Cichorins D-F: Three New Compounds from Cichorium intybus and Their Biological Effects.

Cichorium intybus L., (chicory) is employed in various traditional medicines to treat a wide range of diseases and disorders. In the current investigation, two new naphthalane derivatives viz., cichorins D (1) and E (2), along with one new anthraquinone cichorin F (3), were isolated from Cichorium intybus. In addition, three previously reported compounds viz., ß-sitosterol (4), ß-sitosterol ß-glucopyranoside (5), and stigmasterol (6) were also isolated from Cichorium intybus. Their structures were established via extensive spectroscopic data, including 1D (1H and 13C) and 2D NMR (COSY, HSQC and HMBC), and ESIMS. Cichorin E (2) has a weak cytotoxic effect on breast cancer cells (MDA-MB-468: IC50: 85.9 µM) and Ewing's sarcoma cells (SK-N-MC: IC50: 71.1 µM); cichorin F (3) also illustrated weak cytotoxic effects on breast cancer cells (MDA-MB-468: IC50: 41.0 µM and MDA-MB-231: IC50: 45.6 µM), and SK-N-MC cells (IC50: 71.9 µM). Moreover compounds 1-3 did not show any promising anthelmintic effects.

Antioxidant study of flavonoid derivatives from the aerial parts of Rhus natalensis growing in Saudi Arabia.

Phytochemical study of the CH(2)Cl(2) soluble fraction of the aerial parts of R. natalensis resulted in the isolation and identification of six flavonoid derivatives, ß-amyrin and ß-sitosterol glucoside (daucosterol). The isolated compounds were identified utilizing physical, chemical and different spectral methods including UV, 1D- 2D-NMR and MS. The compounds were identified as four flavanones; 7-O-methyl hesperetin (1), 7-O-methyl naringenin (4), (-)-homoeriodictyol (eriodictyonone) (5), eriodictyol-7-methyl ether (6) and two flavones; 7-O-methyl isokaemferide (2) and genkwanin (3). The isolated compounds as well as some available standards representing structurally similar flavones and flavanones were used to study their antioxidant potential using DPPH and try to explore the impact of structures on the antioxidant activity. In other assays flavanones were less active than flavones as antioxidant due to lack of the C-4 carbonyl group in conjugation with 2,3-double bond. However, in DPPH assay based on the ability of molecules to donate hydrogen flavanones were found more active than flavones.

Quantitative analysis of biomarker rutin in different species of genus Ficus by validated NP and RP-HPTLC methods.

Biomarker rutin was analyzed in methanol extracts of leaves of five different species of genus Ficus (Ficus carica, Ficus nitida, Ficus ingens, Ficus palmata and Ficus vasta) by NP-HPTLC (Method I) and RP- HPTLC methods (Method II). The development and validation for method I was carried out with silica gel 60F254 plates using EA: GAA: FA: H2O (10:1:1:2.5, v/v/v/v) as developing system. Method II was carried out on silica gel 60F254 RP-18 plates using mobile phase ACN: H2O (4:6 v/v). Both analyses were scanned at 305 nm and were found to give well resolved peak of rutin at Rf0.28±0.01 and 0.68±0.03 for Method I and Method II, respectively. The percentage of rutin was found to be 0.51% & 0.66% in F. ingens, 0.24% & 0.54% in F. palmata and 0.14% & 0.17% in F. vasta by Method I & Method II, respectively. Method II (RP-HPTLC) was found to be more accurate, precise and sensitive than Method I. Method II can be used as an important tool for standardization and quality control of bulk drugs and in-process formulations of rutin.

Densitometric validation and analysis of biomarker ß-amyrin in different Acacia species (leaves) grown in Kingdom of Saudi Arabia by high performance thin-layer chromatography.

