Phytotoxicity of Phthalate Plasticisers: 1. DIAGNOSIS AND COMMERCIAL IMPLICATIONS

The toxicity caused by a volatile constituent from certain samplesof flexible polyvinyl chloride (PVC) was due to dibutyl or diisobutylphthalate (DBP or DIBP) plasticisers. It has caused seriousfinancial losses in the horticultural industry. The two phthalateesters have low volatilities, so any toxicity lasts for manyyears. Radish (Raphanus sativus L. cv. Cherry Belle) seedlings,exposed to an air stream containing 160–180 ng dm^–3of butyl phthalates developed chlorotic leaves within 3–4d and died within 12 d. Neither dioctyl nor diisodecyl phthalate(DOP nor DIDP) produced damage in the test plants. Measurementsof photosynthetic and respiratory gas exchange in intact shootsof affected radishes showed that photosynthesis was severelyinhibited whilst respiration was virtually unaffected. Electronmicrographs of sections from young leaves showed disruptionof thylakoid formation and granai stacking. In mature leaves,thylakoids and grana were well formed but chloroplasts wereswollen and the thylakoids were pushed towards the vacuolarside of the chloroplast. Sensitivity to toxic phthalates variesbetween species; all members of the Cruciferae tested were susceptible,tomato less so, and lettuce and ryegrass were resistant. Toxicityof DIBP, from PVC glazing strip, caused a reduction in cropvalue of ?20 000 per acre per year in commercially grown, monocroptomatoes. Key words: Phthalates, plasticiscd PVC, radish bioassay, glasshouse, tomato, toxicity     

INSECTICIDES: THEIR ROUTE OF ENTRY, MECHANISM OF TRANSPORT AND MODE OF ACTION

(1) The assumption that the circulatory system of the insect is instrumental in transporting insecticides to their site of action appeared not to be based on good evidence. On the contrary, experiments specifically designed to test the hypothesis provided ample evidence to refute the idea. Salient points to disprove the haemolymph route of entry can be summed up as follows: (a) A topically applied dose of insecticide does not readily penetrate the insect and the minor fraction that does so is largely retained in the body wall. The small amount that actually passes into the blood is too small to cause symptoms of toxicity if injected into the haemocoel. (b) The amount of insecticide present in the haemolymph (and CNS) does not appear to have any bearing on toxicity - internally introduced insecticides are, in fact, basically very much less toxic than those externally applied. Where injected doses appear to be more toxic than equal amounts topically applied, this is due to the boosting effect of organic solvent carriers. Tests with parabiotically joined insects provide support for the view that haemolymph-borne insecticide is of no consequence. (c) The topographical proximity of the locus of external application with the site of action (the thoracic ganglia) seems to be important irrespective of the general direction of the blood flow, and this should not be so if the circulatory system was instrumental in the transport of insecticide. (d) The introduction into the haemocoel of material such as olive oil, which is an excellent absorbent for insecticides, does not affect the toxicity (speed of action) of externally applied compounds to a significant extent. It should have a pronounced effect if haemolymph-borne insecticide were an essential element in the process of poisoning. (e) As judged by speed of action, blocking of the blood circulation does not hamper the insecticide's movement to the site of action. (2) Only two other feasible routes remain. (a) The insecticide might reach the CNS via peripheral nerves and nerve cord, but the results of histochemical assays of cholinesterase inhibition in the insect's CNS make the idea improbable for organo-phosphates. The nerve route is also incompatible with the observation that a wax barrier blocked the movement in and over the body wall so as to delay the onset of symptoms of toxicity, as such a barrier would not hinder movement into lateral nerves near the locus of application. (6) The only other feasible alternative, i.e. entry by means of lateral transport via the integument of the body wall and tracheae, is supported by autoradiographic and other evidence which showed the insecticide to accumulate in the tracheal system. It is further supported by the fact that inter-tracheal introduction is faster acting than topical treatment, indicating that the tracheal system offers a very effective pathway to the internal organs. (3) Regarding the mechanism of entry, earlier reviews and text books maintain this to be associated exclusively with penetration into and through the integument by a physicochemical process. However, there is good evidence to show that an active process (requiring metabolic activity as the driving force) plays an essential part in lateral movement in the integument - the epidermis, being the only living tissue continuous throughout the general integument, must perform this function. (4) As to the mode of action, the new hypothesis expounded here implies a single mode based on the fact that insecticides cause the extrusion of fluid from the epidermis into the cuticle and beyond, fluid lost from the epidermal cell layer being replaced from haemolymph and internal tissues. The precise mechanism is not clear but could conceivably involve an as yet hypothetical local endocrine system designed to keep the water content in the integument within certain limits. It is suggested that water extrusion affects the integument's permeability to respiratory gases, resulting in a rate of respiration not commensurate with metabolic need, and that the insecticide's arrival in the trachea (tracheoles) of the CNS leads to excitation and knockdown. Death is thought most likely to be due to dehydration of the CNS and subsequent histological degeneration.     

