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AbstractThree triorganotin(IV) compounds, R3Sn(L), with R = CH3(1), n-C4H9(2) and C6H5(3), and LH = 4-[(2-chloro-4-methylphenyl)carbamoyl]butanoic acid, were prepared and confirmed by various techniques. A five-coordinate, distorted trigonal-bipyramidal geometry was elucidated for tin(IV) centres both in solution and solid states. An intercalation mode was confirmed for the compound SS-DNA interaction by UV-visible, viscometric techniques and molecular docking. MD simulation revealed stable binding of LH with SS-DNA. Anti-bacterial investigation revealed 2to be generally the most potent, especially against Saand Ab, i.e. having the lowest MIC values (≤0.25 μg/mL) compared to the standard anti-biotics vancomycin-HCl (MIC = 1 μg/mL) and colistin-sulphate (MIC = 0.25 μg/mL). Similarly, the anti-fungal profile shows 2exhibits 100% inhibition against Caand Cnfungal strains and has MIC values (≤0.25 μg/mL) comparatively lower than standard drug fluconazole (0.125 and 8 μg/mL for Caand Cn, respectively). Compound 2has the greatest activity with CC50≤ 25 μg/mL and HC50> 32 μg/mL performed against HEC239 and RBC cell lines. The anti-cancer potential was assessed against the MG-U87 cell line, using cisplatin as the standard (133 µM), indicates 2displays the greatest activity (IC50: 5.521 µM) at a 5 µM dose. The greatest anti-leishmanial potential was observed for 2(87.75 at 1000 μg/mL) in comparison to amphotericin B (90.67). The biological assay correlates with the observed maximum of 89% scavenging activity exhibited by 2. The Swiss-ADME data publicised the screened compounds generally follow the rule of 5 of drug-likeness and have good bioavailability potential.

Herein we have determined the heavy metals concentrations (Pb, Cd, and Ni) estimated in River Swat water, irregated soils samples, fodder plant’s parts, farmed animal milk/meat samples and human blood from two location Mingora and Barikot in District Swat, Pakistan, using atomic absorption spectrophotometer. Heavy metals such as Cd, Pb, and Ni were found 0.016 ± 0.008, 0.50 ± 0.03, and 0.022 ± 0.004 mg/L in Mingora drain water, respectively, while in the Barikot sample the aforementioned metal were in the range of 0.014 ± 0.01, 0.29 ± 0.02, and 0.108 ± 0.08 mg/L. In the field water samples of Mingora the Cd, Pb and Ni were detected in the range of 0.008 ± 0.001, 0.65 ± 0.05 and 0.032 ± 0.006 mg/L, respectively, while in the field water samples of Barikot contained Cd = 0.016 ± 0.007 mg/L, Pb = 0.48 ± 0.04 mg/L and Ni = 0.043 ± 0.003 mg/L. Drain soil of Mingora contained the highest concentrations of heavy metals, with Cd = 3.9 ± 0.62 mg/kg, Pb = 45.5 ± 3.2 mg/kg, and Ni = 19.95 ± 2.1 mg/kg, whereas field soil contained Cd = 1.6 ± 0.44 mg/kg, Pb = 54.5 ± 2.26 mg/kg, and Ni = 34.75 ± 3.2 mg/kg. Cd in the Barikot drain soil was 3.95 ± 0.71 mg/kg, while it was 0.8 ± 0.06 mg/kg in the field soil. Lead in the same drain sample was 33 ± 3.23 mg/kg, while it was 72 ± 4.15 mg/kg in the field sample. Ni concentrations in Barikot drain soil samples was 13.85 ± 1.1 mg/kg, while 6.9 ± 0.8 mg/kg was detected in field samples. From the results it can be concluded that appreciable concentrations of heavy metals are present in milk and meat samples of farmed animals whereas significant quantities are also there in human blood samples indicating the transport of the selected metals from water through fodder plants into human. However, it may not be the sole reason heavy metal contaminations in human blood other factors like inhalation etc. may also be equally responsible.

Silymarin-loaded zein polysaccharide core–shell nanoparticles (SZPCS-NPs) were synthesized where sodium alginate and pectin offer stability and controlled release qualities to zein, a maize protein, having excellent biocompatibility. The present study is an attempt to develop zein–silymarin polysaccharide core–shell nanostructures to enhance water solubility, thereby improving bioavailability and producing enhanced biological responses in living systems. SZPCS-NPs were prepared using pH-induced antisolvent precipitation method. Five different types of SZPCS-NPs were synthesized using different combinations of sodium alginate and pectin, namely P100–A00 (non-uniform size ranging from 20 to 100 nm), P70–A30 (spherical and uniform size measuring approximately 80 nm in diameter), P50–A50, P30–A70, and P00–A100 exhibited irregular shapes with the presence of some triangular and oval structures and non-uniform size ranging from 20 to 100 nm. The SZPCS-NPs P70–A30 possessed the best results in terms of shape, size, and other characterization studies. Furthermore, the SZPCS-NPs possessed a percent drug loading of 72.5% and entrapment efficiency of 51.7%, respectively. The resulting SZPCS-NPs exhibited an excellent relative bioavailability percentage of 97.4% in comparison to commercial silymarin, having 58.1%, and crude silymarin, having 46.97% bioavailability percentage, correspondingly. In addition, SZPCS-NPs possessed an almost two folds’ increase in antioxidant activity in comparison to crude and commercially available silymarin. Similarly, SZPCS-NPs also showed better stabilization in hepatic biomarker enzymes and possessed better hepatoprotective activity for a period of 6 weeks, in contrast to commercial and crude silymarin formulations.

