Phytochemical and biological evaluation of Buddleja polystachya growing in Saudi Arabia.

Several Buddleja species were the target of phytochemical and biological studies; however, nothing was reported concerning the chemistry of Buddleja polystachya Fresen. growing in Saudi Arabia. Sixteen constituents were isolated from the aerial parts of B. polystachya using various chromatographic techniques and were identified by the help of different spectral techniques including 1D, 2D NMR and mass spectrometry. Moreover, the different fractions were evaluated for their anti-inflammatory and hypoglycemic activities. The isobenzofuranone derivative (4-hydroxy-7-methylisobenzofuranone) (4), has been isolated for the first time from this natural source, B. polystachya, along with fifteen known compounds namely; phenolic fatty acid ester, 1'(4-hydroxyphenyl) ethanol ester of docosanoic (1), uvaol (2), sakuranetin (3), kumatakenin (5), cirsimaritin (6), 5-hydroxy-3,7,4'-trimethoxyflavone (7), oleanolic acid (8), herbacetin 3,7,8-trimethyl ether (9), ursolic acid (10), verbascoside (11), linarin (12), luteolin 7-O-ß-D-glucoside (13), luteolin 7-(6"-caffeoyl)-O-ß-D-glucopyranoside (14), luteolin (15), and 6-O-α-L-(4''-O-trans-cinnamoyl) rhamnopyranosylcatalpol (16). Regarding the biological activities investigated, the ethyl acetate fraction showed the most significant anti-inflammatory activity, followed by the n-butanol and the aqueous fractions. As for the petroleum ether and dichloromethane fractions, their anti-inflammatory effects were moderate. The highest hypoglycemic activity was possessed by the ethyl acetate fraction, followed by the dichloromethane fraction and the n-butanol fraction showed the weakest activity.

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.

Effect of some plants' extracts used in Sudanese folkloric medicines on carrageenan-induced inflammation.

Investigations for anti-inflammatory potential and categorization of Sudanese medicinal plants according to their potency. Anti-inflammatory effect of plants' extracts of 17 genera were studied using the carrageenan induced inflammation in rats' paws. The plant extracts were obtained using methanol and dichloromethane as solvent and administered intra peritoneally at the concentration of 2g/kg body weight. The results obtained in this experiment strongly support and validate the traditional uses of these Sudanese medicinal plants to treat various inflammatory diseases. 63.9% of plants extracts showed marked inhibition of inflammation induced by carrageenan (78.3% out of this percentage represented by methanolic extract), 27.8% showed no activity and 8.3% enhanced the carrageenan induced inflammation. The anti-inflammatory effect of many of these plants has not been reported previously, yet they have been extensively used in Sudanese folkloric medicine. The result of this study justify the traditional medicinal use of the evaluated plants species in treating inflammatory disorders and helped in categorizing the investigated plants into most useful, moderately useful and least useful category for inflammatory diseases. Out of the 17 investigated plant species 05 belongs to most useful and 06 belongs to moderately useful category. However, toxicity studies are required to prove the safety of these plant materials.

Molecular mechanisms that underlie the sexual stimulant actions of Avicennia marina (Forssk.) Vierh. and Crocus sativus L.

The effects of extracts and sub-fractions of Avicennia marina, Crocus sativus and sildenafil on the sexual behavior of male rats and their effects on the intracavernosal pressure (I.CV), intracavernosal cyclic GMP and dihydrotestosterone plasma level were examined. The sexual behavior was followed for four hours using infra-red video cameras to quantify the effects on various male sexual behaviors. The results revealed that the active sub-fraction in case of A. marina was the hexane fraction of the chloroform extracts (C/H) whereas that of C. sativus was the hexane fraction of the alcoholic extract (A/H). (C/H), (A/H) and sildenafil significantly increased the total sexual stimulation index from 53.8±2.7 (control) to 406±7.8, 225±4 and 401±30.1, respectively (P<0.001, N=6). They significantly increased the index of successful mounting and ejaculation from 2.6±0.5 (control) to 40±2.7, 21±2.3 and 18±1.7, respectively (P<0.01, N=6). They significantly increased the cyclic GMP level from 0.94±0.07 (control) to 3.1±0.13, 1.59±0.11 and 3.66±0.19 ng/mg wet tissue, respectively (P<0.05, N=7). They did not affect dihydrotestosterone plasma level. (C/H), (A/H) and sildenafil increased the (I.CV) pressure by 4.8±0.3, 1.4±0.8 and 4.2±0.9 mmHg. The (C/H) seemed to be more active than sildenafil and twice active than (A/H). Both extracts and sildenafil acted via an increase in cyclic GMP.