Biomarker ß-amyrin was analyzed in the leaves of four different Acacia species (A. salicina, A. loreta, A. hamulosa and A. tortilis) grown in Kingdom of Saudi Arabia by a validated HPTLC method. The chromatography was performed on glass-backed silica gel 60 F254 HPTLC plates using solvents toluene: methanol (9:1, v/v) as mobile phase. The developed TLC plate was derivatized with anisaldehyde and scanned at 520 nm. A sharp peak of ß-amyrin was found at Rf=0.58±0.01. The r2 and the linear regression equation for ß-amyrin was found to be 0.991 and 19.913X+107.803, respectively in the concentration range of 100-800 ng. The percentage of ß-amyrin was found to be maximum 2.70% w/w in A. tortilis, 1.85% w/w in A. loreta and 1.80% w/w in A. hamulosa while it was totally absent in A. salicina. This study conceives maiden reporting of quantification of ß-amyrin in four different species of Acacia by validated HPTLC method. The developed method for the analysis of ß-amyrin was proved to be reproducible by statistical analysis hence it can be employed for further analysis of ß-amyrin in plasma, other biological fluids and in finished products available in the market.

A novel ß-lactam derivative, albactam from the flowers of Albizia lebbeck with platelets anti-aggregatory activity in vitro.

A novel ß-lactam derivative, albactam, was isolated from the alcoholic extract of the flowers of Albizia lebbeck. It showed a significant anti-aggregatory activity against adenosine diphosphate and arachidonic acid induced guinea-pigs' platelets aggregation in vitro. Six more known compounds were also isolated and fully characterized by measuring 1D and 2D NMR, two of them are the triterpenes ß-amyrin and 11α, 12α-oxidotaraxerol, two ceramide derivatives and two flavonoids, kampferol 3-O-rutinoside and rutin.

Quantification of glycyrrhizin in anti-stress herbal formulations by validate HPTLC method: a rational paradigm towards quality control of herbals.

In the present study an analytical method of high-performance thin-layer chromatography (HPTLC) has been developed for quantification of glycyrrhizin for marketed antistressliquorice root capsules (LRC) and herbal tea (HT). Chromatography was performed by using mobile phase ethyl acetate (EA): glacial acetic acid (GAA): Methanol (MeOH): water (H(2)O) in proportion of 6:2:2:1, v/v/v/v. The developed plate was scanned and quantified densitometrically at absorption maxima 254nm. The method was validated for various analytical parameters viz. precision, accuracy, recovery, robustness, specificity, detection and quantification limits. The developed system was found to give compact spot for glycyrrhizin (R(f)= 0.33± 0.001). The linearity relationship was described by the equation Y=6.841X+ 70.428. The limit of detection (34 ng band(-1)), limit of quantification (101 ng band(-1)), recovery (99.4-99.8%), and precision (<1.84% and <1.62%; intraday and interday, respectively) were found satisfactory for glycyrrhizin. Linearity range for glycyrrhizin was 100-600ng (r(2)=0.998). The amount of glycyrrhizin was estimated by comparing the peak area of standard and the same was present in crude extract. The content of glycyrrhizin was estimated as 11.4% and 4.7% w/w in sample LRC and HT, respectively. The proposed method will be useful to quantify the therapeutic dose of glycyrrhizin in herbal formulations as well as in bulk drug.

Phytochemical and pharmacological study of Ficus palmata growing in Saudi Arabia.

Phytochemical study of the aerial parts of Ficus palmata utilizing liquid-liquid fractionation and different chromatographic techniques resulted in the isolation of a new isomer of psoralenoside namely, trans-psoralenoside (5) in addition to, one triterpene: germanicol acetate (1), two furanocoumarins: psoralene (2), bergapten (3), one aromatic acid vanillic acid (4) and the flavone glycoside rutin (6). Structures of the isolated compounds were established through physical, 1D- and 2D-NMR and MS data. The total extract and fractions of the plant were examined in vivo for its possible effects as hepatoprotective, nephroprotective, antiulcer and anticoagulant activities in comparison with standard drugs. Hepatoprotective activity was assessed via serum biochemical parameters including aspartate aminotransferase (AST), alanine aminotransferase (ALT), gamma glutamyl transpeptidase (GGT), alkaline phosphatase (ALP) and total bilirubin. Tissue parameters such as non-protein sulfhydryl groups (NP-SH), malonaldehyde (MDA) and total protein (TP) were also measured. In addition to tissue parameters, nephroprotective effect was evaluated by measuring the serum levels of sodium, potassium, creatinine and urea. Histopathological study for both liver and kidney cells was also conducted. Antiulcer activity was explored by observing stomach lesions after treatment with ethanol. Whole blood clotting time (CT) was taken as a measure for the anticoagulant activity of the extract. Antioxidant activity of the total extract and fractions of the plant was measured using 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and ascorbic acid as standard.