THE MODE OF ACTION OF VITAMIN D

1. The purpose of this review article is to re-evaluate and integrate many of the observations related to the physiological effects of vitamin D, using as a working hypothesis the concept that the vitamin may be acting analogously to a steroid hormone in terms of its ability to interact with genetic information and ultimately elicit a physiological response. Prior to this time the problem of the mechanism of action of vitamin D has primarily been approached from the point of view that the vitamin was acting as a cofactor for some specific enzymic reaction. 2. The physiological activities of vitamin D are integrated with those of parathyroid hormone to provide a homeostatic control for the regulation of primarily calcium and secondarily phosphate metabolism. It is proposed that the role of vitamin D in this homeostatic control mechanism is older and more fundamental than that of parathyroid hormone. The interaction of vitamin D on skeletal calcium metabolism may have evolved before the effects of the vitamin on intestinal calcium absorption. 3. There are several physiological defects of calcium metabolism—rickets, osteo-malacia, vitamin D-resistant rickets and idiopathic hypercalcaemia—all of which may be a consequence of an aberration in one or another of the interlocking steps of the vitamin D-dependent and calcium-dependent homeostatic control mechanism. 4. The most thoroughly established action of vitamin D in vivo is to promote or facilitate the intestinal absorption of calcium. Although the exact biochemical details of this process are not available, this may involve vitamin D-mediated synthesis of the appropriate enzyme systems or the alteration of membrane structure necessary for calcium absorption. It is not yet unequivocally established whether calcium absorption is an energy-dependent active transport process or is a passive carrier-mediated or simple diffusion process. 5. The exact action of vitamin D on bone metabolism is not as well established, but the primary effect of the vitamin is likely to mediate bone resorption. The vitamin D-dependent activities of the cell in both the intestine and bone are to absorb calcium and transfer it to the blood. 6. No direct effects of vitamin D on intestinal absorption of phosphate have been found. Furthermore the validity of a vitamin D-mediated renal reabsorption of phosphate is questioned, for the major effects of vitamin D are cation oriented. If the renal effects of vitamin D are true, it is postulated that the mechanism of action of the vitamin here on the anion, phosphate, is fundamentally different from its cation oriented mechanism. 7. There is a lag in the action of vitamin D on the vitamin mediated: (a) transport of calcium both in vivo in rats and chicks, and in vitro with everted intestinal slices; (b) the apparent increased permeability of intestinal mucosa; (c) increased levels of citric acid in serum or bone; (d) the increased incorporation of radioactive inorganic phosphorus into intestinal mucosa phospholipids. As shown by the use of radioactive vitamin D, this lag is not due to a lack of the vitamin in the target organs. 8. Whereas large, unphysiological doses of radioactive vitamin D localize in all tissues and all subcellular fractions, small physiological doses of radioactive vitamin D localize predominantly in the nucleus of the intestinal mucosa. The amount of vitamin D localized in the nucleus would appear to be too low for the vitamin to function as a cofactor, and is more indicative of an interaction on or with deoxy-ribonucleic acid. 9. Actinomycin D, an inhibitor of DNA-directed RNA synthesis, inhibits the action of vitamin D in mediating intestinal calcium absorption and bone resorption. Vitamin D also stimulates messenger-RNA synthesis in intestinal mucosa within 1/2 hr. of vitamin treatment. Vitamin D may play a crucial role, along with parathyroid hormone and calcium, in a DNA, gene-dependent, homeostatic control mechanism for cal, ium metabolism. In this system the vitamin D molecule has certain very specific structural requirements which are probably a reflection of the specificity of its receptor molecule, rather than structural requirements for a cofactor-enzyme relationship.     

