Proteomics analysis reveals a potential new target protein for the lipid-lowering effect of Berberine8998.

Berberine8998 is a newly synthesized berberine derivative with better lipid-lowering activity and improved absorption. The objective of this study was to investigate the effects of berberine8998 on serum cholesterol and lipid levels in vivo and to examine the mechanisms involved. Hamsters on high-fat diet (HFD) were administered berberine or berberine8998 (50 mg·kg-1·d-1, ig) for 3 weeks. Berberine8998 administration significantly lowered the total cholesterol, triglycerides and LDL-C levels in HFD hamsters. Bioinformatics revealed that berberine and berberine8998 shared similar metabolic pathways and fatty acid metabolism was the predominant pathway. Western blot validation results showed that peroxisomal acyl-coenzyme A oxidase 1 (ACOX1) and long-chain fatty acid-CoA ligase 1 (ACSL1), two proteins involved in fatty acid metabolism, were expressed differently in the berberine8998 group than in the untreated group and the berberine treatment group. Biochemistry results showed that berberine8998 significantly lowered the non-esterified fatty acid (NEFA) levels, which may lead to a reduction in TG levels in the berberine8998 treatment group and the differences observed in proteomics analyses. Pharmacokinetic analysis conducted in rats. After administration of berberine or berberine8998 (50 mg/kg, ig), berberine8998 exhibited a remarkably improved absorption with increasing bioavailability by 6.7 times compared with berberine. These findings suggest that berberine8998 lowers cholesterol and lipid levels via different mechanisms than berberine, and its improved absorption makes it a promising therapeutic candidate for the treatment of hypercholesterolemia and obesity.

Stable molluscicide formulation of an aqueous extract of Euphorbia myrsinites.

Aqueous extracts of Euphorbia myrsinites L. (Euphorbiaceae) were tested for molluscicidal activity against Biomphalaria glabrata; LC50 values of 15.1 and 8.9 ppm were obtained for the stem and leaf extracts, respectively, which are within the WHO limit for an effective molluscicide. However, the extracts were found to be unstable at room temperature and the level of activity fell rapidly (about 50% after 7 days at 20 °C). Moreover, the extracts were shown to be cytotoxic and would thus, if used as a molluscicide, be potentially hazardous to the user. As a result, attempts were made to produce a simple formulation that was stable and easy to handle, thereby reducing the danger to the user, but which would decompose rapidly in aqueous solution after application, thus reducing any lasting ecological damage. A product based on spray drying the aqueous extract of the leaves and stems led to a preparation that, although slightly lower in activity than the original extract, was stable at room temperature for at least a year, but which decomposed in aqueous solution at a similar rate to the original extract.

6-Methylcryptoacetalide, 6-methyl-epicryptoacetalide and 6-methylcryptotanshinone from Salvia aegyptiaca.

From the whole plant of Salvia aegyptiaca, 6-methylcryptoacetalide, 6-methyl-epicryptoacetalide and 6-methylcryptotanshinone have been isolated and characterized, mainly by spectroscopic means. In addition to these novel diterpenoids, the known compounds 3beta-hydroxy-olean-12-en-28-oic acid, 3beta-hydroxy-oleana-11,13(18)-dien-28-oic acid, sitosterol-3beta-glucoside, sitosterol, stigmasterol, 5-hydroxy-7,3',4'-trimethoxyflavone and 5, 6-dihydroxy-7,3',4'-trimethoxyflavone were isolated.

Cissampeloflavone, a chalcone-flavone dimer from Cissampelos pareira.

From the aerial parts of Cissampelos pareira L. (Menispermaceae), a chalcone-flavone dimer has been isolated which, mainly from NMR spectroscopic and MS data, was proved to be 2-(4-hydroxy-3-methoxyphenyl)-7-(4-methoxyphenyl)-6-(2-hydroxy-4,6-dimethoxybenzoyl)-furano[3,2-g]benzopyran-4-one. This has been assigned the trivial name cissampeloflavone. The compound has good activity against Trypanosoma cruzi and T. brucei rhodesiense and has a low toxicity to the human KB cell line.

Headspace, solid-phase micro-extraction, gas chromatographic-mass spectrometric analysis of terpenoids in the latex of Euphorbia species.

