New Caledonia: A Hot Spot for Valuable Chemodiversity Part 3: Santalales,Caryophyllales, and Asterids

The flora of New Caledonia encompasses more than 3000 plant species and an endemism of almost 80%. New Caledonia is even considered as one of the 34 ‘hot spots’ for biodiversity. Considering the current global loss of biodiversity and the fact that several drugs and pesticides become obsolete, there is an urgent need to increase sampling and research on new natural products. In this context, here, we reviewed the chemical knowledge available on New Caledonian native flora from economical perspectives. We expect that a better knowledge of the economic potential of plant chemistry will encourage the plantation of native plants for the development of a sustainable economy which will participate in the conservation of biodiversity. This review is divided into three parts, and the third part which is presented here summarizes the scientific literature related to the chemistry of endemic santalales, caryophyllales, and asterids. We show that the high rate of endemism is correlated with the originality of phytochemicals encountered in New Caledonian plants. A total of 176 original natural compounds have been identified from these plants, whereas many species have not been investigated so far. We also discuss the economic potential of plants and molecules with consideration of their medicinal and industrial perspectives. This review finally highlights several groups, such as Sapotaceae, that are unexplored in New Caledonia despite the high chemical interest in them. These plants are considered to have priority in future chemical investigations.     

Regulation of testicular function in men: implications for male hormonal contraceptive development

In the adult male, the testes produce both sperm and testosterone. The function of the testicles is directed by the central nervous system and pituitary gland. Precise regulation of testicular function is conferred by an elegant feedback loop in which the secretion of pituitary gonadotropins is stimulated by gonadotropin hormone-releasing hormone (GnRH) from the hypothalamus and modulated by testicular hormones. Testosterone and its metabolites estradiol and dihydrotestosterone (DHT) as well as inhibin B inhibit the secretion of the gonadotropins both directly at the pituitary and centrally at the level of the hypothalamus. In the testes, LH stimulates testosterone synthesis and FSH promotes spermatogenesis, but the exact details of gonadotropin action are incompletely understood. A primary goal of research into understanding the hormonal regulation of testicular function is the development of reversible, safe and effective male hormonal contraceptives. The administration of exogenous testosterone suppresses pituitary gonadotropins and hence spermatogenesis in most, but not all, men. The addition of a second agent such as a progestin or a GnRH antagonist yields more complete gonadotropin suppression; such combination regimens effectively suppress spermatogenesis in almost all men and may soon bring the promise of hormonal male contraception to fruition.     

Examining male roles in population policies and family planning programs

"This paper will discuss the following: why population policies and programs have traditionally focused on women; what the limitations of current male contraceptives are and why research into new methods [has] proved unfruitful; and why these policies and programs would be more productive if they were to direct more attention toward men."     

BET proteins: Investigating BRDT as a potential target for male contraception

While many contraception options are available for women, birth control methods for men are limited to condoms and vasectomy. Past research into male contraceptives has focused on hormonal options but the associated side effects have thus far precluded this method from reaching the market. Non-hormonal male contraceptives and vas occlusion have also been explored, but to date no method has progressed past clinical testing. Recent interest in epigenetic research has unveiled a new potential non-hormonal male contraceptive target: the testis-specific bromodomain BRDT. Potent inhibitors for bromodomain-containing proteins are described in the literature, but a BRDT-specific compound has yet to be designed, prepared and tested. The high similarity between bromodomain proteins of the BET family makes development of selective and specific inhibitors both difficult and necessary. Selective inhibition of BRDT by a small molecule is an exciting new target in the search for a new non-hormonal male contraceptive.     

Chemosensory exploration of male scent by female rock lizards result from multiple chemical signals of males

Multiple sexual signals may convey information on males' quality. However, most research focused on visual signals, ignoring chemical signals. In vertebrates, chemical signals are probably often a multicomponent mixture of several active compounds, but they are not well known. We examined the potential additive and interactive effects of 2 compounds (oleic acid and ergosterol) naturally found in femoral gland secretions of male rock lizards on chemosensory exploration behavior of females. Tongue-flick (TF) rates of females to male secretions may result from the combination of responses to multiple compounds. There may be an additive or synergetic effect because male secretions with the highest proportions of both compounds received the highest TF rates, suggesting that their scents were more intriguing. However, there might be an interactive effect too; female TF rates were higher to males' scent with high proportions of ergosterol alone, even if proportions of oleic acid were low, than to high proportions of oleic acid but with low proportions of ergosterol. Further bioassays testing TF behavior of females to standard compounds, presented alone or combined in different concentrations confirmed these findings. Variations in female TF behavior might be explained because different compounds signal different male traits of different importance for females. Our study suggested that femoral secretion of male rock lizards may act as a multicomponent chemical signal.     

