Prapration of Tablet from Pencil Cactus for Treatment of Piles by Direct Compression method

The intention of current review is to make available upto-date information on morphology, ecological biodiversity, medicinal uses, phytochemistry and pharmacological activities on different parts of Euphorbia tirucalli (E. tirucalli). This plant has a number of medicinal uses. Latex of E. tirucalli is vesicant and rubefacient which is used for rheumatism, warts, cough, asthma, ear-ache, tooth-ache and neuralgia. It acts as a purgative in small doses while in big doses it is bitter irritant and emetic. Milky juice is alexiteric, carminative and purgative. It is useful in whooping cough is used in treatment of piles. gonorrhea, asthma, leprosy, dropsy, dyspepsia, enlargement of spleen, colic, jaundice and stone in bladder. The fresh milky juice is good alternative in syphilis and a good application in neuralgia. A decoction of branches is used in gastralgia and colic. Bark is used in treatment of fractures. Poultices prepared from the stem are useful to repair the broken bones. Boiled root liquid acts as an emetic in cases of snake-bite and for infertility in women. The wood is used for rafters, toys and veneering purposes. It is also useful against leprosy and foot paralysis subsequent to childbirth. E. tirucalli is reported to have euphol, β-sitosterol, euphorbol hexacosonate, cycloeuphordenol, cyclotirucanenol, tirucalicine, tri-methyl ellagic acid, gallic acids, terpenic alcohol. genotoxic/mutagenic, hepatoprotective, insect repellants, immunomodulatory, larvicidal, molluscicidal/ovicidal/piscicidal, myelopoiesis, proteolytic/chitinolytics pharmacological activities. There is a need to isolate dynamic constituents, their biological trial, molecular mechanisms, experimental protection and legalization of therapeutic uses of E. tirucalli. The collected information will be helpful to locate up study protocol for expansion in curative and treat a variety used in treatment of piles., isoeuphorol, taraxasterol, tirucallol, euphorone, euphorcinol, euphorbins, 12-deoxy4βhydroxyphorbol-13-phenyl acetate-20-acetate, 12, 20- dideoxyphorbol-13-isobutyrate, glut-5-en-3-β-ol, 3,3′- diO-methylellagic acid, euphorbin-A (polyphenol), tirucallin-A (7) (tannin), tirucallin-B (11), euphorbin-F (14) (dimers), cycloartenol, 24- methylenecycloartenol, ingenol triacetate, 12-deoxy-4β-hydroxyphorbol- 13- phenyl acetate-20-acetate, taraxerone, euphorginol, taraxerol, campesterol, stigmasterol, palmitic acid, linoleic acid, β-amyrin, etc. Active phytoconstituents. E. tirucalli have possessed activity in humanly mphocytes, analgesic, anthelmintics, antiarthritic, antibacterial/antifungal/antimicrobial Antihemerrhoids. Keywords: Euphorbia tirucalli Morphology Ecological biodiversity Medicinal uses Phytochemistry Anticance antihemerrhoids

Alkali metal cations can inhibit non-covalent catalysis

The study concerns the effect of inorganic salts on supramolecular catalysis. The model reaction is the acid hydrolysis of the ammonium phenyl acetate derivative promoted by cucurbit[7]uril macrocycle. When salt is absent, the macrocycle is insensitive to the ionic strength of the solution, and the reaction rate linearly depends on the concentration of hydronium ions (H3O+). After the addition of inorganic salts, in particular, Na+ and K+ ions, the catalytic effect of the macrocycle is suppressed. The kinetic and binding data collected by us evidence the formation of the ternary complexes between the cations, macrocycle, and substrate, which are less prone to H3O+ attack. This type of inhibition corresponds to a rare uncompetitive model in contrast to a more common competitive one that relies on the displacement of the substrate. This study shows that special care must be taken when studying catalysis in solutions that contain metal cations, such as regular water and inorganic buffers.

