Sea Lamprey Alarm Cue Comprises Water- and Chloroform- Soluble Components.

A diversity of aquatic organisms manage predation risk by avoiding waters activated with conspecific alarm cues, a chemical mixture released from injuries. The sea lamprey (Petromyzon marinus) is a nocturnal migratory species that relies on its alarm cue to navigate around areas of predation risk when moving through river channels. Identification of the cue's chemistry would allow managers to harness this innate behavioral response to guide migrating sea lamprey to traps (invasive population in the Laurentian Great Lakes) or to fish passage devices where dams block migrations in their native range. We pursued isolation of the sea lamprey alarm cue through behaviorally guided fractionation, fractionating the alarm cue into water-soluble and chloroform-soluble fractions, each of which elicited a substantial avoidance response. Recombining the two fractions restored full reactivity, suggesting the alarm cue mixture contains components that exhibit high solubility in water (e.g., nitrogenous compounds), chloroform (e.g., lipids), or perhaps materials that dissolve readily in either solvent. We further screened 13 individual compounds or pure isolates and 6 sub-fractions from the water-soluble fraction and found one of the pure isolates, isoleucine, evoked an avoidance response on its own, but not consistently when found in other mixtures. In a third experiment, we observed no behavioral response after recombining 32 compounds isolated and identified from the water-soluble fraction. These results confirm other suggestions that the process of elucidating alarm cue constituents is challenging. However, we suggest the pursuit is worthwhile given the strong evidence for the utility of alarm cues for use in the conservation and management of fishes and other aquatic organisms.

The effect of putrescine on space use and activity in sea lamprey (Petromyzon marinus).

Fish use odor to avoid exposure to predation and disease. Harnessing these odors as repellents is proving useful for management initiatives that conserve native species or control invasive populations. Here, we evaluated the behavioral response of invasive sea lamprey to putrescine, a decay molecule that many prey organisms avoid. Putrescine is found in tissue extracts that contain sea lamprey alarm cue, and human saliva, two mixtures known to elicit flight and avoidance responses in migratory sea lamprey. We used two behavioral assays to evaluate metrics of repellency: behavioral preference (space use) and change in activity rates and found context-dependent results. In smaller assays with individual fish, we found that putrescine had no effect on sea lamprey activity but did induce avoidance. In larger assays with multiple animals, sea lamprey did not avoid putrescine. Our results also showed consistent changes in activity and avoidance behavior in sea lamprey exposed to alarm cue in the smaller assay, concluding that this design could prove useful as a high-throughput screening tool. We also investigated a novel odor identified in sea lamprey skin, petromyzonacil, and found no behavioral effects to this odor on its own or in synergy with putrescine. Our results show limited evidence that putrescine acts as robust repellent for sea lamprey and highlight the importance of environmental context when interpreting avoidance behavior in laboratory settings.

The edible seaweed Laminaria japonica contains cholesterol analogues that inhibit lipid peroxidation and cyclooxygenase enzymes.

In this study, 5 sterols were isolated and purified from Laminaria japonica, commonly known as edible brown seaweed, and their structures were identified based on detailed chemical methods and spectroscopic analyses. Spectroscopic analyses characterized 5 sterols as 29-Hydroperoxy-stigmasta-5,24(28)-dien-3ß-ol, saringosterol (24-vinyl-cholest-5-ene-3ß,24-diol), 24-methylenecholesterol, fucosterol (stigmasta-5,24-diene-3ß-ol), and 24-Hydroperoxy-24-vinyl-cholesterol. The bioactivities of these sterols were tested using lipid peroxidation (LPO) and cyclooxygenase (COX-1 and -2) enzyme inhibitory assays. Fucosterol exhibited the highest COX-1 and -2 enzyme inhibitory activities at 59 and 47%, respectively. Saringosterol, 24-methylenecholesterol and fucosterol showed higher LPO inhibitory activity at >50% than the other compounds. In addition, the results of molecular docking revealed that the 5 sterols were located in different pocket of COX-1 and -2 and fucosterol with tetracyclic skeletons and olefin methine achieved the highest binding energy (-7.85 and -9.02 kcal/mol) through hydrophobic interactions and hydrogen bond. Our results confirm the presence of 5 sterols in L. japonica and its significant anti-inflammatory and antioxidant activity.

Zanzibar yam (Dioscorea sansibarensis Pax) isolates exhibit cyclooxygenase enzyme and lipid peroxidation inhibitory activities.