Chemical and Biological Aspects of Garcinol and Isogarcinol: Recent Developments

The natural polyisoprenylated benzophenone derivatives garcinol and isogarcinol are secondary plant metabolites isolated from various Garcinia species including Garcinia indica. This review takes stock of the recent chemical and biological research into these interesting natural compounds over the last five years. New biological sources and chemical syntheses are discussed followed by new insights into the activity of garcinol and isogarcinol against cancer, pathogenic bacteria, parasite infections and various inflammatory diseases.     

Delivering non-hormonal contraceptives to men: advances and obstacles

There have been major advances in male contraceptive research during the past two decades. However, for a contraceptive to be used by men, its safety requires more stringent scrutiny than therapeutic compounds for treatment of illnesses because the contraceptives will be used by healthy individuals for an extended period of time, perhaps decades. A wide margin is therefore required between the effective dose range and doses that cause toxicity. It might be preferable that a male contraceptive, in particular a non-hormone-based compound, is delivered specifically and/or directly to the testis and has a rapid metabolic clearance rate, reducing the length of exposure in the liver and kidney. In this article, we highlight the latest developments regarding contraceptive delivery to men and with the aim of providing useful information for investigators in future studies.     

Microbiological coal desulphurization

Sulphur compounds present in coal impose severe limitations on its utilization since sulphur-containing gases emitted into the atmosphere upon direct combustion of coal cause serious environmental pollution problems. Removal of sulphur compounds from coal by microbial action has many advantages over physical and chemical desulphurization methods. The potential use of various microorganisms for the removal of sulphur compounds from coal is presented. Environmental conditions and major process variables affecting the process performance are identified and their possible effects are discussed. Various process schemes for microbial desulphurization (MDS) of coal are suggested. It is concluded that microbial methods have a high potential in removing sulphur compounds from coal. However, more research and development work is needed in this field to overcome present technological problems.     

Improved synthesis of mestranol and ethinyl estradiol (EE) related degradation products as authentic references

Preparative chemical methods for the synthesis of 10 degradation or photodecomposition products of mestranol and ethinyl estradiol (EE) are described. The synthesized compounds are useful as reference materials and standards for pharmaceutical analysis of mestranol and EE as bulk chemical or in formulated product. New synthetic methods were presented and the known synthetic procedures were improved. Detailed structural characterization of the degradation or photodecomposition products of mestranol and EE and related compounds was reported.     

New Caledonia: A ‘ Hot Spot’ for Valuable Chemodiversity

The flora of New Caledonia encompasses more than 3000 plant species and almost 80% are endemic. New Caledonia is considered as a ‘hot spot’ for biodiversity. With the current global loss of biodiversity and the fact that several drugs and pesticides become obsolete, there is an urgent need to increase sampling and research on new natural products. In this context, we review the chemical knowledge available on New Caledonian native flora from economical perspectives. We expect that a better knowledge of the economic potential of plant chemistry will encourage the plantation of native plants for the development of a sustainable economy which will participate in the conservation of biodiversity. In the second part of this review, we focus on the results exposed in 60 scientific articles and describe the identification of 225 original compounds from basal angiosperms and eudicot rosids. We discuss the economic potential of plants and molecules from medicinal and industrial perspectives. This review also highlights several plants and groups, such as Amborella sp., Piperaceae, or Phyllanthaceae, that are unexplored in New Caledonia despite their high chemical interest. Those plants are considered to have priority in future chemical investigations.     

Lonidamine and analogue AF2785 block the cyclic adenosine 3', 5'-monophosphate-activated chloride current and chloride secretion in the rat epididymis

The cystic fibrosis transmembrane conductance regulator (CFTR) or the small conductance cAMP-activated chloride channel encoded by the CFTR gene has been shown to play an important role in the formation of the epididymal fluid microenvironment. Mutation of the gene has led to widespread effects on male reproduction. Like other ion channels, CFTR is amenable to pharmacological intervention. Blocking CFTR in the epididymis could in principle lead to disruption of the epididymal fluid environment. We report for the first time two indazole compounds: lonidamine and 1-(2, 4-dichlorobenzyl)-indazole-3-acrylic acid (AF2785) are potent blockers of CFTR in the epididymis. When added to the external solution under whole-cell patch clamp conditions, AF2785 and lonidamine inhibited the cAMP-activated chloride current in rat epididymal cells with apparent IC(50) values of 170.6 and 631.5 microM, respectively; by comparison the IC(50) value for diphenylamine-2-carboxylate, a well-known chloride channel blocker was 1294 microM. In cultured rat epididymal epithelia mounted in a Ussing chamber, AF2785 and lonidamine inhibited the cAMP-stimulated short-circuit current (a measure of chloride secretion) when added to the apical bathing solution with potency greater than any known chloride channel studied. It is proposed that in view of the important role CFTR plays in male reproduction, further study with these and other new indazole compounds for their CFTR blocking actions can provide a new avenue of research into the development of novel male contraceptives.     