Teucrium yemense(Defl), locally known as Reehal Fatima, is a medicinal plant commonly grown in Saudi Arabia and Yemen. Phytochemical investigation of the aerial parts of T. yemenseyielded six new neoclerodane diterpenoids, namely fatimanol A–E (1, 2, 3, 5, and 6) and fatimanone (4), and the known teulepicephin (7). As both the Teucriumgenus and the related Lamiaceaefamily have previously been widely reported to possess anthelmintic and antimicrobial activities, the structural and biological characterization of the seven diterpenoids was pursued. The structures of the new compounds were elucidated from their 2D NMR and MS profiles and by comparison to related compounds. The structure of fatimanol D (5) was confirmed by X-ray crystallographic analysis. The new structures contribute to the breadth of knowledge of secondary metabolites in this genus.

C8H18CuNa2O11, monoclinic, P21/n(no. 14), a= 9.9625(5) Å, b= 14.0145(7) Å, c= 11.3376(6) Å, β= 97.602(2)°, V= 1569.04(14) Å3, Z= 4, Rgt(F) = 0.0178, wRref(F2) = 0.0482, T= 200 K.

Monosaccharidic push-pull butadienes are interesting building blocks for the synthesis of various heterocyclic and natural products due to their biological prevalence and significant p-electron interactions between donor and acceptor groups. A series of 1,5-anhydro-3,4,6-tri-O-benzyl-2-deoxy- 2-formyl-D-arabino-hex-1-enitol (2) and 1,5-anhydro-3,4-di-O-benzyl-2-deoxy-2-formyl-L-erythrohex- 1-enitol (4) derived push-pull branched chain sugars have been synthesized by condensation with active methylene compounds using basic aluminum oxide (Al2O3) or anhydrous sodium acetate (NaOAc) at room temperature. The compounds have been fully characterized by spectroscopic techniques and elemental analyses.

C16H26N2S, monoclinic, P21/n(no. 14), a= 6.4855(4) Å, b= 20.1110(12) Å, c= 11.2575(7) Å, β= 92.014(2)°, V= 1467.41(16) Å3, Z= 4, Rgt(F) = 0.0324, wRref(F2) = 0.0889, T = 200 K.

C19H30N2O2S, monoclinic, P21/n(no. 14), a= 6.4977(5) Å, b= 28.728(2) Å, c= 10.1806(8) Å, β= 101.549(3)°, V= 1861.9(2) Å3, Z= 4, Rgt(F) = 0.0460, wRref(F2) = 0.1213, T= 296 K.

Treatment of 2(3)-formyl-glycals 1, 3, 5 with alkyl cyanoacetates afforded 2(3)-[(E)-2-cyano-2- alkoxycarbonyl-vinyl]-2(3)-deoxy-1,5(2, 6)-anhydro-hex-1(2)-enitols 2, 4, 6 which were reacted with aniline to yield nicotinonitrile acyclo-C-nucleosides 7, 9. Nicotinic acid ester acylo-C-nucleosides 11 were obtained by the reaction of 2,6-anhydro-1,4,5-tri-O-benzyl-3-[(E)-2-cyano-2-alkoxycarbonylvinyl]- 3-deoxy-D-erythro-hex-2-enitols 6 with ammonia.

C9H11ClN4O2, orthorhombic, Pbca(no. 61), a= 8.9735(4) Å, b= 12.2946(7) Å, c= 19.3751(11) Å, V= 2137.6(2) Å3, Z= 8, Rgt(F) = 0.0355, wRref(F2) = 0.1087, T= 200(2) K.

C14H11N3S2, triclinic, P1̅ (no. 2), a= 5.7607(5)Å, b= 9.8397(9) Å, c= 12.0920(11) Å, α= 72.899(4)°, β= 81.833(4)°, γ= 86.796(5)°, V= 648.40(10) Å3, Z= 2, Rgt(F) = 0.0295, wRref(F2) = 0.0797, T= 200(2) K.

C8H13N3S2, triclinic, P1̅ (no. 2), a= 7.4803(3) Å, b= 8.4562(3) Å, c= 9.3531(3) Å, α= 67.688(1)°, β= 74.017(1)°, γ= 85.008(1)°, V= 526.07(3) Å3, Z= 2, Rgt(F)= 0.0256, wRref(F2)= 0.0736, T= 200 K.

For Abstract see ChemInform Abstract in Full Text.

For Abstract see ChemInform Abstract in Full Text.