动脉壁脑啡肽的含量,存在部位及作用途径

用放射免疫法测得兔动脉的亮氨酸脑啡肽(L-ENK)和甲硫氨酸脑啡肽(M-ENK)样免疫活性物的含量(pg/mg组织湿重)分别为耳动脉38.99±17.29,134.67±8.11;肾动脉31.10±7.76,93.60±18.22,肠系膜动脉25.70 13.60,88.43±18.16。动物经注射交感神经末梢化学切割剂6-OHDA后,这三种动脉中L-ENK样免疫活性物的含量均明显下降(P<0.001);切除颈上神经节使支配耳动脉的交感神经溃变后,或离体耳动脉条受电场刺激后,脑啡肽(ENK)样免疫活性物的含量也都显著下降(P<0.001);但注射利血平则无明显影响,用荧光法测定培育动脉条的浴槽液中NE的含量,观察到ENK可抑制电场刺激所引起的NE的释放。结果提示,动脉壁的L-ENK和M-ENK存在于交感神经末梢中,它可因受电场刺激而释放,可能通过激活突触前膜阿片受体,减少交感神经末梢释放NE,从而抑制动脉的收缩活动。     

STUDIES IN THE MODE OF ACTION OF INSECTICIDES

Acetylcholine, choline chloride, acetyl-β-methylcholine, benzoylcholine, carbamyl choline, adrenaline and d -tubocurarine are non-toxic when injected into the locust. Prostigmine is also non-toxic, and eserine considerably less toxic to the locust than to man.
The toxic effect of tetraethyl pyrophosphate (TEPP) cannot be antagonized by injection of atropine or enhanced by d -tubocurarine.
The injection of acetylcholine chloride following injection of TEPP does not affect subsequent mortality.
These findings are discussed, and it is suggested that the physiology of the nervous system of the insect is unlike that of the mammal, neither cholinesters nor adrenaline being concerned in it. Phosphorus insecticides are thought to inhibit a general esterase not specifically connected with cholinesters.     

Dormancy in Seeds of Charlock: III. OCCURRENCE AND MODE OF ACTION OF AN INHIBITOR ASSOCIATED WITH DORMANCY

The dormancy of charlock seeds appears to be associated withthe presence of an inhibitor which accumulates within the seed.This inhibitor diffuses into the external solution when seedsare placed in water under germination conditions or controlledexperimental conditions. A small quantity of inhibitor diffusesfrom the seed coats but most arises from the embryo. The increasein temperature was measured by comparing the relative growth-ratesof the radicles of excised charlock embryos in water and intest solutions of diffusate. The results suggest that the rateof accumulation of inhibitor in the external solution is controlledby diffusion, and that there is continuous production of inhibitorin the tissues of the embryo which have a low oxgyen tension.The critical concentration of the inhibitor which completelyprevents cell elongation is rapidly attained in seeds whichare dormant. The inhibitor is unlikely to be a mustard oil,such as allylisothio-cyanate.     

EVIDENCE ON THE SITE OF ACTION OF GROWTH RETARDANTS

1. The ability of five growth retardants to inhibit the GA-inducedand endogenous growth of Avena leaf sections has been investigated.The retardants vary in effectiveness. The order, from most effectiveto least, is Phosfon D, Amo-1618, C011, CCC and B995. 2. The inhibition of growth caused by Phosfon D and Amo-1618is not reversed by GA. It is apparent that the retardants donot compete with GA at the site of GA-action. 3. Addition of IAA will partially reverse the inhibition inducedby Phosfon D or Amo-1618. It is concluded that the retardantsact in part in Avena leaf sections by interfering with the auxinmetabolism of the tisssue. ¹ Supported in part by grants G-14578 and GB-1950 from the NationalScience Foundation ² Present address: Department of Botany, University of Washington,Seattle, Washington     

精胺抑制人精子的体外受精能力

以精子穿透去透明带仓鼠卵试验(SPA)为模型,评价了精胺对人精子体外受精能力的影响。精胺(0.25—8.0mmol/L)可抑制人精子体外获能和受精,其抑制作用与精胺浓度呈正相关,此种抑制作用是可逆的。用 HPLC 测定精子精胺含量表明,精子获能后精胺含量明显下降。dbcAMP(0.5—1.0mmol/L)或咖啡因(10mmol/L)可拮抗精胺抑制人精子体外获能。其拮抗作用随 dbcAMP 浓度而增强。钙离子载体 A 23187 2/μmol/L 或胰蛋白酶0.05%均可拮抗精胺抑制人精子穿卵率。上述结果提示,精胺可能通过降低精子 cAMP 含量和抑制钙内流或顶体酶活性,从而阻止人精子体外获能和受精。     

