Phytochemical and in vitro screening of some Ficus and Morus spp. for hypolipidaemic and antioxidant activities and in vivo assessment of Ficus mysorensis (Roth)

Phytochemical screening of air-dried leaves and fruit juice of certain Ficus and Morus spp. have been studied. In an in?vitro study, the ethanol and hexane extracts of the investigated plants were evaluated against hyperlipidaemia by estimating the rate limiting enzyme of cholesterol biothenysis; β-hydroxy-β-methylglutaryl coenzyme A reductase (HMG-CoA reductase). The antioxidant activity was evaluated by reduction of DPPH(-) free radical. Extra phytochemical screening of Ficus extracts was undertaken, which recorded potent hypolipidaemic and antioxidant activities. The more pronounced extract, Ficus mysorensis (hexane extract), was evaluated in?vivo by estimation of the lipid profile and certain antioxidant parameters in hypercholesterolemic rats. The hexane fraction was chromatographed and six isolated compounds were identified. Furthermore, its saponifiable fraction was identified by a MS/MS technique. In conclusion, F. mysorensis recorded hypolipidaemic and antioxidant effects. Detailed studies of the isolated compounds must be undertaken for an evaluation against hypercholesterolemia and free radical elevation.     

A New Flavanone from the Bark of Morus macoura Miq.

“Sang Bai Pi”, the bark of mulberry, has been used as herbal medicine to treat diabetes, arthritis, rheumatism for thousands of years. Phytochemical studies on some Morus species revealed that they contained phenolic compounds1. Macrourone C (1) was isolated from Morus macroura Miq. In this paper, the structure of 1 was elucidated on the basis of spectoscopic evidence.Figure 1 Structure and Key HMBC for 1 1Macrourone C (1), a yellow powder, exhibited dark blue fluorescence under UV li…     

In vitro cytotoxic and antiviral activities of Ficus carica latex extracts

The latex of fig fruit (Ficus carica) is used in traditional medicine for the treatment of skin infections such as warts and also diseases of possible viral origin. Five extracts (methanolic, hexanic, ethyl acetate, hexane-ethyl acetate (v/v) and chloroformic) of this species were investigated in?vitro for their antiviral potential activity against herpes simplex type 1 (HSV-1), echovirus type 11 (ECV-11) and adenovirus (ADV). To evaluate the capacity of the extracts to inhibit the replication of viruses, the following assays were performed: adsorption and penetration, intracellular inhibition and virucidal activity. Observation of cytopathic effects was used to determine the antiviral action. The hexanic and hexane-ethyl acetate (v/v) extracts inhibited multiplication of viruses by tested techniques at concentrations of 78 μg mL(-1). These two extracts were possible candidates as herbal medicines for herpes virus, echovirus and adenovirus infectious diseases. All extracts had no cytotoxic effect on Vero cells at all tested concentrations.     

Experimental and computational approaches to reveal the potential of Ficus deltoidea leaves extract as α-amylase inhibitor

Ficus deltoidea leaves extract are known to have good therapeutic properties such as antioxidant, anti-inflammatory and anti-diabetic. We showed that 50% ethanol-water extract of F. deltoidea leaves and its pungent compounds vitexin and isovitexin exhibited significant (p < 0.05) α-amylase inhibition with IC₅₀ (vitexin: 4.6 μM [0.02 μg/mL]; isovitexin: 0.06 μg/mL [13.8 μM] and DPPH scavenging with IC₅₀ (vitexin: 92.5 μM [0.4 μg/mL]; isovitexin: 0.5 μg/mL [115.4 μM]). Additionally, molecular docking analysis confirmed that vitexin has a higher binding affinity (-7.54 kcal/mol) towards α-amylase compared to isovitexin (?5.61 kcal/mol). On the other hand, the molecular dynamics findings showed that vitexin-α-amylase complex is more stable during the simulation of 20 ns when compared to the isovitexin-α-amylase complex. Our results suggest that vitexin is more potent and stable against α-amylase enzyme, thus it could develop as a therapeutic drug for the treatment of diabetes.     

