Evaluation of reversible contraceptive potential of Cordia dichotoma leaves extract

Abstract: Objectives Cordia (family Boraginaceae) is a genus of deciduous flowering trees or shrubs comprising more than 300 species distributed widely in the tropical regions. The aim of this review was to provide exhaustive scientific information on traditional uses, phytochemistry and pharmacological activities of the 36 important species with medicinal value from the genus Cordia, to divulge prospects for further research on its therapeutic potential. Key findings Leaves, fruit, bark and seed of a majority of the species were found to possess abundant ethnomedicinal value, but leaves were found to be used most frequently to treat many ailments such as respiratory disorders, stomach pain, wound, inflammation, myalgia, cough, dysentery and diarrhoea. The phytochemical investigation of 36 species resulted in isolation of 293 chemical constituents from various chemical classes. The crude extracts, fractions, essential oils and pure compounds isolated from various Cordia species were reported to have a varied range of pharmacological activities. Summary Many of the traditional uses of the genus Cordia were supported by the results obtained from pharmacological studies performed using various extracts or pure compounds. More attention should be given to the biological evaluation using pure phytochemicals and to identify the mechanism of actions and exploring this genus for new drug discovery.

Abstract: Species of the genus Cordia, Boraginaceae, are widely studied with regard to the various ethnobotanical and ethnopharmacological aspects. They are found principally in tropical and subtropical regions of the American, Asian and African continents, where they occur in various countries. In the genus Cordia, there are many species cultivated for ornamental plants, wood and medicinal applications, where they are extensively utilized by traditional communities. In the last decades, scientific studies of Cordia species have intensified, demonstrating the great interest in phytochemical, biological and pharmacological studies. In this review, we describe the principal botanical aspects, ethnopharmacological information and evaluation of the bioactive and pharmacological properties of Cordia, its phytochemical constituents and the most common classes of secondary metabolites identified. The information reported in this work contributes scientifically to recognizing the importance of the genus Cordia as a target in the search for new biotechnological investments.

Abstract: Species of the genus Cordia, Boraginaceae, are widely studied with regard to the various ethnobotanicaland ethnopharmacological aspects. They are found principally in tropical and subtropical regions of theAmerican,AsianandAfricancontinents,wheretheyoccurinvariouscountries.InthegenusCordia,thereare many species cultivated for ornamental plants, wood and medicinal applications, where they areextensively utilized by traditional communities. In the last decades, scientific studies of Cordia specieshaveintensified,demonstratingthegreatinterestinphytochemical,biologicalandpharmacologicalstud-ies. In this review, we describe the principal botanical aspects, ethnopharmacological information andevaluation ofthebioactiveandpharmacologicalpropertiesofCordia,itsphytochemicalconstituentsandthe most common classes of secondary metabolites identified. The information reported in this workcontributes scientifically to recognizing the importance of the genus Cordia as a target in the search fornew biotechnological investments.© 2015 Sociedade Brasileira de Farmacognosia. Published by Elsevier Editora Ltda. All rights reserved.

Abstract: Broussonetia papyrifera leaves (BPL) as a traditional Chinese medicine are also used in livestock feed for stimulating reproduction, adipose tissue and muscle development; however, the mechanism of their action is still unknown. Through estrogen biosynthesis-guided fractionation in human ovarian granulosa-like KGN cells, five new phenolic glycosides, broussoside A–E(1–5), along with fifteen known dietary phenolic compounds, were isolated from the n-butanol extract of BPL, and their structures were elucidated on the basis of NMR spectra analysis and chemical evidence. New compounds 3, 4, 5 and the known compounds 9 and 10 were found to potently inhibit estrogen biosynthesis in KGN cells. In addition, compounds 9, 17, 18, and 20 showed strong antioxidant activity against ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt) and DPPH (1, 1′-diphenyl -2-picryl-hydrazyl radical) assays. These findings suggest that BPL may improve meat quality through the regulation of estrogen biosynthesis. Furthermore, they may be useful for the discovery of potential aromatase modulators from natural products. Finally, they could be considered as a new source for natural antioxidants.

Abstract: Leishmaniasis is an epidemic in various countries, and the parasite Leishmania donovani is developing resistance against available drugs. In the present study the antileishmanial action of piperolactam A (PL), isolated after bioactivity guided fractionation from root extracts of Piper betle was accentuated in detail. Activity potentiation was achieved via cyclodextrin complexation. Crude hydro-ethanolic extract (PB) and three fractions obtained from PB and fabricated PL-hydroxypropyl-β-cyclodextrin (HPBCD) nanoparticles were evaluated for antileishmanial activity. Tests were performed against L . donovani wild-type, sodium stibogluconate, paromomycin and field isolated (GE1) resistant strains in axenic amastigote and amastigote in macrophage models. PL-HPBCD complex was characterized and FITC loaded HPBCD nanoparticles were assessed for macrophage internalization in confocal microscopic studies. Isolated and purified PL from most potent, alkaloid rich ethyl acetate fraction of PB showed high level of antileishmanial activities in wild-type (IC 50 = 36 μM), sodium stibogluconate resistant (IC 50 = 103 μM), paromomycin resistant (IC 50 = 91 μM) and field isolated resistant (IC 50 = 72 μM) strains together with cytotoxicity (CC 50 = 900 μM) in mouse peritoneal macrophage cells. Inclusion of PL in HPBCD nanoparticles resulted in 10-fold and 4–10-fold increase in selectivity indexes (CC 50 /IC 50 ) for wild-type and drug resistant strains, respectively. Drug-carrier interactions were clearly visualized in FT-IR studies. Complete incorporation of PL in HPBCD cavity was ascertained in DSC and XRD analyses. 180 nm size stable nanospheres showed macrophage internalization within 1 h of incubation. Piperolactam A (PL), a representative of the inchoate skeleton of aristolactam chassis might be the source of safe and affordable antileishmanial agents for the cure of deadly Leishmania infections.

