Fused Tricyclic Guanidine Alkaloids: Insights into Their Structure,Synthesis and Bioactivity

A marine natural product possesses a diverse and unique scaffold that contributes to a vast array of bioactivities. Tricyclic guanidine alkaloids are a type of scaffold found only in marine natural products. These rare skeletons exhibit a wide range of biological applications, but their synthetic approaches are still limited. Various stereochemical assignments of the compounds remain unresolved. Batzelladine and ptilocaulins are an area of high interest in research on tricyclic guanidine alkaloids. In addition, mirabilins and netamines are among the other tricyclic guanidine alkaloids that contain the ptilocaulin skeleton. Due to the different structural configurations of batzelladine and ptilocaulin, these two main skeletons are afforded attention in many reports. These two main skeletons exhibit different kinds of compounds by varying their ester chain and sidechain. The synthetic approaches to tricyclic guanidine alkaloids, especially the batzelladine and ptilocaulin skeletons, are discussed. Moreover, this review compiles the first and latest research on the synthesis of these compounds and their bioactivities, dating from the 1980s to 2022.     

Trace elements accumulation in soil and rice plants irrigated with the contaminated water

We carried out a study to see the effect of contaminated water of Nullah Dek on fine rice paddy and straw yields and trace elements accumulation in different parts of rice plants and soil. A site was selected near the bank of Nullah Dek at Kot Pindi Das in the District of Sheikhupura, Pakistan. The water of this nullah is contaminated by industrial effluents carrying different micronutrients. This water was employed to grow rice crop. Water samples were collected before transplanting and during the season with 15 days interval for analysis from 20 July to 1 November 2002 from a spot near village Shamke. Three fine rice varieties, viz. Super Basmati, Shaheen Basmati and Basmati 2000 were transplanted. These rice varieties were grown up to maturity. Paddy and straw yields data were recorded. Six composite soil samples from three random spots were collected from the experimental site before the start of the study to see the status of trace elements in soil. After the harvest of rice crop, soil, paddy and straw samples were analysed for Zn, Cu, Fe and Mn. The chemical analysis of Nullah Dek water showed that total salts concentration was greater than the safe limit, i.e. electric conductance (EC) > 1.0 dS m⁻¹. Even sodium adsorption ratio (SAR) was very high, but there was no problem of high residual sodium carbonate (RSC). Zn, Cu, Fe and Mn were present but within safe limits. The water of Nullah Dek remained within permissible limits of irrigation from onset of rainy season till 15 October. There was an increase in EC, SAR and trace elements concentrations after 15 October but within safe limits. Soil analysis revealed its saline nature, devoid of sodicity. Among trace elements, the zinc ranged between deficiency (<0.5 mg kg⁻¹) and adequate limits (>1.0 mg kg⁻¹). Copper, Mn and Fe were present in adequate amounts. After the harvest of rice crop there was a slight decrease in pH, EC_e and SAR at both the depths, while the concentrations of all trace elements were slightly increased with more in upper layer than the lower layer. Shaheen Basmati produced the maximum paddy yield followed by Basmati 2000 and then Super Basmati. The chemical analysis of paddy samples indicated a sufficient accumulation of zinc (1.68–1.78 mg kg⁻¹), copper (1.38–1.45 mg kg⁻¹), iron (6.12–6.37 mg kg⁻¹) and manganese (2.22–2.42 mg kg⁻¹). Analysis of rice straw also showed sufficient accumulation of zinc (27.50–28.50 mg kg⁻¹), copper (20.0–20.50 mg kg⁻¹), iron (270–280 mg kg⁻¹) and manganese (2.38–2.41 mg kg⁻¹).     

