Experimental and clinical antihypertensive activity of Matricaria chamomilla extracts and their angiotensin-converting enzyme inhibitory activity.

Three different extracts of Matricaria chamomilla L. were evaluated for their antihypertensive activity, these extracts were total alcohol extract (Extract 1), oil extracted (Extract 2), and water lifted after oil extraction (Extract 3). Quantitative and Qualitative analyses were carried out for all extracts. The 3 extracts were proved to be safe for human use. A single oral administration of the plant extracts (200 mg/kg) decreases both systolic and diastolic blood pressure of normotensive rats after 1, 1.5, and 2 hr. Furthermore, groups treated with the evaluated extracts (100 & 200 mg/kg) or Captopril (20 mg/kg) showed a significant reduction in the elevated blood pressure and heart rate. Extract 3 showed the most antihypertensive activity. Serum biochemical parameters and lipid profile levels of treated groups were improved in comparison with induced-hypertensive untreated rats. In evaluation of oxidative damage parameters Glutathione and superoxide dismutase (SOD) in some organs, the investigated extracts or captopril restored the amount of reduced Glutathione in tissues in addition to an increase in the activity of the SOD after a significant depletion of SOD activity. In the clinical study, there was a significant dose dependent decrease in Systolic blood pressure, Diastolic blood pressure, and heart rate compared with their basal values in both normotensive and hypertensive human volunteers after oral administration of Matricaria chamomilla beverages.

Anticandidal Activity of Extracts and a Novel Compound, Amnomopin, Isolated From Petriella setifera.

A novel triterpenoidal compound named 'amnomopin' (3ß-diglucoside-5,12-28-oic acid), which is named IUPAC as 3-O-(2' âž” 1″diglucoside)1,2,3,4,4a,5,6,6a,6b,7,9,10,11,12,12a,12b,13,14b-octadecahydro-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethylpicene-4a-carboxylic acid, was isolated from the extract Petriella setifera. The total alcoholic extract of P. setifera showed a great activity against clinically isolated Candida species, including Candida albicans, Candida dubliniensis, Candida famata, Candida glabrata, Candida inconspicua, Candida kefyr, Candida krusei, Candida norvegensis, Candida parapsilosis and Candida tropicalis. Also, the new compound amnomopin was active against all the investigated Candida species. The highest anticandidal activity of P. setifera extract was obtained against C. kefyr (22.6 ± 1.5 mm), C. albicans and C. norvegensis (21.3 ± 0.63 mm) and C. krusei (20.6 ± 1.5 mm). Moreover, the minimum inhibitory concentrations of both the total extract and the isolated compound were low. The minimum inhibitory concentration of the compound isolated from P. setifera was 0.49 µg/mL against C. kefyr, 0.98 µg/mL against C. albicans and C. norvegensis and 1.95 µg/mL against C. krusei. The oral dosing of the extract and the isolated compound did not show any significant effect on the activity of alanine aminotransferase, aspirate aminotransferase and the levels of blood urea and serum creatinine. Copyright © 2017 John Wiley & Sons, Ltd.

Amhezole, A Novel Fungal Secondary Metabolite from Aspergillus terreus for Treatment of Microbial Mouth Infection.

Bio-guided fractionation of Aspergillus terreus extract leads to isolation of a novel terpenoidal secondary metabolite. The isolated compound and the total alcoholic extract of Aspergillus terreus showed a remarkable activity against microbial mouth infections; namely, Candida albicans, Lactobacillus acidophilus, Streptococcus gordonii, and S. mutan. Moreover, the Minimum Inhibitory Concentration of the isolated compound was determined and showed low values. The combination of each of the alcoholic extract of A. terreus and the isolated compound Coe-Comfort tissue conditioner inhibited the growth of Candida albicans at concentrations of 500 and 7.81 µg/mL, respectively, Lactobacillus acidophilus at concentrations of 250 and 7.81 µg/mL, respectively, Streptococcus gordonii at concentrations of 1000 and 62.50 µg/mL, respectively, and S. mutans at concentrations of 1000 and 125 µg/mL, respectively. The oral dosing of the extract and the isolated compound did not show any significant effect on the activity of alanine aminotransferase, aspirate aminotransferase, and the levels of blood urea and serum creatinine. Copyright © 2017 John Wiley & Sons, Ltd.