Biodegradable and biocompatible inorganic–organic hybrid materials. I. Synthesis and characterization

The hydroxyl or vinyl end-groups of linear or three-arm star-shaped poly(ε-caprolactone) (PCL) chains have been derivatized into triethoxysilane groups reactive in the sol-gel process. New transparent hybrid materials that combine tetraethylorthosilicate (TEOS) and PCL known for biodegradability and biocompatibility have accordingly been prepared. The sol-gel process is, however, limited by the early vitrification of the reactive system. However, thermal posttreatment can overcome these diffusional and/or kinetic limitations as assessed by a set of analytical methods. The thermal stability of PCL is improved by incorporation into the silica network. Conversely, the thermal stability of the ceramer depends on the effective PCL content. The extent of PCL incorporation into the silica network depends on PCL molecular weight, number, and reactivity of the PCL functional groups. IR spectroscopy has shown that hydrogen bonding occurs between the ester groups of PCL and residual OH groups of the silicate component. © 1997 John Wiley & Sons, Inc. J Polym Sci A: Polym Chem 35 : 2295–2309, 1997     

Pyrilocyanines. 36.α-thienyl substituted pyrilo- and thiopyrilocyanines

Symmetrical and nonsymmetrical 2,6- (and 4,6-)-di--thienyl substituted - and -pyrilo- and thiopyrilocyanines have been synthesized. The effect of changing the phenyl groups for -thienyl on the electronic absorption spectral parameters of the dyes obtained is discussed. It was found that such a change leads to a decrease in the effective length and increase in the electron donor ability of the hetero fragments containing these groups. The more intense coloring of the thienyl substituted dyes is due to interaction of the polymethine and quasilocal electronic transitions.For Communication 35 see [1].Institute of Organic Chemistry, National Academy of Sciences of Ukraine Kiev 253660. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 494–500, April, 1998.     

Binary and Ternary Complexes Between Lauryl Hexaoxyethylene, Benzoate and Cyclodextrin. Part I. α-CD

The characterization of binary and ternary complexes of benzoate, lauryl hexaoxyethylene (C₁₂E₆) and -CD is presented. Complexation was characterized by capillary zone electrophoresis and titration microcalorimetry. These techniques suggested that -CD formed two qualitatively different complexes with C₁₂E₆. The stoichiometric ratio of -CD : C₁₂E₆ in the individual complexes was 1 : 1 and 1.4 : 1, with stability constants of2.0 × 10³ M^-1 and 6.4 × 10⁵ M^-1.4, respectively. At higher concentrations of interacting species (10 mM), a precipitate formed. Addition of benzoate seemed to prevent precipitate formation and appeared to increase the stability constants of both binary complexes. Both techniques also indicated formation of ternary complexes between -CD, C₁₂E₆ and benzoate.     

Binary and Ternary Complexes Between Lauryl Hexaoxyethylene, Benzoate and Cyclodextrin. Part II. β-CD

The characterization of binary and ternary complexes of benzoate, lauryl hexaoxyethylene (C₁₂E₆) and -CD is presented. The complexation equilibrium was characterized by UV-Vis spectrophotometry, titration microcalorimetry, capillary electrophoresis, and 2D ROESY ¹H-NMR. Results suggested that -CD forms one complex with C₁₂E₆in the stoichiometric ratio of -CD : C₁₂E₆1.5 : 1, with a stability constant 1.3 × 10⁵ M^-1.5. The 2-D ROESY ¹H-NMR spectrum indicated that C₁₂E₆is included inside the -CD cavity. The primary binding site of C₁₂E₆ is on the lauryl subunit of this molecule. Analogous to a previously reported study of -CD, the combination of -CD and C₁₂E₆precipitated from the solution. Addition of benzoate seemed to dissolve the precipitate and nearly doubled the apparent stability constant of the complex. Results from the various techniques supported formation of ternary complexes between -CD, C₁₂E₆, and benzoate.     

Fluorine containing amino acids and their derivatives. 7. Synthesis and antitumor activity of α- and γ-substituted methotrexate analogs

Three types of reactions of α-substituted malonates, difluoromethylation, alkylation with n,n,n-trifluoroalkyl sulfonates, and Michael addition to 2-substituted-acrylates, conveniently afforded a number of fluorine containing α amino acids such as β-fluorinated-alanines, 2-amino-n,n,n-trifluoroalkanoic acids, and fluorinated glutamic acids as well as other γ-heteroatom substituted glutamic acids. Here, an efficient enzymatic optical resolution using hog kidney acylase was conducted to obtain both optical isomers of 2-amino-n,n,n-trifluoroalkanoic acids. In addition, a novel sulfoxide rearrangement was observed in a base-catalyzed reaction of diethyl α-difluoromethyl-α-sulfoxymalonates. Finally, α- and γ-substituted glutamic acids obtained were used for chemical modification of the antitumor agent methotrexate to reveal remarkable structure-activity relationships. In particular, the significant effects of fluorine substitution on the in vivo antitumor activity were observed.