Analysis of Canarium patentinervium Miq. from Malaysia

Six different extracts of Canarium patentinervium Miq. (Burseraceae) leaves and barks were screened for their phytochemical composition, and antimicrobial and free radical scavenging activities. Among the different extracts tested, the ethanol extract of leaves showed significant antimicrobial and radical scavenging activities. The most susceptible micro-organisms were found to be Gram-positive bacteria (Staphylococcus aureus, methicillin-resistant Staphylococcus aureus or MRSA) and Gram-negative bacteria (Pseudomonas aeruginosa). Phytochemical analysis of the extracts revealed that the antimicrobial and the radical scavenging activities are mainly due to the presence of tannins and flavonoids. The results obtained suggest that Canarium patentinervium Miq. could be exploited in the management of various infectious diseases

PHYTOCHEMICAL SCREENING OF ARTABOTRYS CRASSIFOLIUS HOOK.F. & THOMSON (ANNONACEAE JUSS.)

Objective: The aim of the present study was to determine the phytochemical constituents of Artabotrys crassifolius.   Methods: The leaves and barks of Artabotrys crassifolius were extracted sequentially with hexane, chloroform and ethanol. The corresponding crude extracts obtained were then subjected to phytochemical screening.   Results: The phytochemical analysis of crude extracts of Artabotrys crassifolius demonstrated the presence of alkaloids, cardiac glycosides, flavonoids, phenolic compounds, saponins and terpenoids.   Conclusion: The chemical profile of these crude extracts can serve as a useful reference for further investigations in pharmacological activities of Artabotrys crassifolius. Keywords Phytochemical analysis, Artabotrys crassifolius, Annonacea

Coordination chemistry and bioactivity of Ni2+, Cu2+, Cd2+ and Zn2+ complexes containing bidentate schiff bases derived from S-benzyldithiocarbazate and the X-ray crystal structure of bis[S-benzyl-β-N-(5-methyl-2-furylmethylene)dithiocarbazato]cadmium(II).

New bidentate isomeric NS and NS′ Schiff bases were derived from the condensation of S-benzyldithiocarbazate (SBDTC) with 5-methyl-2-furyldehyde and 2-furyl-methylketone. Reaction of NS ligand with Ni(II), Cu(II), Cd(II) and Zn(II) salts gave solid complexes. Only the Ni(II) complex of the NS′ ligand was isolated. All complexes were characterized by a variety of physico-chemical techniques, viz. elemental analyses, molar conductivity, i.r. and electronic spectral studies. The Schiff bases behaved as uninegatively charged bidentate ligands. Square-planar structures have been proposed for the Cu(II) complex containing the NS Schiff base ligand and the Ni(II) complexes of the bidentate NS and NS′ Schiff base ligands. Single crystal X-ray diffraction study of [Cd(NS)2] showed that the complex was bis chelated with a distorted tetrahedral structure. The antimicrobial properties of the Schiff bases and their metal complexes indicate that the organic compounds are stronger antifungal agents than their complexes with the metals studied. However, the zinc complex of the Schiff base, S-benzyl-β-N-(5-methyl-2-furyl)methylenedithiocarbazate, (NS), was found to be highly active against CEM-SS (Human cell T-lymphoblastic leukemia) with a CD50 value of 2.0 μg cm−3, while [Cd(NS)2] was moderately active with a CD50 value of 4.95 μg cm−3. None of the compounds were found to be active against HT-29 (Human colon adenocarcinoma cells). The bioactivity of a previously reported tridentate NNS Schiff base (SBD1) and its metal complexes with nickel(II) and copper(II) are also discussed

Synthesis, Characterization, and Bioactivity of Schiff Bases and Their Cd2+, Zn2+, Cu2+, and Ni2+ Complexes Derived from Chloroacetophenone Isomers with S-Benzyldithiocarbazate and the X-Ray Crystal Structure of S-Benzyl-β-N-(4-chlorophenyl)methylenedithiocarbazate

Two bidentate Schiff base ligands having nitrogen sulphur donor sequence were derived from the condensation of S-benzyldithiocarbazate (SBDTC) with 2-chloroacetophenone and 4-chloroacetophenone to give S-benzyl-β-N-(2- chlorophenyl)methylenedithiocarbazate (NS2) and S-benzyl-β-N-(4- chlorophenyl)methylenedithiocarbazate (NS4) isomers. Each of the ligands was then chelated with Cd2+, Zn2+, Cu2+, and Ni2+. The compounds were characterized via IR spectroscopy and melting point while the structure of NS4 was revealed via X-ray crystallography. Finally, the compounds were screened for antimicrobial activity to investigate the effect that is brought by the introduction of the chlorine atom to the benzene ring. X-ray crystallographic analysis showed that the structure of NS4 is planar with a phenyl ring that is nearly perpendicular to the rest of the molecules. The qualitative antimicrobial assay results showed that NS4 and its complexes lacked antifungal activity while Gram-positive bacteria were generally inhibited more strongly than Gram-negative bacteria. Furthermore, NS4 metal complexes were inhibited more strongly than the ligand while the opposite was seen with NS2 ligand and its complexes due to the partial solubility in dimethyl sulfoxide (DMSO). It was concluded that generally NS2 derivatives have higher bioactivity than that of NS4 derivatives and that the Cd complexes of both ligands have pronounced activity specifically on K. rhizophila

