TAXONOMIC BIBLIOGRAPHY OF VASCULAR AQUATIC PLANTS IN SOUTHERN AFRICA

SUMMARY

The length mass relationship for a Labeo capensis population is described by the equation M = 0,0134 L^2'999 where 2,999 represents a constant the value of which indicates isometric growth. There is very little difference between the length/mass relationship for males and that for females and this is similar to the results found by Mulder (1973) for L. capensis in the Vaal River. The length/mass relationships for gravid males and females are different from that of the population as a whole indicating that maturity does result in a change of the body form which is in accordance with the results of Mulder (1973).

A modified formula to take into account, small length intervals of an age group, is used to calculate the relative condition factor for Labeo capensis from the Caledon River for a consecutive “winter” and “summer” period. The results show that the conhd1t10ni for Labeo capensis of the 0⁺, 1⁺ and 2⁺ age groups is better in the summer period than in the winter period, whereas in the older age groups 3⁺ to 5⁺ the condition in winter is better than in summer. This can be attributed to the attainment of sexual maturity at the age of 3⁺ years and the presence of large quantities of fat deposited in the body during the winter months, which are then utilised for the development of the gonads prior to spawning. These results are similar to those obtained for the same species by Mulder (1973) in the Vaal River and by Bloemhof (1974) in the Hardap Dam.     

Synthesis,Characterization, and Anti‐Amoebic Activity of N‐(Pyrimidin‐2‐yl)benzenesulfonamide Derivatives

A new series of N‐(pyrimidin‐2‐yl)benzenesulfonamide derivatives, 3a – 3i and 4a – 4i , was synthesized from pyrimidin‐2‐amines, 2a – 2i , with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds were elucidated by elemental analysis, FT‐IR, ¹H‐ and ¹³C‐NMR, and ESI mass‐spectral data. In vitro anti‐amoebic activity was evaluated against HM1 : IMSS strain of Entamoeba histolytica. The IC₅₀ values were calculated by using the double dilution method. The results were compared with the IC₅₀ value of the standard drug ‘metronidazole’. The selected compounds were tested for their cytotoxic activities by cell‐viability assay using H9C2 cardiac myoblasts cell line, and the results indicated that all the compounds displayed remarkable >80% viabilities to a concentration of 100 μg/ml.     

Cyclopaldic Acid,Seiridin, and Sphaeropsidin A as Fungal Phytotoxins,and Larvicidal and Biting Deterrents against Aedes aegypti (Diptera: Culicidae): Structure?Activity Relationships

Aedes aegypti L. is the major vector of the arboviruses responsible for dengue fever, one of the most devastating human diseases. From a preliminary screening of fungal phytotoxins, cyclopaldic acid ( 1 ), seiridin ( 2 ), sphaeropsidin A ( 4 ), and papyracillic acid ( 5 ) were evaluated for their biting deterrent and larvicidal activities against Ae. aegypti L. Because compounds 1, 2, 4 , and 5 exhibited mosquito biting deterrent activities and 1 and 4 demonstrated larvicidal activities, further structure? activity relationship studies were initiated on these toxins. In biting‐deterrence bioassays, 1, 2, 4 , and 5 , 3,8‐didansylhydrazone of cyclopaldic acid, 1F , 5‐azidopentanoate of cyclopaldic acid A, 1G , the reduced derivative of cyclopaldic acid, 1 H , isoseiridin ( 3 ), 2′‐O‐acetylseiridin ( 2A ), 2′‐oxoseiridin ( 2C ), 6‐O‐acetylsphaeropsidin A ( 4A ), 8,14‐methylensphaeropsidin A methyl ester ( 4B ), and sphaeropsidin B ( 4C ) showed activities higher than the solvent control. Sphaeropsidin B ( 4C ) was the most active compound followed by 2A , while the other compounds were less active. Biting‐deterrence activity of compound 4C was statistically similar to DEET. In the larvicidal screening bioassays, only compounds 1 and 4 demonstrated larvicidal activities. Based on LD₅₀ values, compound 4 (LD₅₀ 36.8 ppm) was significantly more active than compound 1 (LD₅₀ 58.2 ppm). However, the activity of these compounds was significantly lower than permethrin.     

Synthesis and characterization of 5,7-dihydroxyflavanone derivatives as novel protein tyrosine phosphatase 1B inhibitors

A series of 5,7-dihydroxyflavanone derivatives were synthesized and identified as reversible and competitive protein tyrosine phosphatase (PTP) 1B inhibitors with IC₅₀ values in the micromolar range. Compound 4k had the most potent in vitro inhibition activity against PTP1B (IC₅₀ = 2.37?±?0.37 μM) and the greatest selectivity (3.7-fold) for PTP1B relative to T-cell protein tyrosine phosphatase. Cell-based studies revealed that 4k was membrane-permeable and enhanced insulin receptor tyrosine phosphorylation in CHO/hIR cells.     