Paraoxonase 1, B Vitamins Supplementation, and Mild Cognitive Impairment

Background: Identification of modifiable risk factors that affect cognitive decline is important for the development of preventive and treatment strategies. Status of paraoxonase 1 (PON1), a high-density lipoprotein-associated enzyme, may play a role in the development of neurological diseases, including Alzheimer’s disease. Objective: We tested a hypothesis that PON1 status predicts cognition in individuals with mild cognitive impairment (MCI). Methods: Individuals with MCI (n = 196, 76.8-years-old, 60% women) participating in a randomized, double-blind placebo-controlled trial (VITACOG) were assigned to receive a daily dose of folic acid (0.8 mg), vitamin B12 (0.5 mg) and B6 (20 mg) (n = 95) or placebo (n = 101) for 2 years. Cognition was analyzed by neuropsychological tests. Brain atrophy was quantified in a subset of participants (n = 168) by MRI. PON1 status, including PON1 Q192R genotype, was determined by quantifying enzymatic activity of PON1 using paraoxon and phenyl acetate as substrates. Results: In the placebo group, baseline phenylacetate hydrolase (PhAcase) activity of PON1 (but not paraoxonase activity or PON1 Q192R genotype) was significantly associated with global cognition (Mini-Mental State Examination, MMSE; Telephone Inventory for Cognitive Status-modified, TICS-m), verbal episodic memory (Hopkins Verbal Learning Test-revised: Total Recall, HVLT-TR; Delayed Recall, HVLT-DR), and attention/processing speed (Trail Making A and Symbol Digits Modalities Test, SDMT) at the end of study. In addition to PhAcase, baseline iron and triglycerides predicted MMSE, baseline fatty acids predicted SDMT, baseline anti-N-Hcy-protein autoantibodies predicted TICS-m, SDMT, Trail Making A, while BDNF V66M genotype predicted HVLT-TR and HVLT-DR scores at the end of study. B-vitamins abrogated associations of PON1 and other variables with cognition. Conclusion: PON1 is a new factor associated with impaired cognition that can be ameliorated by B-vitamins in individuals with MCI.

Influence of Harvest Date and Grape Variety on Sensory Attributes and Aroma Compounds in Experimental Icewines of Ukraine

Icewine is a sweet dessert wine whose sensory and chemical attributes are caused by technology peculiarities including the special climatic conditions and acceptable grape varieties. This study aimed to evaluate the sensory characteristics and aromatic compounds in experimental icewines produced from the grape varieties Rkatsiteli, Telti kuruk, Marselan, and Moldova that had been picked in the Odessa region at temperatures of at least minus 7 °C during the 2015 (H1) and 2016 (H2) harvests. Sensory attributes were determined by trained experts, and descriptors for icewines were chosen by consensus. A total of 33 aromatic compounds including 12 that exceeded the threshold were identified using chromatographic analysis. Rkatsiteli icewine obtained from H1 was characterized by the highest concentration of geraniol, 1-octanol, and 2-phenyl acetate, influencing the pronounced citrus and sweet fruit aromas in sensory profiles. The highest concentrations of ethyl hexanoate and ethyl octanoate associated with aromas of dried fruits were detected in Moldova and Marselan icewines made from H2. No 1-hexanol and benzyl alcohol were found in Rkatsiteli and Telti kuruk icewines. Only Moldova and Marselan icewines had γ-nonalactone and benzaldehyde, respectively. Sensory parameters and the quantity of aromatic compounds of Ukrainian experimental icewines depended on harvest date and grape varieties.

Effect of Microcapsule Content on Diels-Alder Room Temperature Self-Healing Thermosets

A furan functionalized epoxy-amine thermoset with an embedded microcapsule healing system that utilizes reversible Diels-Alder healing chemistry was used to investigate the influence of microcapsule loading on healing efficiency. A urea-formaldehyde encapsulation technique was used to create capsules with an average diameter of 150 µm that were filled with a reactive solution of bismaleimide in phenyl acetate. It was found that optimum healing of the thermoset occurred at 10 wt% microcapsule content for the compositions investigated. The diffusion of solvent through the crack interface and within fractured samples was investigated using analytical diffusion models. The decrease in healing efficiency at higher microcapsule loading was attributed partially to solvent-induced plasticization at the interface. The diffusion analysis also showed that the 10% optimum microcapsule concentration occurs for systems with the same interfacial solvent concentration. This suggests that additional physical and chemical phenomena are also responsible for the observed optimum. Such phenomena could include a reduction in surface area available for healing and the saturation of interfacial furan moieties by reaction with increasing amounts of maleimide. Both would result from increased microcapsule loading.

Crystal structure of the coordination polymer catena-poly[[bis[hydroxy(phenyl)acetato-κ2 O 1,O 2]zinc(II)]-μ2-1,2-bis(pyridin-4-yl)ethane-κ2 N:N′]

In the title polymeric ZnII compound, [Zn(C8H7O3)2(C12H12N2)] n , the Zn cation is coordinated by two N atoms from 1,2-bis(pyridin-4-yl)ethane unit and four O atoms from two mandelate [or hydroxy(phenyl)acetate] anions in a slightly distorted octahedral coordination geometry. The 1,2-bis(pyridin-4-yl)ethane unit bridges two ZnII cations, related by an inversion centre, to form a polymeric chain along [110]. The crystal structure features extensive O—H...O and weak C—H ...O hydrogen bonds, with C—H ... π interactions and π–π interactions also being present. The centroid–centroid distance between the phenyl ring of the mandelate group and the 1,2-bis(pyridine-4-yl)ethane moiety is 4.951 (2) Å. The 1,2-bis(pyridin-4-yl)ethane ligand is disordered over two positions, with a refined occupancy of 0.578 (14) for the major component.