New Caledonia: A ‘Hot Spot’ for Valuable Chemodiversity. Part 1: Gymnosperms

The flora of New Caledonia encompasses more than 3,000 species and almost 80% of them are endemic. New Caledonia is considered as a ‘hot spot’ for biodiversity. With the current global loss of biodiversity, and the fact that several drugs and pesticides are becoming obsolete, there is an urgent need to increase sampling and research on new natural products. In this context, we review the chemical information available on New Caledonian native flora from economical perspectives. We expect that a better knowledge of the economic potential will encourage the plantation of native plants for the development of a sustainable economy which will participate in the conservation of biodiversity. In the first part of this review, we discuss the results reported in 18 scientific articles on the chemicals isolated from 23 endemic conifers of New Caledonia. Several bioactive and original products, such as neocallitropsene or libocedrins, have been isolated from these conifers. This review also highlights several groups, such as Podocarpus spp., that are unexplored in New Caledonia despite the fact that they have been described in other countries to contain a wide range of original bioactive compounds. Those plants are considered as priority for future chemical investigations.     

Use of testosterone alone as hormonal male contraceptive

The world population continues to grow rapidly while resources for sustainable living dwindle and manmade ecological problems increase proportionally to the overpopulation. Family planning is required to reduce population growth in developing countries and to stabilize populations in developed countries. Contraception makes abortion superfluous and provides the key to family planning. Women increasingly demand that men share the burden and risks of contraception and ?? as opinion polls show ?? men would be willing to use contraceptives if they were available. Research has established the principle of hormonal male contraception based on suppression of gonadotropins and spermatogenesis. All hormonal male contraceptives use testosterone, but in East Asian men, testosterone alone can suppress spermatogenesis to a level compatible with contraceptive protection. In Caucasians additional agents are required of which progestins are favoured.     

The hide-and-seek game: men's perspectives on abortion and contraceptive use within marriage in a rural community in Zimbabwe

This paper is based on a study aimed at understanding the perceptions of men to induced abortion and contraceptive use within marriage in rural Zimbabwe. Two qualitative methods were combined. Men were found to view abortion not as a reproductive health problem for women. Instead, they described abortion as a sign of illicit sexual activity and contraceptive use as a strategy married women use to conceal their involvement in extramarital sexual activity. Men felt anxious and vulnerable for lack of control over women. In the absence of verbal communication on sexual matters, women and men resort to what are called here 'hide-and-seek' strategies, where women acquire and use contraceptives secretly while men search for evidence of such use. It is concluded that promoting women's sexual and reproductive health requires both short- and long-term strategies. The short-term strategy would entail providing women with reproductive technology they can use without risking violence. The long-term strategy would entail understanding men's concerns and the way these are manifested. In turn this requires the use of methodologies that encourage dialogue with research participants, in order to capture their deep meanings and experiences.     

THE EFFECT OF GESTATION ON THE RATE OF DECLINE OF MILK SECRETION WITH THE ADVANCE OF THE PERIOD OF LACTATION

1. Data are presented showing that the course of decline of milk secretion with the advance of the period of lactation in farrow cows follows the course of decline of a monomolecular chemical reaction, that is each month''s milk production is a constant percentage of the production of the preceding month (94.77 per cent in the case of the cow under consideration), from which it is inferred that milk secretion is limited by a chemical reaction initiated at parturition, and declining with the decrease of the concentration of the limiting substance as it is transformed into milk. 2. Data are presented showing that the decline in milk secretion due to pregnancy is related to the increase in weight of gestating animals, from which it is inferred that growth of the fetus is in part, at least, responsible for the decline in the milk flow due to the demand of the fetus for nutrients to support its life processes.     

The Scent of Symmetry: A Human Sex Pheromone that Signals Fitness?