Abstract: 1 Methods of Plant Analysis.- 1.1 Introduction.- 1.2 Methods of extraction and isolation.- 1.3 Methods of separation.- 1.4 Methods of identification.- 1.5 Analysis of results.- 1.6 Applications.- 2 Phenolic Compounds.- 2.1 Introduction.- 2.2 Phenols and phenolic acids.- 2.3 Phenylpropanoids.- 2.4 Flavonoid pigments.- 2.5 Anthocyanins.- 2.6 Flavonols and flavones.- 2.7 Minor flavonoids, xanthones and stilbenes.- 2.8 Tannins.- 2.9 Quinone pigments.- 3 The Terpenoids.- 3.1 Introduction.- 3.2 Essential oils.- 3.3 Diterpenoids and gibberellins.- 3.4 Triterpenoids and steroids.- 3.5 Carotenoids.- 4 Organic Acids, Lipids and Related Compounds.- 4.1 Plant acids.- 4.2 Fatty acids and lipids.- 4.3 Alkanes and related hydrocarbons.- 4.4 Polyacetylenes.- 4.5 Sulphur compounds.- 5 Nitrogen Compounds.- 5.1 Introduction.- 5.2 Amino acids.- 5.3 Amines.- 5.4 Alkaloids.- 5.5 Cyanogenic glycosides.- 5.6 Indoles.- 5.7 Purines, pyrimidines and cytokinins.- 5.8 Chlorophylls.- 6 Sugars and their Derivatives.- 6.1 Introduction.- 6.2 Monosaccharides.- 6.3 Oligosaccharides.- 6.4 Sugar alcohols and cyclitols.- 7 Macromolecules.- 7.1 Introduction.- 7.2 Nucleic acids.- 7.3 Proteins.- 7.4 Polysaccharides.

Abstract: Cyclodextrins are cyclic oligosaccharides which have recently been recognized as useful pharmaceutical excipients. The molecular structure of these glucose derivatives, which approximates a truncated cone or torus, generates a hydrophilic exterior surface and a nonpolar cavity interior. As such, cyclodextrins can interact with appropriately sized molecules to result in the formation of inclusion complexes. These noncovalent complexes offer a variety of physicochemical advantages over the unmanipulated drugs including the possibility for increased water solubility and solution stability. Further, chemical modification to the parent cyclodextrin can result in an increase in the extent of drug complexation and interaction. In this short review, the effects of substitution on various cyclodextrin properties and the forces involved in the drug-cyclodextrin complex formation are discussed. Some general observations are made predicting drug solubilization by cyclodextrins. In addition, methods which are useful in the optimization of complexation efficacy are reviewed. Finally, the stabilizing/destabilizing effects of cyclodextrins on chemically labile drugs are evaluated.

Abstract: Acclaimed by students and instructors alike, "Foye's Principles of Medicinal Chemistry "is now in its Seventh Edition, featuring updated chapters plus new material that meets the needs of today's medicinal chemistry courses. This latest edition offers an unparalleled presentation of drug discovery and pharmacodynamic agents, integrating principles of medicinal chemistry with pharmacology, pharmacokinetics, and clinical pharmacy. All the chapters have been written by an international team of respected researchers and academicians. Careful editing ensures thoroughness, a consistent style and format, and easy navigation throughout the text.

Abstract: The short length of the estrous cycle of rats makes them ideal for investigation of changes occurring during the reproductive cycle. The estrous cycle lasts four days and is characterized as: proestrus, estrus, metestrus and diestrus, which may be determined according to the cell types observed in the vaginal smear. Since the collection of vaginal secretion and the use of stained material generally takes some time, the aim of the present work was to provide researchers with some helpful considerations about the determination of the rat estrous cycle phases in a fast and practical way. Vaginal secretion of thirty female rats was collected every morning during a month and unstained native material was observed using the microscope without the aid of the condenser lens. Using the 10 x objective lens, it was easier to analyze the proportion among the three cellular types, which are present in the vaginal smear. Using the 40 x objective lens, it is easier to recognize each one of these cellular types. The collection of vaginal lavage from the animals, the observation of the material, in the microscope, and the determination of the estrous cycle phase of all the thirty female rats took 15-20 minutes.

Abstract: The purpose of this review is to discuss and summarize some of the interesting findings and applications of cyclodextrins (CDs) and their derivatives in different areas of drug delivery, particularly in protein and peptide drug delivery and gene delivery. The article highlights important CD applications in the design of various novel delivery systems like liposomes, microspheres, microcapsules, and nanoparticles. In addition to their well-known effects on drug solubility and dissolution, bioavailability, safety, and stability, their use as excipients in drug formulation are also discussed in this article. The article also focuses on various factors influencing inclusion complex formation because an understanding of the same is necessary for proper handling of these versatile materials. Some important considerations in selecting CDs in drug formulation such as their commercial availability, regulatory status, and patent status are also summarized. CDs, because of their continuing ability to find several novel applications in drug delivery, are expected to solve many problems associated with the delivery of different novel drugs through different delivery routes.