(E)-3-(4-Cyclo­hexyl-3-fluoro­benzyl­idene)chroman-4-one

The title compound, C22H21FO2, exhibits substitutional disorder of the F atom and a H atom in the asymmetric unit with different occupancies, the refined F:H ratio being 0.80 (2):0.20 (2). The dihedral angle between the fluorinated benzene ring and the benzene ring of the chromanone system is 37.30°. There are two relatively high residual electron-density peaks associated with the disorder

Acalypha wilkesiana ‘Java white’: Identification of some bioactive compounds by GC-MS and their effects on key enzymes linked to type 2 diabetes

In this study, we identified bioactive compounds from the ethanolic extracts of the leaves, stem bark and root bark of Acalypha wilkesiana through GC-MS analysis and investigated the effects of these extracts on some of the enzymes linked to type 2 diabetes. Plant parts were extracted sequentially with ethyl acetate, ethanol and water. GC-MS analysis revealed the presence of long-chain alkyl acids, esters, ketones and alcohols including phytol and phytol acetate along with some secondary metabolites such as xanthone, vitamin E and various types of sterols including stigmasterol, campesterol and sitosterol. Ethanolic extracts of all the parts showed a dose-dependent inhibition of α-glucosidase and α-amylase activity. The extracts also demonstrated anti-lipase activity. The ethanolic extract of root bark showed the highest inhibition of enzymes compared to other extracts. The EC50 values (concentrations for 50 % inhibition) of α-glucosidase, α-amylase and lipase inhibition were 35.75 ± 1.95, 6.25 ± 1.05 and 101.33 ± 5.21 µg mL–1, resp. The study suggests that A. wilkesiana ethanolic extracts have the ability to inhibit the activity of enzymes linked to type 2 diabetes. Further studies are needed to confirm the responsible bioactive compounds in this regard

IN VITRO CHEMO-PREVENTATIVE ACTIVITY OF STRELITZIA NICOLAI ARIL EXTRACT CONTAINING BILIRUBIN

Background: The discovery of the only animal pigment, bilirubin, in the plant Strelitzia nicolai has triggered a vast number of questions regarding bilirubin’s formation and its role in the human body. Recent studies have confirmed that bilirubin at certain levels have many medical benefits. Various case studies have revealed that bilirubin is a potent antioxidant. Cervical cancer is one of South Africa’s largest womens’ health crises. It is estimated that it affects one out of 41 South African women and kills approximately 8 women in the country every day. Thus, the aim of this study was to investigate if the aril extract of Strelitzia nicolai (Regel and Körn.) containing bilirubin possesses anti-cancer activity and to determine its effect on the induction of apoptosis. Materials and methods: The DPPH activity was firstly used to determine the antioxidant effect of the extract. Thereafter, the cytotoxic effect was tested using the XTT assay. Apoptosis was confirmed and quantified using the Annexin V-PE kit and the morphology was studied using acridine orange and ethidium bromide. Results: The aril extract decreased cell viability by 52% and induced apoptosis in HeLa cells; as shown by the Annexin V-PE Apoptosis detection kit and morphological studies with acridine orange/ethidium bromide staining. Conclusion: The activity of the extract as a potent antioxidant was immensely enhanced as compared to the bilirubin standard. These results suggest that S. nicolai aril extract containing bilirubin works synergistically as opposed to bilirubin on its own. Furthermore, this extract might be a good candidate for the therapeutic intervention of cervical cancer

3-(3-Meth­oxy­benzyl­idene)chroman-4-one

In the title compound, C17H14O3, the dihedral angle between the meth­oxy­benzene unit and the benzene ring of the chromanone system is 64.12 (3)°. The crystal structure is stabilized by weak C—H⋯O inter­actions

Perfluorophenyl Derivatives as Unsymmetrical Linkers for Solid Phase Conjugation

Linkers play major roles in conjugation chemistry toward the advancement of drug discovery. Two different series of fluorinated linkers were introduced to the backbone of a model peptide using solid phase peptide synthesis. These fluorinated linkers have the potential to conjugate two asymmetrical groups. This has not been done using other fluorinated linkers. This study deals with application of linkers with S, N, and O terminals and reports on the investigation of their chemoselectivity and activity for branching peptide backbones using a chosen model peptide. These fluorinated linkers have unique properties that will make it possible for a large diversity of bioconjugated chemicals for different bioapplications to be designed and synthesized

The chemistry and biological activity of the Hyacinthaceae

Covering: 1914 to 2012The Hyacinthaceae (sensu APGII), with approximately 900 species in about 70 genera, can be divided into three main subfamilies, the Hyacinthoideae, the Urgineoideae and the Ornithogaloideae, with a small fourth subfamily the Oziroëoideae, restricted to South America. The plants included in this family have long been used in traditional medicine for a wide range of medicinal applications. This, together with some significant toxicity to livestock has led to the chemical composition of many of the species being investigated. The compounds found are, for the most part, subfamily-restricted, with homoisoflavanones and spirocyclic nortriterpenoids characterising the Hyacinthoideae, bufadienolides characterising the Urgineoideae, and cardenolides and steroidal glycosides characterising the Ornithogaloideae. The phytochemical profiles of 38 genera of the Hyacinthaceae will be discussed as well as any biological activity associated with both crude extracts and compounds isolated. The Hyacinthaceae of southern Africa were last reviewed in 2000 (T. S. Pohl, N. R. Crouch and D. A. Mulholland, Curr. Org. Chem., 2000, 4, 1287-1324; ); the current contribution considers the family at a global level

Synthesis and Antifungal Studies of (2E)-N-Benzyl-N -phenylbut-2-enediamide and (2E)-N,N -Dibenzylbut-2-enediamide Analogues

A series of eleven butanediamine analogues, of which nine were new, were synthesized by the nucleophilic substitution of aromatic amines and benzylamines with maleic anhydride and tested on four yeast strains of Candida species using the broth microdilution method. Compounds 3a and 3c with an unsubstituted phenyl ring and a 3-methoxyphenyl ring, respectively, are the most active against the fungal species with MIC values ranging from 20.2 to 80.6 M for C. albicans and C. parapsilosis and 178.5 and 161.2 M for C. krusei, respectively