The volatile and semi-volatile terpenoids in the latex of Euphorbia amygdaloides, E. exigua, E. helioscopia, and E. peplus were analyzed by headspace, solid-phase micro-extraction (HS-SPME), coupled with gas chromatography-mass spectrometry. The volatiles were extracted using a 100 microm polydimethylsiloxane SPME fiber under optimized extraction conditions. The compounds detected encompassed a range of chemical classes, but only terpenoids were evaluated. Only sesquiterpene hydrocarbons were detected in the tested samples of E. exigua, E. helioscopia, and E. peplus, with beta-caryophyllene being the major one, but were never recorded in latex samples of E. amygdaloides, in which only the diterpene hydrocarbon kaur-16-ene was detected. Alpha-Humulene was consistently found in samples of E. helioscopia, and E. peplus, but never in those of the other two species. These preliminary results show that the developed procedure is suitable for the analysis of small samples of Euphorbia latex and that, for each individual species, there is very little qualitative difference between samples, regardless of either place or date of collection.

Simultaneous quantification of Panax and Epimedium species using Rapid Resolution Liquid Chromatography (RRLC).

Two Rapid Resolution Liquid Chromatography (RRLC) methods have been developed and validated for simultaneous quantification of eight major ginsenosides from Panax species, namely, R1, Rg1, Re, Rf, Rb1, Rb2, Rc, and Rd, and flavonoids from Epimedium species, namely, epimedins A, B, and C and icariin. The analyses were performed using an Agilent 1200 series RRLC system with Phenomenex Luna C18-HST and Zorbax Eclipse XDB columns. The separation was performed with a gradient mobile phase of A (pure water) and B (acetonitrile) at a flow rate of 1.0 mL/min and 2.5 mL/min, respectively. Both columns were kept at 40 degrees C with the detection wavelength set at 203 nm. Specific eluted compounds were identified by using reference samples of ginsenosides R1, Rg1, Re, Rf, Rb1, Rc, Rb2, and Rd, and epimedins A, B, C and icariin. Baseline separation was achieved in less than 15 minutes for the Phenomenex Luna column and 4 minutes for the Zorbax Eclipse column. Characteristic RRLC profiles were established for complex mixtures of ginsenosides from Panax species and flavonoids from Epimedium species. Both methods developed here are effective for the quality control of formulated products containing both Panax and Epimedium varieties.

Simultaneous quantification of Echinacea species, Flos Lonicerae, Radix Scutellaria and Fructus Forsythiae combinations by rapid resolution liquid chromatography.

Echinacea angustifolia and E. purpurea are commonly used in North America for their anti-bacterial effects. Flos Lonicerae, Radix Scutellaria and Fructus Forsythiae are traditional Chinese medicinal herbs commonly used for the treatment of complaints such as pneumonia, acute upper respiratory tract infection, and acute bronchitis. A reproducible, simple, and reliable rapid resolution liquid chromatographic (RRLC) method has been developed to analyze extracts of products formulated containing E. angustifolia, E. purpurea, Flos Lonicerae, Radix Scutellariae and Fructus Forsythiae simultaneously in one run in less than 6 minutes. The method uses a C18-HST column, a mobile phase consisting of 0.1% aqueous phosphoric acid solution and acetonitrile, and UV detection at 327 nm and 229 nm. A stability test was performed that revealed that chlorogenic acid is more stable in acidic pH, and hence it is best to keep the extract of E. augustifolia, E. purpurea, Flos Lonicerae, Radix Scutellariae and Fructus Forsythiae in mild acidic conditions at approximately pH 5.

Simultaneous quantification of polyherbal formulations containing Rhodiola rosea L. and Eleutherococcus senticosus Maxim. using rapid resolution liquid chromatography (RRLC).

An RRLC method capable of simultaneous identification and rapid quantification of six biologically active compounds (salidroside, tyrosol, rosarin, rosavin, rosin, rosiridin) in Rhodiola rosea L. and two active compounds (eleutheroside B and eleutheroside E) in Eleutherococcus senticosus Maxim. was developed. The chromatographic analyses were performed on a reversed phase Phenomenex C18 (2)-HST column at 40°C with a neutral mobile phase (purified water and acetonitrile) gradient system at a flow rate of 1.0ml/min and UV detection at 205 and 220nm simultaneously. Baseline separation of eight active compounds was achieved within 8min. This developed method provides good linearity (R>0.9997), precision (RSD<1.99%) and recovery of the bioactive compounds. The RRLC method developed is capable of controlling the quality of R. rosea and E. senticosus raw herbs, commercial extracts, as well as polyherbal formulations containing R. rosea and E. senticosus as ingredients. This RRLC method is accurate and sensitive; in addition, it greatly increases sample analysis throughput with reduced analysis time, which is suitable for routine quality control analysis.

Rapid resolution liquid chromatography (RRLC) analysis for quality control of Rhodiola rosea roots and commercial standardized products.