MODE OF ACTION OF MALEIC HYDRAZIDE ON THE GROWTH OF ESCHERICHIA COLI AND AVENA COLEOPTILE SECTIONS

1. MH was found to suppress the growth and respiration of E. colias well as the IAA-induced growth of Avena coleoptile sections.
2. These suppressions could be reversed more or less strikinglyby the addition of a trace of heavy metals such as Co, Mn, Ni,Zn, Cu, or Mo.
3. The reversal could also be achieved by cysteine,thioglycollate,or fumarate, the latter two substances being,however, lesseffective.
4. The inhibition of the growth of E.coli by MH was completelyrelieved by the addition of IAA. Conversely,the inhibitionof the microbial growth by high concentrationsof IAA couldbe relieved by the addition of MH.
5. It was inferredthat MH may block certain heavy metal-catalyzedprocess, inwhich some thiol substance and IAA are participating,probablyby combining with the heavy metal.

(Received June 23, 1960; )     

ACTION MODE,PERSISTENCE AND CONTROL VALUE OF FIPRONIL FOR RICE GRASSHOPPERS OXYA (ORTHOPTERA: CANTANTOPIDAE)*

Abstract From June to Oct. 1996, cage and field experiments with Fipronil, a new insecticide from the phenyl pyrazole family, were carried out in Hanzhong basin, Shaanxi Prov. The aim was to evaluate the action mode, persistence and control value of Fipronil in rice grasshoppers management. The main results were as follows: ¹ at low doses of 4 g a. i. /ha and 8 g a. i. /ha, Fipronil was found to be an effective contact and stomach pesticide against Oxya spp. The knocking effect of contact was quicker than that of stomach; ² the residual effect of Fipronil on Oxya spp. was over 3 weeks, significantly longer than that of conventional insecticides; ³ the difference between effects of 4 g a. i. /ha and 8 g a. i. /ha was mainly shown in terms of survival time of the grasshoppers after treatment, and there was almost no difference as to control results; ⁴ one month after the treatment, the density of Oxya in quadrats treated by Fipronil was significantly lower than that in quadrats treated with Fenpropathoursin, and the application of Fipronil retrieved 12. 6% of rice production loss when compared with the output in control field.     

锐劲特对稻蝗(直翅目:斑腿蝗科)的作用方式、持效性及防治价值的研究(英文)

１９９６年６月至１０月,在陕西省汉中盆地对锐劲特（苯基吡唑类新型杀虫剂）进行了笼罩和田间实验。目的在于弄清该杀虫剂对稻蝗的作用方式及防治价值。结果如下：１）低剂量的锐劲特（４ ｇ／ｈａ和８ ｇ／ｈａ活性物质）对稻蝗有很强的触杀和胃毒作用。触杀击倒的作用较胃毒的作用迅速;２）锐劲特对稻蝗的控制作用长达３周以上,明显长于通用杀虫剂;３）两种剂量的锐劲特作用于稻蝗时,其区别只表现在施药后稻蝗存活时间的长短,在控制效果上无明显差异;４）与空白对照田的产量相比,施用锐劲特后可挽回１２％的稻谷损失。     

Eurocin,a New Fungal Defensin: STRUCTURE,LIPID BINDING,AND ITS MODE OF ACTION*

Antimicrobial peptides are a new class of antibiotics that are promising for pharmaceutical applications because they have retained efficacy throughout evolution. One class of antimicrobial peptides are the defensins, which have been found in different species. Here we describe a new fungal defensin, eurocin. Eurocin acts against a range of Gram-positive human pathogens but not against Gram-negative bacteria. Eurocin consists of 42 amino acids, forming a cysteine-stabilized α/β-fold. The thermal denaturation data point shows the disulfide bridges being responsible for the stability of the fold. Eurocin does not form pores in cell membranes at physiologically relevant concentrations; it does, however, lead to limited leakage of a fluorophore from small unilamellar vesicles. Eurocin interacts with detergent micelles, and it inhibits the synthesis of cell walls by binding equimolarly to the cell wall precursor lipid II.     

