Phytochemistry and Biological Activities of Werneria and Xenophyllum species / Fitoquímica y actividades biológicas de especies de Werneria y Xenophyllum

Plants of the genera Werneria (Asteraceae) and Xenophyllum (genus extracted from Werneria) are used in traditional medicine of Latin America for the treatment of mountain sickness, hypertension and gastrointestinal disorders. Only a small number of species of these genera have been studied, leading to the isolation of compounds belonging to the classes of benzofurans, chromenes, acetophenones, coumarates, diterpenes and pyrrolizidine alkaloids. Some of the plant extracts and/or compounds have shown antimicrobial, anti-HIV, hypotensive and photoprotective activities.

Las plantas de los géneros Werneria (Asteraceae) y Xenophyllum (género extraido de Werneria) son usadas en la medicina tradicional de América Latina para el tratamiento del mal de montaña, hipertensión y desórdenes gastrointestinales. Solo un pequeño número de especies de estos géneros ha sido investigado, lográndose aislar compuestos que pertenecen a las clases de benzofuranos, cromenos, acetofenonas, cumaratos, diterpenos y alcaloides pirrolizidínicos. Algunos de los extractos y/o compuestos de dichas plantas han mostrado actividades antimicrobianas, anti-HIV, hipotensoras y fotoprotectoras.

Study on physicochemical properties of paeonol-Helix aspersa muller nanogel and its inhibitory effects on hypertrophic scar tissue in rabbit ear / 中国中药杂志

To prepare Helix aspersa muller-paeonol nanogel( PAE-HAM-Gels) with anti-proliferative scar effect,evaluate its skin penetration,retention and irritation,and to investigate its prevention and treatment effect for hypertrophic scar in rabbit ears. The dermal retention,transdermal rate and cumulative permeability of paeonol were investigated in vitro by using the modified Franz diffusion cell and the abdominal skin of suckling pigs,SD rats and KM mice,respectively,and the in vitro permeation curves were drawn. The normal skin of the back of New Zealand rabbits was continuously treated with PAE-HAM-Gels for 7 days,and the physiological state of the skin was observed under light microscope after HE staining by using homologous left and right contrast method. The hypertrophic scar model in rabbit ears was established,and the New Zealand rabbits were randomly divided into blank group,model group,positive drug group,PAE-Gels group and PAE-HAM-Gels group. After 28 days of administration,the scar hyperplasia rate and scar elevation index( SEI) of each group were calculated; the scar tissues were taken and stained with Masson for observation of collagen fibers and muscle fibers hyperplasia under light microscope,and the expression level of TGF-β1 in each group was detected. The Qnof PAE-HAM-Gels in aqueous solution was in line with the Higuchi equation,and its transdermal rate,cumulative permeation and dermal retention in different animal skins were all higher than those of PAE-Gels. The skin of the drug-administered group was intact,without erythema,edema or other phenomena; under light microscope,the subcutaneous tissue and the epidermal cells were neatly arranged with uniform thickness,which showed no difference from the blank group. The scar hyperplasia rate of the PAE-HAM-Gels group was 62. 50%; SEI was 2. 17±0. 33 and TGF-β1 was( 815. 4±34. 69) ng·L~(-1),significantly different from those in model group( P<0. 01). Masson staining showed that as compared with the model group,the number of collagen fibers and muscle fibers was small and the arrangement was loose and tidy in the PAE-HAM-Gels group,with regular arrangement of chondrocytes and a small number of inflammatory cells and microvessels.PAE-HAM-Gels have good transdermal properties and dermal retention without skin irritation,offering a promising therapeutic strategy for transdermal delivery during the prevention and treatment of hypertrophic scar in rabbit ears.

Synthesis of some novel phthalazinone, quinazolinone derivatives and screeing antimicrobial activity of selective compounds

4-[1 H-INDOL-3-YL]-1H-2, 3-benzoxazin-1-one [1] aminolysis with some sulfa drugs and 4-amino-acetophenone to give the corresponding sulfonamide and acetyl phenyl derivatives 2a-c and 3, The key intermediate compound 3 condensed with aromatic aldehyde to yield alpha, beta-unsaturated keto compound 4a, b. Compound 1 reacted with sodium azide to give the tetrazol derivative 5. Benzoxazinone derivative 6 was obtained via the interaction of compound 2 with anthranilic acid, which in turn was condensed with hydrazine hydrate, hydroxyl amine hydrochloride/formamide and glutamic acid to yield quinazolinone derivatives 7, 8, 9 and pentandioic acid derivative 10, respectively. Compound 7 reacted with aromatic aldehyde to achieve the Schiff's bases 11a, b, c. Compound [11c] reacted with thioglycolic acid to give thiazole derivative 12. On the other hand, compound 7 reacted with acetic anhdride to give diacetyl derivative 13. Some of the prepared compounds were screened for their antimicrobial activity

Study of photodynamic reactions of p-nitroacetophenone using ESR and optical techniques.

The photosensitizing properties of p-nitroacetophenone (PNAP), a well-known radiosensitizer, have been studied in near UV region. The mechanism of PNAP photosensitization has been investigated by testing the efficiency of singlet oxygen production using photooxidation of 2,2,6,6-tetramethylpiperidine (TEMP) and photodegradation of guanosine. In both the cases, the enhancement effect of deuterated solvents has been observed. Results of these experiments suggest the significant role of type II mechanisms in PNAP photosensitization.