New Activities for Isolated Compounds from Convolvulus austro-aegyptiacus as Anti-ulcerogenic, Anti-Helicobacter pylori and Their Mimic Synthesis Using Bio-guided Fractionation.

Bio-guided fractionation of the total alcoholic extract of Convolvulus austro-aegyptiacus was screened for its anti-ulcerogenic activity, using an absolute-ethanol-induced ulcer model at 500 and 1000 mg/kg doses. Two compounds were isolated from the butanol extract of C. austro-aegyptiacus and identified by 1 H and 13 C nuclear magnetic resonance as scopoletin and scopolin. The isolated compounds (50 mg/kg) showed a remarkable anti-ulcerogenic activity because they exhibited control-ulcer protection by 16.7% and 90.8%, respectively. The acute toxicity study showed that the extract is highly safe; the median lethal dose (LD50) was more than 4000 mg/kg. Moreover, the obtained results were confirmed by the sub-chronic toxicity because the rats that have been administered 1000 mg/kg of the extract for 15 consecutive days showed no alteration in the liver and kidney functions. Copyright © 2015 John Wiley & Sons, Ltd.

Prophylactic and curative anti-ulcerative colitis activity and the possible mechanisms of action of some desert plants.

The aim of the present study was to evaluate both prophylactic and curative anti-ulcerative colitis activity and the possible mechanism of action of seven desert plant extracts. Seven desert plants from different families; Conyza dioscoridis (L.) Desf. (Asteraceae), Euphorbia hirta L. (Euphorpiaceae), Origanum syriacum L. and Salvia lanigera L. (Lamiaceae), Sisymbrium irio L., Solanum nigrum Linn. (Solanaceae) and Solenostemma arghel (Del.) Hayne. (Asclepiadaceae) were separately evaluated at three doses (125, 250, and 500 mg/kg) using the acetic acid-induced colitis model. The investigated extracts possessed prophylactic and curative anti-ulcerative colitis activities in a dose-dependent manner, where Salvia lanigera (87.9) and Solenostemma arghel (89.2) were the most effective extracts whereas the dexamesathone produced 68%. These extracts were further investigated for estimation of their mechanism of action. The in vitro potential radical (DPPH) scavenging activities of the investigated extracts were well supported with the reduction of colonic MDA content for both extracts. Suppression of the inflammatory mediator TNF-α and inhibition of both PLA2 and protease enzymes may play an important role in the anti-ulcerative colitis activities. The investigated extracts were safe for use up to 5 g/kg and the total alcohol extracts of Salvia lanigera and Solenostemma arghel (400 mg/kg for 35 d) showed no alteration on liver and kidney functions. Phytochemical screening of the investigated extracts revealed the presence of flavonoids, tannins, unsaturated sterols, and proteins which could be responsible for the activities.

Anti-leishmanial activities of extracts and isolated compounds from Drechslera rostrata and Eurotium tonpholium.