Acalypha wilkesiana extracts induce apoptosis by causing single strand and double strand DNA breaks

Ethnopharmacological relevance: The seeds of Acalypha wilkesiana have been used empirically by traditional healers in Southwest Nigeria together with other plants as a powder mixture to treat patients with breast tumours and inflammation. Aim of the study: There is an increasing interest among researchers in searching for new anticancer drugs from natural resources, particularly plants. This study aimed to investigate the anticancer properties of Acalypha wilkesiana extracts and the characteristics of DNA damage against brain and lung cancer cells. Materials and methods: The antiproliferative activity of Acalypha wilkesiana extracts (ethyl acetate, hexane, and ethanol) was examined on human glioma (U87MG), human lung carcinoma (A549), and human lung fibroblast (MRC5) cells. Results: Cell viability MTT assay revealed that ethyl acetate extract of the plant possessed significant antiproliferative effects against both U87MG (GI50 = 28.03 ± 6.44 μg/ml) and A549 (GI50 = 89.63 ± 2.12 μg/ml) cells (p value 300 μg/ml). The ethanol extract showed no antiproliferative effects on any cell line examined. Haematoxylin & Eosin (H & E) staining and single cell gel electrophoresis (SCGE) comet assay confirmed that plant extract-treated cells underwent apoptosis and not necrosis. SCGE comet assays confirmed that plant extracts caused both single strand (SSB) and double strand (DSB) DNA breaks that led to the execution of apoptosis. Conclusion: The extracts (especially ethyl acetate and hexane) of Acalypha wilkesiana possess valuable cytotoxic effects that trigger apoptosis in U87MG and A549 cancer cells through induction of DNA SSBs and DSBs

Benzyl N-[(Z)-(1-methyl-2-sulfanyl­propyl­idene)amino]­carbamodithio­ate.

The title compound, C12H16N2S3, was obtained by the condensation reaction of S-benzyl dithio­carbazate and 3-mercaptobutan-2-one. The phenyl ring and thiol (SH) group are approximately perpendicular [S—C—C—C and N—C—C—S torsion angles = 67.8 (3) and 116.9 (2)°, respectively] to the rest of the mol­ecule. In the crystal, mol­ecules are linked by weak S—H(...)S and N—H(...)S hydrogen bonds, π–π inter­actions between the benzene rings [centroid–centroid distance = 3.823 (2) Å] and C—H(...)π inter­actions

Bis{(Z)-[(E)-2-(pyridin-2-ylmethylidene)hydrazin-1-ylidene][(pyridin-2-yl) methylsulfanyl]methanethiolato}nickel(II)

The title compound, [Ni(C13H11N4S 2)2], was obtained by the reaction of S-2- picolyldithiocarbazate and pyridine-2-carbaldehyde with nickel(II) acetate. The NiII atom is located on a twofold rotation axis and is bonded to four N atoms at distances of 2.037 (8) and 2.109 (9) Å, and to two S atoms at a distance of 2.406 (3) Å, leading to a distorted octahedral coordination. The angle between the mean planes of the coordinating moieties of the two symmetry-related tridentate ligands is 83.3 (2)°. In the crystal, complex molecules are linked by weak C - H⋯S hydrogen bonds, π-π interactions between the pyridine rings [centroid-centroid distance = 3.775 (9) Å] and C - H⋯π interactions. The hydrogen-bonding interactions lead to the formation of layers parallel to (010); π-π interactions link these layers into a three-dimensional network

Crude Ethanol Extract of Pithecellobium ellipticum

If left untreated, hypercholesterolaemia can lead to atherosclerosis, given time. Plants from the Fabaceae family have shown the ability to significantly suppress atherosclerosis progression. We selected four extracts from Pithecellobium ellipticum, from the Fabaceae family, to be screened in a 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) assay. The ethanol extract, at a concentration of 500 μg/mL, exhibited superior inhibition properties over the other extracts by demonstrating 80.9% inhibition, while 0.223 μg/mL of pravastatin (control) showed 78.1% inhibition towards enzymatic activity. These findings led to the fractionation of the ethanol extract using ethyl acetate : methanol (95 : 5), gradually increasing polarity and produced seven fractions (1A to 7A). Fraction 7A at 150 μg/mL emerged as being the most promising bioactive fraction with 78.7% inhibition. FRAP, beta carotene, and DPPH assays supported the findings from the ethanol extract as it exhibited good overall antioxidant activity. The antioxidant properties have been said to reduce free radicals that are able to oxidize lipoproteins which are the cause of atherosclerosis. Phytochemical screenings revealed the presence of terpenoid, steroid, flavonoid, and phenolic compounds as the responsible group of compound(s), working individually or synergistically, within the extract to prevent binding of HMG-CoA to HMG-CoA reductase

Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition

Natural products possess a significant role in anticancer therapy and many currently-used anticancer drugs are of natural origin. Cerberin (CR), a cardenolide isolated from the fruit kernel of Cerbera odollam, was found to potently inhibit cancer cell growth (GI 50 values 60% bioavailability and rapid absorption; doses of 1–10 mg/kg CR were predicted to maintain efficacious unbound plasma concentrations (>GI 50 value). CR's potent and selective anti-tumour activity, and its targeting of key signalling mechanisms pertinent to tumourigenesis support further preclinical evaluation of this cardiac glycoside