EFFECT OF DIFFERENT PHOSPHORUS SOURCES ON THE GROWTH,YIELD, ENERGY CONTENT AND PHOSPHORUS UTILIZATION EFFICIENCY IN MAIZE AT RAWALAKOT AZAD JAMMU AND KASHMIR,PAKISTAN

Effect of poultry manure (PM) and four inorganic phosphorus (P) fertilizers sources, i.e., diammonium phosphate (DAP), single super phosphate (SSP), nitrophos (NP) and triple super phosphate (TSP) on crop production and P utilization efficiency (PUE) of maize was studied. Both inorganic P fertilizers and PM applied alone or combined in 50:50 proportions at equivalent rate of 90 kg P₂O₅ ha^?1. Results indicated that inorganic P sources with PM significantly increased plant height, leaf area and chlorophyll content. Average values showed that combined application of inorganic P with PM increased grain yield by 19 and 41% over inorganic P and PM alone, respectively. Similarly, increase in P-uptake due to the combined application of inorganic P + PM was 17% compared to sole inorganic P. Phosphorus utilization efficiency of inorganic P was increased with PM and the highest PUE was recorded in DAP + PM. Generally, combination of DAP + PM proved superior over the remaining P fertilizers.     

Genetic variability of Iranian strains of Pseudomonas syringae pv. syringae causing bacterial canker disease of stone fruits

Strains of Pseudomonas syringae pv. syringae (Pss) were isolated from healthy and diseased stone fruits tissues sampled from 38 stone fruits orchard sites in Iran in 2010 and 2011. These strains were tested for pathogenicity and the presence of the syrB gene and were genetically characterized by using ERIC (enterobacterial repetitive intergenic consensus), REP (repetitive extragenic palindromes), and BOXAIR and IS50 (insertion sequences) primers and PCR. All 78 strains of Pss tested were moderately to highly pathogenic on Loring peach seedlings. A total of 78 isolates of the Pss amplified a 752-bp fragment with the syrB primers. To assess genetic diversity among the strains, genomic DNA was extracted from strains and used in rep-PCR and IS50-PCR analysis. Cluster analysis was performed using UPGMA. The strains of Pss were separated into nine distinguishable genotypic groups by the combination data set of both rep-PCR and IS50-PCR at 73 % similarity level. There was no significant correlation between genetic diversity and geographical origin of the isolates. These results indicate that a combination of rep-PCR and IS50-PCR fingerprinting can be used as a high resolution genomic fingerprinting method for elucidating intrapathovar diversity among strains of Pss. The results of this study demonstrated the existence of a considerable genetic diversity among Pss strains causing canker of stone fruit trees in Iran. In this study, genetic variability in Iranian strains of Pss were established, which will be of immense use in the development of resistant genotypes against this bacterial pathogen.     

Apigenin-induced suicidal erythrocyte death

Apigenin, a flavone in fruits and vegetables, stimulates apoptosis and thus counteracts cancerogenesis. Erythrocytes may similarly undergo suicidal cell death or eryptosis, characterized by cell shrinkage and phosphatidylserine exposure at the cell surface. Triggers of eryptosis include increase of cytosolic Ca(2+) activity ([Ca(2+)](i)), ceramide formation and ATP depletion. The present study explored the effect of apigenin on eryptosis. [Ca(2+)](i) was estimated from Fluo3-fluorescence, cell volume from forward scatter, phosphatidylserine exposure from annexin V binding, hemolysis from hemoglobin release, ceramide utilizing antibodies, and cytosolic ATP with luciferin-luciferase. A 48 h exposure to apigenin significantly increased [Ca(2+)](i) (≥ 1 μM), increased ceramide formation (15 μM), decreased ATP concentration (15 μM), decreased forward scatter (≥ 1 μM), and increased annexin V binding (≥ 5 μM) but did not significantly modify hemolysis. The effect of 15 μM apigenin on annexin V binding was blunted by Ca(2+) removal. The present observations reveal novel effects of apigenin, i.e. stimulation of Ca(2+) entry, ceramide formation and ATP depletion in erythrocytes with subsequent triggering of suicidal erythrocyte death, paralleled by cell shrinkage and phosphatidylserine exposure.     