Crystal structure of a new hydrate form of the NSAID sodium diclofenac

The crystal structure is reported of sodium 2-[2-(2,6-dichloroanilino)phenyl]acetate 3.5-hydrate or tetra-μ-aqua-κ8 O:O-decaaquabis{μ3-2-[2-(2,6-dichloroanilino)phenyl]acetato-κ3 O:O:O}tetrasodium(I) bis{2-[2-(2,6-dichloroanilino)phenyl]acetate}, {[Na4(C14H10Cl2NO2)2(H2O)14](C14H10Cl2NO2)2} n , which represents a new hydrate form of the NSAID sodium diclofenac (SD). The triclinic unit cell contains one ionic compound with formula Na4(C14H10Cl2NO2)4(H2O)14, in which two symmetry-related carboxylate anions C14H10Cl2NO2 − are bonded to a centrosymmetric [Na4]4+ core cationic cluster, while the others are only hydrogen bonded to the cationic cluster. The conformation for the anions is similar to that found in other diclofenac compounds, and the [Na4(Ocarbox)2(H2O)14]4+ cluster displays an unprecedented geometry, which can be described as an incomplete dicubane cluster formed by face-sharing incomplete cubes. A complex framework of O—H...O hydrogen bonds stabilizes the crystal structure. The herein reported crystal structure for SD·3.5H2O in space group P\overline{1} is different from those previously reported for other hydrates, namely SD·4.75H2O (P21) and SD·5H2O (P21/m).

Paraoxonase 1 Phenotype and Protein N-Homocysteinylation in Patients with Rheumatoid Arthritis: Implications for Cardiovascular Disease

Paraoxonase 1 (PON1) is the high density lipoprotein-associated esterase which inhibits the development of atherosclerosis by metabolizing lipid peroxidation products as well as hydrolyzing proatherogenic metabolite of homocysteine (Hcy), Hcy thiolactone, which otherwise reacts with lysine groups of proteins, thus forming N-Hcy-protein in a process referred to as protein N-homocysteinylation. Rheumatoid arthritis (RA) is the chronic inflammatory autoimmune disease associated with increased risk of cardiovascular complications, but the underlying mechanisms are incompletely understood. We examined PON1 status and N-homocysteinylation of serum proteins in patients with RA. Blood was collected from 74 RA patients and 70 control subjects. PON1 activity was measured toward synthetic (paraoxon, phenyl acetate) and natural (Hcy thiolactone) substrates. PON1 protein concentration was measured by ELISA. Total Hcy as well as N-Hcy-protein were measured in serum as well. PON1 activity toward Hcy thiolactone was lower in RA patients than in control subjects which was accompanied by increased concentration of N-Hcy-protein despite normal total Hcy concentration. PON1 protein concentration was unchanged in the RA group, but the specific enzyme activity was reduced. When RA patients were categorized according to the DAS28-ESR score, PON1 concentration and enzymatic activity were lower whereas N-Hcy-protein was higher in those with high disease activity. PON1 activity and Hcy thiolactone were correlated with DAS28-ESR score and myeloperoxidase concentration. In conclusion, RA is associated with deficiency of PON1 activity and increased protein N-homocyseinylation which may contribute to accelerated development of cardiovascular diseases.

New Complexes with Triazole Schiff Bases Derivative Ligand Containing Aspirin: Synthesis, Structure, Conductivity and Magnetic Susceptibility

Complexes of Cu(II) ), Ni (II) and Co (II) of a new triazole Schiff-base of two different ligand ,namely(E)-2-(4-((2-hydroxybenzylidene)amino)4H- 1,2,4-triazol-3-yl)phenyl acetate and (E)-2-(4-((2-hydroxy-4-methoxybenzylidene)amino)-4H-1,2,4-triazol-3-yl)phenyl acetate were prepared and characterized by elemental analysis, 1H, 13C-NMR, FTIR and UV-Visible spectroscopic data. The complex is found to be an ionic in nature by conductivity measurements and have been found to posses 1:2(M:2L) stoichiometry. The magnetic moment values of 1.540–1.7295.B.M. for Cu(II) complexes without doubt recommend octahedral geometry with one unpaired electron for Cu(II) complexes. The magnetic moment values of 3.863–4.039 B.M. for Co(II) complexes that recommend high spin octahedral geometry with three unpaired electron for Co(II) complexes. The magnetic moment value of 2.351B.M. for Ni(II) complex was matches to two unpaired electrons and octahedral geometry. Considerable variations in biological activity with structure and types are observed for these complexes.