Factors associated with adherence to medication among depressed patients from Saudi Arabia: a cross-sectional study.

BACKGROUND: Several studies have investigated the factors associated with adherence to antidepressants, with inconsistent conclusions. However, no similar study has investigated this issue among patients diagnosed with major depressive disorder in Saudi Arabia. The aim of this study is to explore patients' adherence to antidepressant medications, and the factors associated with adherence. METHODS: A non-experimental cross-sectional design was used to measure adherence to antidepressants among major depressive disorder patients, and the factors associated with adherence. The patients were recruited from the outpatient clinic at the Al-Amal Complex for Mental Health in Riyadh, Saudi Arabia, between August 2013 and January 2014. Eligible participants met with one of the research coordinators for assessment of their adherence. Adherence was investigated indirectly by use of the Morisky Medication Adherence Scale, and patients' beliefs were assessed through the Beliefs about Medicine Questionnaire. Information about the severity of their depression, demographics, and other study variables were collected. RESULTS: A total of 403 patients met the inclusion criteria and participated in the study. Of those, 203 (50.37%) were females, while the remaining 200 (49.6%) were males. There was an average age of 39 years (standard deviation, ±11 years). Half of the patients (52.9%) reported low adherence to their antidepressant medication, with statistically significant differences between the low adherence and high adherence scores relating to sex, age, and duration of illness. CONCLUSION: Low medication adherence is a common problem among major depressive disorder patients in Saudi Arabia. Medication-taking behavior among depressed patients is influenced by several factors, mainly patients' beliefs regarding antidepressants. This study has improved the understanding of the factors associated with adherence to antidepressants.

Biological effects of a new set 1,2,4-triazolo[1,5-a]quinazolines on heart rate and blood pressure.

BACKGROUND: Several quinazoline and triazole derivatives are reported to possess a wide-range of interesting pharmacological effects. Although various triazoloquinazoline subclasses having been synthesized and studied, the preparation of 1,2,4-triazolo[1,5-a]quinazolines as antihypertensive agent is still relatively unexplored. In continuation of our earlier research, we aimed at the synthesis and development of various potent antihypertensive 1,2,4-triazoloquinazoline derivatives. RESULTS: A new series of 1,2,4-triazolo[1,5-a]quinazoline derivatives have been synthesized. Their structures were mainly established by spectroscopic methods of analysis (IR, MS, 1H and 13C NMR). Their in vivo antihypertensive activity was evaluated by tail cuff method using Muromachi Blood Pressure Monitor (Model MK 2000) for rats and mice. Some of the tested compounds were found to exhibit valuable effects in terms of heart rate and blood pressure. According to the biological results, some of tested derivatives have abolished completely the tachycardia of the parent compounds and may be studied and modified as potential adrenoblockers and cardiac stimulant. CONCLUSION: New series of fifteen 1,2,4-triazolo[1,5-a]quinazolines were synthesized by convenient methodology from four key molecules, whereby their structures were established by advanced spectroscopic analyses. Some lead compounds have abolished completely the tachycardia of the parent compounds, that may be examined as potent adrenoblockers and some other compounds seem to be a cardiac stimulant or may be modified to enhance their hypotensive activity.

Synthesis and hypoglycemic activity of some new theophylline derivatives.

Thirty-one new theophylline derivatives have been synthesized and evaluated for their hypoglycemic activity. Compounds 24 (56% reduction) and 31 (57% reduction) showed better hypoglycemic activity than the standard drug glibenclamide which showed 52% reduction in serum glucose level. Compound 27 remarkably reduced serum glucose level by 53%. Ten compounds showed varying degrees of hypoglycemic activity ranging from 20 to 37% reduction in serum glucose level compared to the standard drug. The aromatic amide functionality is the common feature of these theophylline hypoglycemic derivatives. However, anthranilamide and or aliphatic amides proved to be the least active compounds in the present series.