A previous study by the authors showed that the body scent of men who have greater body bilateral symmetry is rated as more attractive by normally ovulating (non-pill-using) women during the period of highest fertility based on day within the menstrual cycle. Women in low-fertility phases of the cycle and women using hormone-based contraceptives do not show this pattern. The current study replicated these findings with a larger sample and statistically controlled for men's hygiene and other factors that were not controlled in the first study. The current study also examined women's scent attractiveness to men and found no evidence that men prefer the scent of symmetric women. We propose that the scent of symmetry is an honest signal of phenotypic and genetic quality in the human male, and chemical candidates are discussed. In both sexes, facial attractiveness (as judged from photos) appears to predict body scent attractiveness to the opposite sex. Women's preference for the scent associated with men's facial attractiveness is greatest when their fertility is highest across the menstrual cycle. The results overall suggest that women have an evolved preference for sires with good genes.     

Evidence that androstadienone, a putative human chemosignal, modulates women's attributions of men's attractiveness

Considerable research effort has focused on whether specific compounds found within human body odor influence the behavior or physiology of other individuals. The most intensively studied is 4,16-androstadien-3-one, a chemical which is known to modulate mood and have activational effects in the sympathetic nervous system in a context-dependent manner, but whose action in mate-choice contexts remains largely untested. Here we present evidence that this androgen steroid may modulate women’s judgments of men’s attractiveness in an ecologically valid context. We tested the effects of androstadienone at a speed-dating event in which men and women interacted in a series of brief dyadic encounters. Men were rated more attractive when assessed by women who had been exposed to androstadienone, an effect that was seen in two out of three studies. The results suggest that androstadienone can influence women’s attraction to men, and also that research into the modulatory effects of androstadienone should be made within ecologically valid contexts.     

An integrated database of flavonoids

Flavonoids are polyphenolic compounds that occur ubiquitously in foods of plant origin. Some of these molecules exhibit various physiological activities. Among existing drugs, there are a huge number of compounds bearing a flavonoid-related skeleton. Because of the relevance for pharmaceutical research, it would be beneficial to collect these compounds into a database. Recently, various databases of chemicals were compiled to help biological and/or chemical research, but no comprehensive database of flavonoids with chemical structures and physicochemical parameters, supposedly related to their activity, is available yet. The aim of this research was to merge the information about flavonoids of plant origin and flavonoids used as medicines into a database. Moreover, predictions of activities against various targets were performed using a virtual screening procedure to demonstrate a possible application of the database for pharmaceutical research.     

角蜡蚧和日本龟蜡蚧蜡泌物的超微结构及化学成分分析

采用扫描电镜和气相色谱/质谱联用技术研究了角蜡Ceroplastes ceriferus (Fabricius) 和日本龟蜡蚧C. japonicus Green蜡泌物的超微结构及化学成分。结果表明,这2种蜡蚧分泌蜡质和形成蜡壳的过程基本相似。在1、2龄期分泌的蜡质为“干蜡”,蜡壳为星芒状,虫体周缘的蜡芒均为2大节,与其2个龄期发育相对应,每一个大节又分为若干小节。同时,虫体背面中央蜡质堆积成帽状,也分为均匀的多层。由此说明泌蜡过程具有节律性。虫体周缘与蜡芒对应的突起区上分布着密集的刻点状腺孔,每一个腺孔分泌1根蜡丝,这在以往玻片标本中是观察不到的。雌性第3龄幼虫和成虫期,虫体分泌“湿蜡”,形成龟背状蜡壳,泌蜡腺孔主要为三格腺和四格腺。在肛突区发现了密集的泌蜡腺孔,排列为纵条纹状。从角蜡蚧蜡泌物甲酯化处理样品中检测到14个组分,从直接测试 (未经甲酯化处理) 样品中检测到14个组分;而从日本龟蜡蚧则分别检测到10个组分和25个组分。它们的主要成分是一系列高级的长链饱和与不饱和的烃、脂肪酸、脂肪醇、酯类、醛类以及杂环、多环或大环状化合物。对它们可能的生物生态学功能进行了讨论。     

Male cephalic labial gland secretions of two bumblebee species of the subgenus Cullumanobombus (Hymenoptera: Apidae: Bombus latreille) and their distribution in central Europe

The cephalic labial gland secretion of Bombus semenoviellus males was analyzed, and its chemical composition is reported for the first time. The secretion functions as sex or marking pheromone. Eighty compounds were identified in the secretion, the main one being all-trans-geranylgeranyl acetate (48%). The same compound was shown to form 87% of the labial gland secretion of B. cullumanus males. Both species are closely related and belong to the subgenus Cullumanobombus.