A simple, sensitive and reliable reversed phase Rapid Resolution Liquid Chromatography (RRLC) method was developed and validated for six biologically active compounds (salidroside, tyrosol, rosarin, rosavin, rosin and rosiridin) in Rhodiola rosea L. roots and powder extracts. The method uses a Phenomenex C18 (2)-HST column at 40 degrees C with a neutral gradient system mobile phase (H20 and acetonitrile), a flow rate of 1.0 mL/min, and UV detection wavelengths set at 205 and 254 nm, simultaneously. Baseline separation of the six active compounds was achieved within 8 minutes. The average percentages of rosavins (rosarin, rosavin, and rosin) in authentic R. rosea roots and root powder extracts were quantitatively determined and a characteristic R. rosea roots RRLC profile was established. The RRLC method is accurate and sensitive; in addition, it effectively increases the sample analysis throughput compared with conventional HPLC.

Chemical composition and antioxidant activities of Jeddah corniche algae, Saudi Arabia.

The increased use of natural product in the pharmaceutical industry has led to an increase in demand for screening for bioactive compounds in marine algae. An important economic algae, through chemical composition analysis and their antioxidant activities were investigated in this study. Chemical composition analysis of three algal samples from the Chlorophyta Ulva lactuca (U), Phaeophyta Sargassum crassifolia (S) and Rhodophyta Digenea simplex (D) was tested. Main components were sugars (57.40-185.13 mg/g dry weight), uronic acids (29.3-45.26 mg/g dry weight), sulfate (94.7-181.2 mg/g dry weight), amino acids (7.6-16.7 mg/g dry weight) and small amounts of betaines (2.38-8.47 mg/g dry weight). Hydrolyzed chemical composition analysis fractions of algal extract was shown a great proportion of sugars plus sulfate (as polysaccharide composed) ranges between 332 and 538.2 mg/g dry weight with trace amounts of uronic acids (⩽9%). All three algal extract showed antioxidant activities on lipoxygenase, DPPH and on Ames test. Two of aqueous extracts (U and D) inhibited lipoxygenase activity by less than 50%, where as the methanolic extract (S) caused 76% inhibition of the control. In all cases, the methanolic extract were more inhibitory than the aqueous extract. The (S) showed the highest antioxidant activity with DPPH (69%) in aqueous extract and in methanol extract with Ames test (85%). Both U and D showed antioxidant activity with DPPH in hexane by less of 25% where as in both aqueous and methanolic extracts by less than 50% of the control. Aqueous and methanolic extracts of U and D showed high inhibition by Ames test which caused 70% and 75% respectively. IR spectra of algal extracts (U; D and S) range from 1450 to 750 cm(-1) were very similar absorption band at 1430, 1370, 1250, 1130, 1110, 1050 and 1020 cm(-1). Absorption bands were due to uronic acids, glucosides and sulfate. The presence of sulfated polysaccharide material in the fractions UF2, DF2 and SF2 were found as cell wall storage of marine algae, confirmed by (13)C NMR spectroscopy. It is concluded that the algal species probably have a different components and can be used in the activities of antioxidant enzymes as reduced the risks of enzymes. But the correlation between the chemical composition and antioxidant activities of algal extracts needs further investigation.

Relaxant activity of raspberry (Rubus idaeus) leaf extract in guinea-pig ileum in vitro.

Tea made from the leaves of Rubus idaeus L. (raspberry) has been used for centuries as a folk medicine to treat wounds, diarrhoea, colic pain and as a uterine relaxant. Extracts of dried raspberry leaves prepared with different solvents, (n-hexane, ethyl acetate, chloroform and methanol) were tested in vitro for relaxant activity on transmurally stimulated guinea-pig ileum. The methanol (MeOH) extract exhibited the largest response and also indicated that the active compounds are of a relatively polar nature. Hence the bulk of the leaves were extracted with methanol and the dried extract fractionated on a silica gel column, eluting with chloroform, mixtures of chloroform and methanol and finally methanol. Each fraction was examined by thin layer chromatography and tested for relaxant activity in an in vitro transmurally stimulated guinea-pig ileum preparation. The fractions eluted with chloroform (CHCl(3)) lacked relaxant activity. Samples eluted with CHCl(3)/MeOH (95:5) had moderate relaxant activity, while a second distinctive peak of activity eluted with a more polar solvent mixture (CHCl(3)/MeOH 50:50) provided strong dose dependent responses. Evidence was obtained that there are at least two components of raspberry leaf extract which exhibit relaxant activity in an in vitro gastrointestinal preparation.