Supercritical Fluid Extraction of Phenolic Compounds and Antioxidants from Grape (Vitis labrusca B.) Seeds

Supercritical fluid extraction (SFE) technique was applied and optimized for temperature, CO₂ pressure and ethanol (modifier) concentration using orthogonal array design and response surface methodology for the extract yield, total phenols and antioxidants from grape (Vitis labrusca B.) seeds. Effects of extraction temperature and pressure were found to be significant for all these response variables in SFE process. Optimum SFE conditions (44?~?46 °C temperature and 153?~?161 bar CO₂ pressure) along with ethanol (<7 %) as modifier, for the maximum predicted values of extract yield (12.09 %), total phenols (2.41 mg GAE/ml) and antioxidants (7.08 mg AAE/ml), were used to obtain extracts from grape seeds. The predicted values matched well with the experimental values (12.32 % extract yield, 2.45 mg GAE/ml total phenols and 7.08 mg AAE/ml antioxidants) obtained at optimum SFE conditions. The antiradical assay showed that SFE extracts of grape seeds can scavenge more than 85 % of 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radicals. The grape seeds extracts were also analyzed for hydroxybenzoic acids which included gallic acid (1.21?~?3.84 μg/ml), protocatechuic acid (3.57?~?11.78 μg/ml) and p-hydroxybenzoic acid (206.72?~?688.18 μg/ml).     

免耕条件下秸秆还田对冬小麦-夏玉米轮作系统土壤呼吸及土壤水热状况的影响

【目的】研究免耕条件下秸秆还田对旱地冬小麦-夏玉米轮作系统土壤呼吸及土壤水热状况的影响。【方法】2011年10月至2014年9月,在陕西杨凌设置秸秆全量还田+施肥（S1F1）、秸秆全量还田+不施肥（S1F0）、秸秆半量还田+施肥（S1/2F1）、秸秆半量还田+不施肥（S1/2F0）、秸秆不还田+施肥（S0F1）、秸秆不还田+不施肥（S0F0）6 种不同耕作处理的3年定位试验,测定并分析不同耕作处理下土壤呼吸、土壤水热状况、作物产量、土壤耕作层有机碳含量的差异。【结果】在冬小麦生育期内,各处理土壤呼吸速率均呈先下降后升高再下降的趋势;在夏玉米生育期内,各处理土壤呼吸速率均表现为先升高后下降的趋势。同一生育期内各处理土壤呼吸平均速率及呼吸总量依次为S1F1＞S1/2F1＞S1/2F0＞S0F1＞S1F0＞CK,同种作物不同生育期之间,各处理土壤生育期呼吸总量有逐年降低的趋势。整个研究周期内,土壤温度的变化趋势与每月平均气温的变化趋势相似,不同处理在同一生育期内的土壤温度变化趋势相近,且各处理生育期土壤平均温度均随土壤深度的增加而降低;不同秸秆还田处理冬季土壤温度均高于对照,但生育期土壤平均温度均低于对照。土壤含水量随土壤深度的增加而降低,但受降雨影响,不同轮作周期之间的土壤含水量波动较大,各处理同一生育期的土壤平均含水量均表现为S1F0＞S1F1＞S1/2F0＞S1/2F1＞CK＞S0F1,且不同秸秆还田处理的土壤含水量与对照间的差异均显著（P＜0.05）;土壤温度能够解释土壤呼吸速率变化的32.5%-60.4%,土壤含水量能够解释土壤呼吸速率变化的38.4%-82.5%,不同土层深度间,5 cm土层的温度与土壤呼吸的拟合度性最高,而10-20 cm土层的含水量与土壤呼吸的拟合度最高。相同年份内,不同处理冬小麦和夏玉米产量均表现为S1F1＞S1F0＞S1/2F1＞S0F1＞S1/2F0＞CK,这个研究周期内,冬小麦产量逐年增加,夏玉米在前两季表现为增产,但受极端炎热天气的影响,第三季的产量明显降低。单季作物收获后,各处理同一土层深度的有机碳含量均表现为S1F1＞S1/2F1＞S1F0＞S1/2F0＞S0F1＞CK。且不同秸秆还田处理的土壤有机碳含量逐年升高。【结论】长期免耕秸秆还田能够有效降低农田土壤碳排放、提高农田土壤水分利用率及冬季土壤温度、提高作物产量及土壤有机碳含量。不同秸秆还田处理间以S1F0处理的效果最优。     

Kinetics study on a novel natural inhibitor of alpha-chymotrypsin

The mechanism of inhibition of alpha-chymotrypsin by benzoylsalireposide (1), a phenolic glycoside isolated from Symplocos racemosa, was investigated. Lineweaver-Burk and Dixon plots and their secondary replots showed that 1 was a non-competitive inhibitor of this enzyme with the Ki value of 29.60 microM.