Bioactive flavanoids from Glycosmis arborea

BACKGROUND: Glycosmis is a genus of evergreen glabrous shrub and distributed all over India. It possesses various medicinal properties and is used in indigenous medicine for cough, rheumatism, anemia, and jaundice. Glycosmis arborea is a rich source of alkaloids, terpenoids, coumarins, as well as flavonoids. RESULTS: The chemical investigation of methanol fraction of the leaves of G. arborea led to the isolation of one new flavone C-glycoside along with three known flavanoids, named as 5,7-dihydroxy-2-[4-hydroxy-3-(methoxy methyl) phenyl]-6-C-β-d-glucopyranosyl flavone (4), 5,7,4(′)-trihydroxy-3(′)-methoxy flavone (1), 5,4(′)-dihydroxy-3(′)-methoxy-7-O-β-d-glucupyranosyl flavanone (2), and 5,4(′)-dihydroxy-3(′)-methoxy-7-O-(α-l-rhamnosyl-(1‴→6‴)-β-d-glucopyranosyl) flavanone (3), respectively. The structures of all compounds were elucidated with the help of nuclear magnetic resonance spectrometry. Pure compounds and fractions were evaluated for pest antifeedant and antimicrobial activity. CONCLUSION: Four compounds were isolated from the leaves of G. arborea. Among them, compound 4 showed significant antimicrobial activity

Influence of microjets on flow development for diameter ratio of 1.6 for correctly expanded nozzles

This paper aims to study the microjet’s efficacy as a management tool for the duct’s flow field. The nozzle was correctly expanded for a diameter ratio of 1.6 (i.e., area ratio = 2.56). The Mach numbers considered were from 1.25 to 2. The investigation shows that the development and recovery of the duct flow are smooth at lower Mach numbers. At Mach 1.48, jet noise was reduced considerably when the control is initiated. For higher Mach numbers of the study, namely Mach 1.6, 1.8, and 2.0, The flow’s oscillatory nature was noticed. This phenomenon reiterates that the nozzles flow is wave-dominated. For most of the flow, the flowing nature remains unaltered due to control. The flow remained connected with the duct for duct length twice the nozzle exit diamete

Computational and pharmacological evaluation of stevioside derivatives for antinociceptive and antiinflammatory potential

Purpose: To carry out computational and pharmacological evaluation of two stevioside derivatives in order to develop more effective candidates for analgesia and inflammation.Methods: Primarily, compounds were docked against targets of nociception and inflammation such as cyclooxygenase-1, cyclooxygenase-2, 5-lypooxygenase 12-lypooxygenase, 15-lypooxygenase, prostaglandin synthase, leukotrienes C4 synthase, mu, kappa, and delta receptors to obtain their possible binding modes. Test compounds were then screened in animal model of nociception and inflammation.Results: The results of docking show that IO possesses good affinity when compared to ID. IO showed two hydrogen bonds against COX-1 and COX-2. IO also demonstrated good binding against 5-LOX, 12- LOX and 15-LOX, exhibited four, one and two hydrogen bonds respectively. Against PG synthase and LTC4, both IO and ID produced moderate binding. IO also showed significant binding against opoid receptors (p < 0.05). IO and ID significantly decrease the number of writhes to 21.20 ± 2.1 and 27.0 ± 2.12 at 10 mg/kg in acetic acid mediated pain test respectively. In hot plate method, IO and ID increase the latency period of mice to 14.14 ± 0.40 and 10.50 ± 0.34 s, respectively. IO and ID significantly reduced the paw edema to 1.69 ± 0.14 and 1.94 ± 0.14 mL, respectively, in acute inflammation (p < 0.05). In chronic inflammatory model, IO and ID decreased paw volume to 3.26 ± 0.38 and 4.20 ± 0.38 mL, respectively.Conclusion: The results show that IO is a promising candidate for further development as analgesic and anti-inflammatory agents. However, their pharmacokinetic and pharmacodynamic profiles need to be investigated. Keywords: Computational, Stevioside, Docking, Analgesic, Anti-inflammator

Significant impact of +105 A>C promoter polymorphism in IL-18 cytokine in patients with kidney stone disease