UNDERSTANDING THE MODE OF ACTION OF L-NUCLEOSIDES AS ANTIVIRAL AGENTS: A MOLECULAR MODELING APPROACH

Computer modeling studies have been performed on the several pairs of D- and L-nucleoside inhibitors with the HIV-1 RT model. Additionally, clinically important M184V mutation, which confers the viral resistance against 3TC and FTC, were studied by the same modeling system.     

NATURE OF THE ACTION CURRENT IN NITELLA : VI. SIMPLE AND COMPLEX ACTION PATTERNS

The experiments indicate that the protoplasm of Nitella consists of an aqueous layer W with an outer non-aqueous surface layer X and an inner non-aqueous surface layer Y. The potential at Y is measured by the magnitude of the action curve and the potential at X by the distance from the top of the action curve to the zero line. These potentials appear to be due chiefly to diffusion potentials caused by the activity gradients of KCl across the non-aqueous layers X and Y. The relative mobilities of K⁺ and Cl^- in X and in Y can be computed and an estimate of the activity of KCl in W can be made. In the complete resting state the mobilities of K⁺ and Cl^- in X are not very different from those in Y. The action curve is due to changes in Y which suddenly becomes very permeable, allowing potassium to move from the sap across Y into W, and thus losing its potential. A gradual loss may be due to changes in ionic mobility in Y. When recovery is incomplete and Y has not yet regained its normal potential a stimulus may cause a loss of the potential at Y giving an action curve of small magnitude. The magnitude may vary in successive action curves giving what is called a complex pattern in contrast to the simple pattern observed when recovery is complete and all the action curves are alike. Complex patterns occur chiefly in cells treated with reagents. Untreated cells usually give simple patterns. A variety of complex action patterns is discussed. It is evident that the cells of Nitella show much more variation than such highly specialized cells as muscle and nerve which give stereotyped responses. In some cases it may be doubtful whether the all-or-none law holds.     

STUDIES ON PLANT GROWTH-REGULATING SUBSTANCES XI. AUXIN ANTAGONISM IN RELATION TO A THEORY ON MODE OF ACTION OF ARYL- AND ARYLOXY-ALKANECARBOXYLIC ACIDS

A study has been made of the antagonistic effects of a range of phenoxy and other acids on the growth-promoting activity of a number of auxins as assessed by the Avena cylinder and pea curvature tests. The compounds examined as inhibitors were selected on a logical basis, these molecules not possessing the structural requirements considered necessary for growth-regulating activity, yet possessing groupings which might allow them to accumulate at a site of action from which the growth response by auxins might be initiated. Our previous demonstrations that inactive stereoisomers of x-aryloxy propionic acids can competitively inhibit the activity of their active enantiomorph has been confirmed and a similar antagonism has been found to operate with other inactive aryloxy acids. Such competitive antagonism is discussed in relation to a 'three-point' contact theory on mode of action.     

PHYTOCHROME ACTION IN ORYZA SATIVA L. III. THE SEPARATION OF PHOTOPERCEPTIVE SITE AND GROWING ZONE IN COLEOPTILES, AND AUXIN TRANSPORT AS EFFECTOR SYSTEM

• 1 In 4-day-old etiolated rice seedlings, 3 mm of the coleoptile tip did mainly perceive the photostimulus to cause the phytochrome-dependent inhibition of coleoptile elongation. At this age, cell elongation occurred most in the middle portion of coleoptiles in the dark, and was reversibly controlled by a brief exposure of the tip to red and far-red light. Thus, the photoperceptive site was evidently separated from the growing zone in intact rice coleoptiles.
• 2 The red-light-induced inhibition of coleoptile elongation was nullified by the removal of tip followed by the exogenous application of IAA. The sensitivity of thus treated coleoptiles to IAA was gradually lost during intervening darkness between the irradiation and the decapitation, and a 50% loss was obtained at ca. 6th hour at 26°C.
• 3 Polar auxin transport from coleoptile tips was remarkably prevented at the period between, at least, 2nd and 4th hour after red irradiation, and it recovered to the level of dark control by the 6th hour. Far-red light given immediately after red irradiation reversed the yield of diffusible auxin up to that of far-red control.