Structure-activity relationships of bergenin derivatives effect on α-glucosidase inhibition

The α-glucosidase inhibitory activities of bergenin derivatives were evaluated. Bergenin derivatives were synthesized from bergenin which is a characteristic compound of B. ligulata. A new bergenin derivative, 11-O-(3′,4′-dimethoxybenzoyl)-bergenin showed the highest potent inhibitory activity among those of bergenin derivatives. The presence of substituents at 3′,4′-position in bergenin derivatives altered the α-glucosidase inhibitory activity. 11-O-(3′,4′-dimethoxybenzoyl)-bergenin was noncompetitive inhibitor for α-glucosidase. The present study reveals that bergenin derivatives could be classified as a new group of α-glucosidase inhibitors.     

Enantio-Selectivity of Human Nucleoside Monophosphate Kinases

Over recent years, there has been a renewed interest in the development of l-nucleosides as safe and efficacious drugs for the treatment of viral infections. Biological activity of these compounds requires phosphorylation to their triphosphate form, involving nucleoside monophosphate kinases in the second step. In order to characterize the activation pathway of l-nucleosides of the pyrimidine series, we studied the enantio-selectivity of human uridylate-cytidylate and thymidylate kinases. The results showed that these enzymes are only weakly enantio-selective and are thus probably involved in the activation of l-nucleosides in vivo. An activation pathway for telbivudine (l-dT) was therefore proposed.     

Structure-activity relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton

Selective estrogen receptor (ER) down-regulators (SERDs) are pure ER antagonists that also induce ER degradation upon binding to the receptor. Although SERDs have been developed for the treatment of ER-positive breast cancers for nearly a decade, their precise mechanism(s) of action and structure-activity relationship are still unclear. Generally, Western blotting is used to examine the effects of SERDs on ER protein levels, but the methodology is low-throughput and not quantitative. Here, we describe a quantitative, high-throughput, luciferase-based assay for the evaluation of SERDs activity. For this purpose, we established stable recombinant HEK-293 cell lines expressing ERα fused with emerald luciferase. We also designed and synthesized new diphenylmethane derivatives as candidate SERDs, and evaluated their SERDs activity using the developed system in order to examine their structure-activity relationship, taking EC₅₀ as a measure of potency, and E_max as a measure of efficacy.     

Structural requirement of tunicamycin V for MraY inhibition

Elucidating a structure-activity relationship study by evaluating a series of truncated analogues is a simple but important and effective tactic in medicinal chemistry based on natural products with a large and complex chemical structure. In this study, a series of truncated analogues of tunicamycin V were designed and synthesized and their MraY inhibitory activity was investigated in order to gain insight into the effect of these moieties on MraY inhibition.     

乌牛早茶园蜡蝉类与其8种天敌空间关系的聚块样方方差分析

为了分析在不同聚块大小条件下,天敌对蜡蝉类Fulgoroidea空间上跟随关系的密切程度、聚集原因和聚集范围,为评价蜡蝉类的天敌优势种和确定样方大小提供科学依据,运用聚块样方方差分析法、灰色关联度法、空间聚集强度指数法、种群聚集均数法和ρ指数法对安徽省合肥市乌牛早茶园不同大小聚块条件下的蜡蝉类及其8种天敌进行分析。蜡蝉类与其8种天敌均方差峰值时聚块样方数的关联度分析结果表明:与蜡蝉类空间上跟随关系密切的前三位天敌依次是茶色新圆蛛Neoscona theisi(0.8010)、草间小黑蛛Erigonidium graminicolum(0.7617)和三突花蟹蛛Misumenops tricuspidatus(0.7613)。在聚块内基本样方数K为1、2、4、8时,随着聚块内基本样方数的增多,聚集分布格局时的扩散系数C不断增大,均匀和随机格局时扩散系数不断减小。聚块内基本样方数K为1、2、4、8时其相互之间的蜡蝉类及其天敌的空间分布聚集程度差异均不显著。蜡蝉类及其天敌的种群聚集均数λ多数情况均大于2,其聚集是该虫本身原因引起的,并且λ的绝对值随着聚块内基本样方数的增加而不断增大。用蜡蝉类不同大小聚块的ρ指数判断个体群聚集时的最小范围是聚块中有4个基本样方,即本文的16 m~2。为该虫抽样时确定样方大小提供了科学依据。聚块样方方差分析法是分析害虫与天敌空间关系的一种简便而又实用的方法。