Background: Inflammation may be one cause of nephrolithiasis and the interleukin-18 (IL-18) encoding gene   polymorphisms at +105 A>C has been implicated in several inflammation related diseases. The aim of this study was to test whether IL-18+105 A>C polymorphisms could act as genetic marker for renal stone disease. A case-control study was conducted to observe the genotype distribution of IL-18+105 A>C, to elucidate the possible role of this SNP as risk factor in renal stone development and to examine its correlation with the clinico-pathologic variables.Methods: Using the Polymerase Chain Reaction-Restriction Fragment Length Polymorphism (PCR-RFLP) technique, we tested the genotype distribution of 160 nephrolithiasis patients in comparison with 200 disease free controls from the same geographical region.  Results: We observed significant differences of IL-18+105 A to C between the controls and patients with odds ratio 5.4 (P = 0.001). The prevalence of the variant genotypes AC + CC in the patients was higher than that in the controls (45% v/s 30%) and showed a significant association (P = 0.003). Moreover, the frequency per copy of the C allele of IL-18+105 A>C was found to be implicated more in patient group 0.27 as against only 0.16 in controls (P = 0.0003). Further, males and subjects with C is implicated in renal stone disease, and that the rare, C related allele is connected with higher susceptibility to nephrolithiasis.

Synthesized copper oxide nanoparticles via the green route act as antagonists to pathogenic root-knot nematode, Meloidogyne incognita

This investigation explains the green synthesis, characterization and biocontrol potential of copper oxide nanoparticles (CuONPs) against second-stage juveniles (J2s) of root-knot nematode, Meloidogyne incognita infesting chickpea. Mono-disperse, spherical, pure CuONPs were synthesized from Jatropha curcas leaf with particle sizes ranging from 5 to 15 nm in diameter. Antagonistic activities of synthesized CuONPs were studied against Meloidogyne incognita. The highest mortality of J2s was found in the 200 ppm concentration of CuONPs at 24 h of exposure. The exact concentration also showed maximum inhibition of J2s hatching from egg masses after six days of exposure. It was worth noting that 25 ppm concentration was the least effective. The pot experiment showed that CuONPs significantly reduced the root infection caused by M. incognita and enhanced chickpea plants’ growth and physiological attributes (Chlorophyll and carotenoid content). The results depicted when the concentration of CuONPs was increased, J2s mortality rate was also increased. We highlighted the antinematode influence of green synthesized CuONPs. Thus, it will offer an excellent eco-friendly strategy to optimize yield under pathogens attack and provide prospects of green synthesized-based nanoparticles development for pests control. Plants mediated CuONPs will also help in resolving the current toxicity concerns and future challenges in the agriculture

Hypoglycemia in Patients with Type-2 Diabetes Mellitus Nephropathy

Objective: To find out the frequency of hypoglycemia in Type-2 Diabetics having nephropathy Methodology: This cross-sectional observational study was carried out in Medical Teaching Institute Khyber Teaching Hospital. Department of Medicine, from August 21, 2020, to January 21, 2021. Two-hundred and eighty-one (281) patients with Type 2 diabetic nephropathy were observed in due course and were subjected to detailed history and examination. A sample of 5 ml venous blood was obtained from the patients to measure blood glucose levels to detect hypoglycemia. Experienced pathologists analyzed all investigations. Results: The mean ± Standard deviation (SD) of age in this study was 60± 10.26 years. Female patients outnumbered males in this study. Hypoglycemia was reported in 21% of patients while 79% did not have hypoglycemia. Conclusion: Type-2 diabetics having nephropathy are prone to hypoglycemia. These patients should be carefully observed for clinical and biochemical features of hypoglycemia

ZnO Nano-swirlings for Azo Dye AR183 photocatalytic degradation and antimycotic activity

The sol-gel technique was used to fabricate ZnO Nano-swirlings (ZNsw) at a predetermined agitation rate (of \u3e\u3e 1900 rpm), with around 21.94 gm of zinc acetate dihydrate and 0.2 g cetyltrimethylammoniumbromide (CTAB) and a cationic surfactant (drop-wise). The impact of the predetermined agitation condition on the molecular size and morphology of ZNsw is examined, and the outcomes are dissected by useful characterization tools and techniques viz. XRD, SEM embedded with EDS, TEM, FT-IR and UV–visible. The SEM and TEM results suggest that the product formed into a big cluster of adequate ZNsw, containing a significant quantity of folded long thread-lengths. Each group indicated a fair amount of the volume of these lengths. The photocatalytic process of ZNsw was carried out as a result of the irradiation time due to the deterioration of Azo Dye AR183, resulting in approximately 79 percent dye discoloration following an 80-min UV light irradiation in the presence of ZNsw. Additionally, the synthesized ZNsw was tested for antagonistic activity, and the growth hindrance of two plant pathogenic fungal strains found. Per cent inhibition in growth of Rhizoctonia solani and Alternaria alternata were observed in response to ZNsw

Endo-cannabinoids system and the toxicity of cannabinoids with a biotechnological approach

