Imperatorin from the aerial parts of Cleome viscosa L.: a characterization study and evaluation of the antibacterial activity.

Cleome viscosa L., a member of the family Cleomaceae, is a potential medicinal plant, known for several bioactive properties such as: anticancer, antidiabetic, antioxidant, anti-inflammatory, antimicrobial, wound healing, etc. Our study aimed to isolate a bioactive compound and assess its antibacterial activity. The crystal compound imperatorin was isolated and reported for the first time from the aerial parts of C. viscosa. The isolation was made using silica gel (100-200 mesh) column chromatography. The structure of imperatorin was investigated through single-crystal XRD, unit cell molecules, FTIR, and ESI-MS spectral analysis. The results validated imperatorin's triclinic crystal structure and P2i/c distance group. The electronic structure was also calculated (4.28/6.21 D) along with the frontier molecular orbital, dipole moment, atomic charges, and electrostatic map of particles in gaseous stage and active site. Imperatorin showed highest activity at 40 µg/mL concentration against Gram + ve bacteria: Staphylococcus aureus (3 ± 0.2 mm), Bacillus subtilis (3 ± 0.6 mm), and Gram -ve bacteria: Klebsiella pneumoniae (3 ± 0.2 mm), Escherichia coli (5 ± 0.2 mm). The study highlights that the compound can be isolated in larger quantities as the plant is easily available across the tropics.

Greater efficiency of polyherbal drug encapsulated biosynthesized chitosan nano-biopolymer on diabetes and its complications.

Diabetes is a highly complex disease that has an adverse impact on the lives of individuals, and the current medicines used to manage diabetes have obvious side effects. Medicinal plants, on the other hand, may serve as an alternate source of anti-diabetic drugs. A polyherbal combination has a higher and more extensive therapeutic potential than a single herb. Yet, due to deterioration during the absorption process, the usage of this drug still yields inadequate results. Encapsulation of polyherbal drug with chitosan nanoparticles is one of the key ways to solve this problem due to its biocombatibilty, slow and targeted drug delivery characteristics. In the present study, the chitosan was derived from prawn shell and the chitosan nanoparticles had been prepared by ionic-gelation method. The anti-diabetic polyherbal drug (Andrographis paniculata, Andrographis alata, Adhatoda zeylanica, Gymnema sylvestre, Syzygium cumini, and Justicia glabra) was encapsulated with a bio-derived chitosan biopolymer. The drug loading efficiency was about 85 %. The chemical and physical properties of the chitosan and drug-loaded chitosan nanoparticles had been analyzed by FT-IR absorption, XRD, SEM, TEM and EDAX analysis. The antidiabetic efficiency, hepatoprotective activity and antihyperlipedimic activity of the chitosan nanoparticles, polyherbal drug and polyherbal drug encapsulated with chitosan nanoparticles were assessed in a group of rats. The polyherbal drug reduced the serum glucose level from 306.4 mg/dL to 134.47 mg/dL, while the polyherbal drug encapsulated with chitosan nanoparticles reduced to 127.017 mg/dL. This was very close to the serum glucose level of non-diabetic rat (124.65 mg/dL). Further, it considerably increased the insulin level close to that of non-diabetic rat. Thus, the polyherbal drug encapsulated with chitosan nanoparticles showed superior efficiency in antidiabetic and also diabetic complications.

Mosquito larvicidal properties of various extract of leaves and fixed oil from the seeds of Caesalpinia bonduc (L) Roxb.

A Preliminary laboratory trial was undertaken to determine the efficacies of petroleum ether, ethanolic, aqueous extracts of dried leaves and fixed oil from the seeds of Caesalpinia bonduc (L). Roxb (Family: Caesalpiniaceae) at various concentrations against the fourth instar larvae of Culex quinquefasciatus by following the WHO guidelines. Hundred per cent mortality was observed in 1% concentration of petroleum ether and ethanolic extract of leaf, whereas it was 55% in 2.5% concentration of aqueous extract and 92.6% in 2.5% concentration of fixed oil. The active constituent responsible for the mortality is to be isolated to come up with a promising larvicidal agent, which will be economic, non pollutant and ecofriendly.

Crystal structure of the complex formed between a group I phospholipase A2 and a naturally occurring fatty acid at 2.7 A resolution.

This is the first evidence of a naturally bound fatty acid to a group I Phospholipase A(2) (PLA(2)) and also to a PLA(2) with Asp 49. The fatty acid identified as n-tridecanoic acid is observed at the substrate recognition site of PLA(2) hydrophobic channel. The complex was isolated from the venom of Bungarus caeruleus (Common Indian Krait). The primary sequence of the PLA(2) was determined using the cDNA method. Three-dimensional structure has been solved by the molecular replacement method and refined using the CNS package to a final R factor of 19.8% for the data in the resolution range from 20.0 to 2.7 A. The final refined model is comprised of 912 protein atoms, one sodium ion, one molecule of n-tridecanoic acid, and 60 water molecules. The sodium ion is located in the calcium-binding loop with a sevenfold coordination. A characteristic extra electron density was observed in the hydrophobic channel of the enzyme, into which a molecule of n-tridecanoic acid was clearly fitted. The MALDI-TOF measurements of the crystals had earlier indicated an increase in the molecular mass of PLA(2) by 212 Da over the native PLA(2). A major part of the ligand fits well in the binding pocket and interacts directly with His 48 and Asp 49. Although the overall structure of PLA(2) in the present complex is similar to the native structure reported earlier, it differs significantly in the folding of its calcium-binding loop.

Toxicity of Nerium indicum Miller seed extract on bandicoot rat, Bandicota bengalensis Gray.

Crude extract (12.5 ml/kg) of N. indicum seed gave 100% mortality of B. bengalensis. Humanness assessment study revealed that this plant orgin chemical caused low pain and sufferings to the target pests.

Evaluation of psychopharmacological effects of Clerodendrum phlomidis Linn. extract.

The methanolic extract of Clerodendrum phlomidis Linn. (MECP) leaves was evaluated for its psychopharmacological activities in several experimental models using Swiss albino mice and Wistar albino rats. The MECP was found to cause significant reduction in spontaneous activity, and decreases in exploratory behavioral profiles by the Y-maze and head dip test. It also showed reduction in muscle relaxant activity by rotarod, 30 degrees inclined screen and traction tests, as well as significantly potentiated the phenobarbitone sodium-induced sleeping time in the doses examined (200, 400 and 600 mg/kg body wt.). All the results were compared with respective controls for the evaluation of significance.

Characterization of multidrug resistance and monitoring of tumor response by combined 31P and 1H nuclear magnetic resonance spectroscopic analysis.

A combined 31P and 1H nuclear magnetic resonance (NMR) spectroscopic study was carried out in drug-sensitive and adriamycin- and mitoxantrone-resistant P388 murine leukemic cells. Typical spectral changes characteristic of multidrug resistance were observed in resistant cells compared to drug-sensitive cells. Quantitative comparison of phosphate metabolites ATP, phosphocreatine, phosphomonoesters and phosphodiesters revealed a significant alteration in the metabolism of resistant cells. The elevated levels of energy metabolites supported the energy-dependent process of drug efflux in resistant cells. An increased rate of glycolysis in resistant cells as indicated by the elevated lactate level further supported this. The near total loss of energy metabolites and marked decrease in phospholipid metabolites in sensitive cells upon treatment with drug compared to unaltered metabolite levels in resistant cells suggested that the spectral changes can reveal the subtle differences in tumor response between drug-sensitive and -resistant cells. The results substantiate the potential of this non-invasive method to characterize the multidrug resistance phenotype and monitor tumor response.