Citrus medica "Otroj": attenuates oxidative stress and cardiac dysrhythmia in isoproterenol-induced cardiomyopathy in rats.

Citrus medica L. commonly known as Otroj, is an important medicinal plant reputed for its nutritious and therapeutic uses. The present work was undertaken to investigate the protective effect of the ethanolic extract of otroj (EEOT) against isoproterenol (ISO)-induced cardiotoxicity in rats. In addition, the antioxidant activity and the phenolic and flavonoidal contents were determined. Rats were administered EETO (250 and 500 mg/kg) or vehicle orally for 15 days along with ISO (85 mg/kg, s.c.) on the 14th and 15th day. ISO induced cardiac dysfunction, increased lipid peroxidation and alteration of myocyte-injury specific marker enzymes. ISO also showed an increase in levels of plasma cholesterol, triglycerides (TG), LDL-C, and VLDL-C. Moreover, the histological investigations showed myocardial necrosis and inflammation. EETO treatment brought the above parameters towards normal level. Moreover, in vitro DPPH radical scavenging and ß-carotene-linoleic acid tests of the EEOT exhibited a notable antioxidant activity in both assays used. In addition, histopathological examination reconfirmed the protective effects of EEOT. Thus, the present study reveals that C. medica alleviates myocardial damage in ISO-induced cardiac injury and demonstrates cardioprotective potential which could be attributed to its potent antioxidant and free radical scavenging activity.

Studies on tracheorelaxant and anti-inflammatory activities of rhizomes of Polygonatum verticillatum.

BACKGROUND: The present study describes the tracheorelaxant and anti-inflammatory effects of Polygonatum verticillatum which may support its medicinal use in hyperactive airway complaints and inflammatory disorders. METHODS: The tracheorelaxant activity of crude extract of the rhizomes of P. verticillatum (PR) was assessed in isolated guinea-pig tracheal tissues immersed in tissue organ bath filled with Tyrode's solution and a continuous supply of carbogen gas (95% O2 and 5% CO2). The contractile and relaxant responses of the tissue were measured using isometric transducers coupled with Power-Lab data acquisition system. The anti-inflammatory effect was evaluated in carrageenan-induced rat paw edema model, while the lipoxygenase inhibitory activity was performed in the in-vitro assay. Various chromatographic and spectroscopic techniques were used for the isolation and characterization of pure molecules. RESULTS: In isolated guinea-pig tracheal preparations, PR caused complete inhibition of the high K+ (80 mM) and carbachol-induced contractions however, it was more potent against K+ than CCh, similar to verapamil. Pretreatment of the tissue with PR, displaced the Ca2+ concentration-response curves to the right, similar to that induced by verapamil, indicating the presence of Ca2+ channel blocking like activity. When tested on carrageenan-induced rat paw edema, PR demonstrated a marked reduction in edema with 65.22% protection at 200 mg/kg, similar to aspirin. In the in-vitro assay, PR showed lipoxygenase inhibitory activity (IC50: 102 ± 0.19 µg/mL), similar to baicalein. Bioactivity-guided fractionation led to the isolation of 2-hydroxybenzoic acid and ß-sitosterol. CONCLUSIONS: These results indicate that the plant possesses tracheorelaxant, mediated possibly through a Ca2+ channel blockade mechanism, and anti-inflammatory activities, which may explain the medicinal use of this plant in airway disorders and inflammation.

New flavane gallates isolated from the leaves of Plicosepalus curviflorus and their hypoglycemic activity.

Two new flavane gallates were isolated from the leaves of Plicosepalus curviflorus. The structure of the new compounds was established as 2S,3R-3,3',4',5,7-pentahydroxyflavane-5-O-gallate (1) and 2S,3R-3,3',4',5,5',7-hexahydroxyflavane-4',5-di-O-gallate (2), respectively. In addition, seven known compounds (-)-catechin (3), quercetin (4), lupeol (5), ß-sitosterol (6), pomolic acid (7), ß-sitosterol 3-O-ß-d-glucopyranoside (8) and 4-methoxycinnamic acid (9) were reported for the first time from the genus Plicosepalus. Compounds 1, 2 and 3 were investigated for their hypoglycemic activity and showed significant hypoglycemic activity in Swiss Albino mice.