Cannabinoids have shown diverse and critical effects on the body systems, which alter the physiological functions. Synthetic cannabinoids are comparatively innovative misuse drugs with respect to their nature of synthesis. Synthetic cannabinoids therapy in healthy, chain smokers, and alcoholic individuals cause damage to the immune and nervous system, eventually leading to intoxication throughout the body. Relevant studies were retrieved using major electronic databases such as PubMed, EMBASE, Medline, Scopus, and Google Scholar. The extensive use of Cannabis Sativa L. (C. Sativa) and its derivatives/analogues such as the nonpsychoactive dimethyl heptyl homolog (CBG-DMH), and tetrahydrocannabivarin (THCV) amongst juveniles and adults have been enhanced in recent years. Cannabinoids play a crucial role in the induction of respiratory, reproductive, immune and carcinogenic effects; however, potential data about mutagenic and developmental effects are still insufficient. The possible toxicity associated with the prolong use of cannabinoids acts as a tumor promoter in animal models and humans. Particular synthetic cannabinoids and analogues have low affinity for CB1 or CB2 receptors, while some synthetic members like Δ9-THC have high affinity towards these receptors. Cannabinoids and their derivatives have a direct or indirect association with acute and long-term toxicity. To reduce/attenuate cannabinoids toxicity, pharmaceutical biotechnology and cloning methods have opened a new window to develop cannabinoids encoding the gene tetrahydrocannabinolic acid (THCA) synthase. Plant revolution and regeneration hindered genetic engineering in C. Sativa. The genetic culture suspension of C. Sativa can be transmuted by the use of Agrobacterium tumefaciens to overcome its toxicity. The main aim of the present review was to collect evidence of the endo-cannabinoid system (ECS), cannabinoids toxicity, and the potential biotechnological approach of cannabinoids synthesis

Effect of individual, simultaneous and sequential inoculation of pseudomonas fluorescens and meloidogyne incognita on growth, biochemical, enzymatic and nonenzymatic antioxidants of tomato (Solanum lycopersicum l.)

This study was conducted on tomato (Solanum lycopersicum cv. K-21) to investigate the bioprotective nature of Pseudomonas fluorescens and its interactive effects with Meloidogyne incognita in terms of growth biomarkers, changes in biochemical attributes and modulation in antioxidant enzymes of the tomato plant. In this study, we grew tomato plants with M. incognita and P. fluorescens in separate pots, simultaneously and sequentially (15 days prior or post) after 15 days of seed sowing. The sequential inoculation of Mi15→Pf maximally increased the root-knot index and decreased the nematode population. It was also noted that inoculation suppressed the plant growth biomarkers in comparison to control. However, maximum suppression in nematode reproduction and increment in growth and physiological attributes were observed when P. fluorescens was applied 15 days prior to the nematode (Pf15→Mi) as compared to control. All the treatments showed an increase in antioxidant enzymes. Expression of phenol content and defensive enzymes such as peroxidase (POX) and superoxide dismutase (SOD) increased, in contrast to a significant reduction in malondialdehyde (MDA) and hydrogen peroxide (H2 O2 ) contents when compared with the untreated inoculated plants. However, the highest levels of POX and SOD, and a lowest of phenol, MDA and H2 O2 were displayed in the treatment Pf15→Mi, followed by Mi+Pf and Mi15→Pf

Natural product-inspired synthesis of coumarin–chalcone hybrids as potential anti-breast cancer agents

Twelve novel neo-tanshinlactone–chalcone hybrid molecules were constructed through a versatile methodology involving the Horner–Wadsworth–Emmons (HWE) olefination of 4-formyl-2H-benzo [h]chromen-2-ones and phosphonic acid diethyl esters, as the key step, and evaluated for anticancer activity against a series of four breast cancers and their related cell lines, viz. MCF-7 (ER + ve), MDA-MB-231 (ER-ve), HeLa (cervical cancer), and Ishikawa (endometrial cancer). The title compounds showed excellent to moderate in vitro anti-cancer activity in a range of 6.8–19.2 µM (IC50). Compounds 30 (IC50 = 6.8 µM and MCF-7; IC50 = 8.5 µM and MDA-MB-231) and 31 (IC50 = 14.4 µM and MCF-7; IC50 = 15.7 µM and MDA-MB-231) exhibited the best activity with compound 30 showing more potent activity than the standard drug tamoxifen. Compound 30 demonstrated a strong binding affinity with tumor necrosis factor α (TNF-α) in molecular docking studies. This is significant because TNFα is linked to MCF-7 cancer cell lines, and it enhances luminal breast cancer cell proliferation by upregulating aromatase. Additionally, virtual ADMET studies confirmed that hybrid compounds 30 and 31 met Lipinski’s rule; displayed high bioavailability, excellent oral absorption, favorable albumin interactions, and strong penetration capabilities; and improved blood–brain barrier crossing. Based on the aforementioned results, compound 30 has been identified as a potential anti-breast cancer lead molecule