The fungal extract of Drechslera rostrata and Eurotium tonpholium showed a significant anti-leishmanial activity against Leishmania major; IC50 was 28.8 and 28.2 µg/mL, respectively. Seven compounds, five from D. rostrata (H1-H5) and two from E. tonpholium (H6 and H7), were isolated and identified using different spectroscopic analysis including (1) HNMR, (13) CNMR, Hetero-nuclear multiple bond connectivity (HMBC), Hetero-nuclear Multiple Quantum Correlation (HMQC), and EI-MS. The isolated compounds are: di-2-ethylhexyl phthalate (1), (22E)-5α,8α-epidioxyergosta-6,22-diene-3ß-ol (2),1,3,8-trihydroxy-6-methyl-nthraquinone (3), aloe-emodine 8-O-glucopyranoside(4), 2R, 3R,4R,5R hexane 1, 2, 3, 4, 5, 6 hexole (Mannitol) (5), 1,8-dihydroxy-3-methoxy-6-methyl-anthraquinone (6) and 1, 4, 5-trihydroxy-7-methoxy-2-methyl-anthraquinone (7). However, compounds (1) and (6) showed activity against L. major with IC50 of 3.2 and 10.38 µg/mL, respectively. On the other hand, oral administration of the two extracts (100 mg/kg) and compounds 1 and 6 (50 mg/kg) showed very good activity when compared with the anti-leishmanial drug Pentostam (125 mg/kg). Interestingly, the complete heeling activity of the extracts and compounds (1) and (6) was obtained after 13-17 days of treatment, while complete healing activity of Pentostam was obtained after 28 days. No alteration on liver and kidney functions was recorded on animals treated with the two extracts for 15 consecutive days.

Anti-ulcerative colitis activity of compounds from Euphorbia granuleta Forssk.

The aim of the present study was to evaluate the anti-ulcerative colitis (UC) activity of the total alcohol extracts of Euphorbia granuleta Forssk. (Euphorpiaceae), isolate and identify the active compounds that could be responsible for the activity, in addition to determination of the possible mechanism of action. Six compounds were isolated and identified from this plant: three phenolic compounds (kampferol, kampferol-3-glucoside and kampferol-3-galactoside) in addition to three steroidal compounds (1-ethoxypentacosane, heptacosan-1-ol and ß-sitosterol). Three compounds (heptacosan-1-ol, ß-sitosterol and kampferol-3-galactoside) were found to be responsible for the anti-UC activity of E. granuleta extract. The anti-UC activity of these compounds may be explained by reducing the pro-inflammatory cytokine tumor necrosis factor-alpha (TNF-α), in addition to reduction of colonic malondialdehyde (MDA) contents. No side effects were reported on liver and kidney functions. The active compounds reduced both serum TNF-α and mucosal MDA levels.

Antiulcerogenic activities of the extracts and isolated flavonoids of Euphorbia cuneata Vahl.

The total alcohol extracts of Euphorbia cuneata Vahl.(Euphorbiaceae) were screened for antiulcerogenic activity using an ethanol-induced ulcer model at doses of 125, 250 and 500 mg/kg. The extracts possessed antiulcerogenic activity in a dose-dependent manner. Four flavonoidal compounds were isolated and identified as naringenin, aromadendrin, apigenin and 4'-O-methoxy-luteolin-7-O-rhamnoglucoside, each demonstrating antiulcerogenic activity with curative ratios ranging from 75.78% to 88.23%. In addition, the alcohol extracts and isolated compounds were shown to scavenge the 1,1-diphenyl,2-picrylhydrazyl radical by different ratio, with the most effective being 4'-O-methoxy-luteolin-7-O-rhamnoglucoside (91.14%). The antioxidant activity of the alcohol extracts and the isolated compounds may explain the antiulcerogenic properties. No side effects were observed on either liver or kidney functions.

New biological activities of Casimiroa edulis leaf extract and isolated compounds.

The phytochemical investigation of Casimiroa edulis Llave et Lex (Rotaceae) afforded four coumarins: umbelliferone (1), esculetin (2), imperatorin (3) and xanthotoxol (4). The identification of these compounds was achieved by using a combination of m.p., UV, EI-mass, ¹H NMR and ¹³C NMR spectroscopy. Essential oil extracts were analysed by GC/MS leading to the identification of 60 components. Sesquiterpene hydrocarbons accounted for the major make up of the oil. Microbiological screenings of the oil and successive plant fractions were performed, showing promising activity against a number of microorganisms with Minimum inhibitory concentrations (MIC) comparable to the standard antibiotics such as chloramphenicol and kanamycin. The plant ethanol extract (400 mg/kg) and the isolated coumarins (60 mg/kg) showed anticoagulant activity. Analyses to determine the activity of the extracts on liver and kidney function were performed, revealing no negative or detrimental effects.