Synthesis, analgesic and anti-inflammatory evaluation of some novel quinazoline derivatives.

Two series of some new 2,4,6-trisubstituted-quinazoline derivatives were prepared and screened for their analgesic, anti-inflammatory activity and acute toxicity. Four compounds were more potent analgesic agents than the reference drug Indomethacin and thirteen compounds showed significant anti-inflammatory activity. Seven compounds showed combined ability to inhibit both pain and inflammation. Compounds tested for acute toxicity showed no toxic symptoms or mortality rates 24 h post-administration implying their good safety margin.

Effect of Commiphora opobalsamum (L.) Engl. (Balessan) on experimental gastric ulcers and secretion in rats.

The ulcer protective potential of an ethanol extract of Commiphora opobalsamum (L.) Engl. (Burseraceae) 'Balessan' was assessed against different acute gastric ulcer models in rats induced by necrotizing agents (80% ethanol, 0.2M NaOH and 25% NaCl), hypothermic restraint stress, pyloric ligation (Shay) and indomethacin. Balessan, 250 and 500 mg/kg administered orally (intraperitoneally in Shay rat model) showed a dose-dependent ulcer protective effects in all the above ulcer models. Besides, the extract offered protection against ethanol-induced depletion of stomach wall mucus and reduction in nonprotein sulfhydryl (NP-SH) concentration. Ethanol treatment also caused histopathological lesions of the stomach wall. Pretreatment with Balessan extract provided a complete protection of gastric mucosa through supporting both the offensive and defensive factors. Balessan extract was also showed a large margin of safety without any apparent adverse effects in rats.

Drug-induced pulmonary fibrosis.

Pulmonary fibrosis is characterized by the accumulation of excessive connective tissue in the lungs. Its causes include chronic administration of some drugs for example bleomycin, cyclophosphamide, amiodarone, procainamide, penicillamine, gold and nitrofurantoin; exposure to certain environmental factors such as gases, asbestos and silica and bacterial or fungal infections. Some systemic diseases also predispose to the disease for example rheumatoid arthritis and systemic lupus erythematosus. The disease is associated with release of oxygen radicals and some mediators such as tumor necrosis factor-alpha TNF-alpha, transforming growth factor-beta TGF-beta, PDGF, IGF-I, ET-I and interleukins 1, 4, 8 and 13. The symptoms of the disease include dyspnea, non-productive cough, fever and damage to the lung cells. It is diagnosed with the aid of chest radiography, high resolution computed tomographic scanning and the result of pulmonary function tests. Drug-induced pulmonary fibrosis may involve release of free oxygen radicals and various cytokines for example IL-Ibeta and TNF-alpha via activation of nuclear transcription factor NF-beta as in the case of bleomycin and mitomycin or via release of TGF-beta as in case of tamoxifen or via inhibition of macrophages' and lymphocytes' phospholipases as in the case of amiodarone with the resultant accumulation of phospholipids and reduction of the immune system.

Prevention of experimentally-induced gastric ulcers in rats by an ethanolic extract of "Parsley" Petroselinum crispum.

An ethanolic extract of Parsley, Petroselinum crispum (Mill.) Nym.ex A.W. Hill (Umbelliferae), was tested for its ability to inhibit gastric secretion and to protect gastric mucosa against the injuries caused by pyloric ligation, hypothermic restraint stress, indomethacin and cytodestructive agents (80% ethanol, 0.2 M NaOH and 25% NaCl) in rats. The extract in doses of 1 and 2 g/kg body weight had a significant antiulcerogenic activity on the models used. Besides, ethanol-induced depleted gastric wall mucus and non-protein sulfhydryl contents were replenished by pretreatment with Parsley extract. Acute toxicity tests showed a large margin of safety for the extract. The phytochemical screening of Parsley leaves revealed the presence of tannins, flavonoids, sterols and/or triterpenes.