Several phenanthrenes (1-5), phenolics (6-8) and steroidal sapogenins (9-11) were isolated for the first time from the aqueous and methanolic extracts of Dioscorea sansibarensis Pax yam collected from Tanzania. Chemical structures of all the isolates (1-11) were determined by using 1D and 2D nuclear magnetic resonance spectral methods. All pure isolates were evaluated for anti-inflammatory activity using in vitro cyclooxygenase enzyme (COX-1 and -2) inhibitory assays. Among the isolates tested, phenanthrenes 3-5 showed the highest COX-1 and -2 enzyme inhibitory activity whereas phenolics (6-8) and steroidal sapogenins (9-11) exhibited moderate inhibition when compared to non-steroidal anti-inflammatory drugs aspirin, ibuprofen and naproxen. Compounds 6-11 were evaluated for antioxidant activity using lipid peroxidation inhibitory (LPO) assay for the first time and exhibited moderate LPO inhibition.

Cyclooxygenase Enzyme and Lipid Peroxidation Inhibitory Terpenoids and Steroidal compounds as Major Constituents in Cleome viscosa Leaves.

Bioassay guided study of Cleome viscosa Linn. (Cleomaceae) leaves led to the isolation of a new cembrenoid diterpene (1: ) and three known compounds (2:  - 4: ) from the hexane extract. The chemical structures of these compounds were elucidated by spectroscopic methods such as NMR (1D and 2D), HRMS and IR and identified and afforded compound 1: , malabaric acid (2: ), stigmast-4-en-3-one (3: ) and stigmast-4-ene-3,6-dione (4: ). This is the first report of compounds 1: and 2: from C. viscosa Linn. Isolates were evaluated for anti-inflammatory activity using in vitro cyclooxygenase enzyme (COX-1 and -2) inhibitory assays. The novel cembrenoid diterpene (1: ) exhibited IC50 values of 8.4 µM for COX-1 enzyme and 45.2 µM for COX-2 enzyme, respectively. Similarly, malabaric acid (2: ) exhibited IC50 values of 11.5 µM for COX-1 enzyme and 46.9 µM for COX-2 enzyme, respectively. Their inhibitory activities were in par with non-steroidal anti-inflammatory drugs aspirin, ibuprofen and naproxen. Sterols 3: and 4: gave IC50 values of 62.6 and 67.9 µM, respectively for COX-1 enzyme while indicating weak COX-2 enzyme inhibition. Lipid peroxidation inhibitory (LPO) and MTT assays were used to determine antioxidant activity of these compounds. Compounds 1:  - 4: showed LPO inhibition with IC50 values between 82 and 100 µM and moderate antioxidant activity in the MTT assay. Biological activities reported for these compounds are for the first time and it support anecdotal medicinal claims of C. viscosa Linn. leaves.

Evaluation of health benefits of sea lamprey (Petromyzon marinus) isolates using in vitro antiinflammatory and antioxidant assays.

Sea lamprey (Petromyzon marinus), a parasitic fish which survives on blood of other fishes, is consumed as a delicacy in many countries. Our earlier studies on sea lamprey compounds that showed potential to deter adult sea lampreys yielded several sterols, glycerides, free fatty acids, amino acids, organic acids and nitrogenous compounds. Therefore, this study was to assess the health-benefits of these compounds including additional isolates from HPLC fractions that kept aside due to lack of activity in sea lamprey deterrent assays. In vitro cyclooxygenase enzymes (COX-1 and -2) and lipid peroxidation (LPO) inhibitory assays, respectively, were used to determine antiinflammatory and antioxidant activities. Among the tested sterols, cholesteryl eicosapentaenoate and cholesteryl arachidonate exhibited IC50 values of 14.6 and 17.7 µg/mL for COX-1 and 17.3 and 20.8 µg/mL for COX-2, respectively. Cholesteryl palmitate and cholesteryl oleate showed moderate COX-1 and COX-2 enzyme inhibition at 25 µg/mL. Amino acids arginine, tyrosine, glutamic acid, tryptophan and asparagine also showed moderate COX-1 and COX-2 inhibition at the same concentration. Among the twelve new isolates from fractions that we did not investigate earlier, a novel uracil derivative petromyzonacil showed COX-1 and COX-2 inhibition at 25 µg/mL by 35 and 15%, respectively. Cholesterol esters tested at 25 µg/mL exhibited LPO inhibition between 38 and 82 percent. Amino acids cysteine, methionine, aspartic acid, threonine, tryptophan, histidine, glutamic acid, phenylalanine and tyrosine at 25 µg/mL showed LPO inhibition between 37 and 58% and petromyzonacil by 32%. These assay results indicate that consumption of sea lamprey offer health-benefits in addition to nutritional benefits.

Chemical Composition and Anti-Inflammatory and Antioxidant Activities of Extracts from Cultivated Morel Mushrooms, Species of Genus Morchella (Ascomycota).

Species of genus Morchella are high-value edible mushrooms. They are sought after by culinary experts due to their aroma, flavor, meaty texture, and health benefits. M. rufobrunnea, M. sextelata, and M. americana were chosen in this study and investigated for their medicinal quality by using in vitro anti-inflammatory and antioxidant assays. This sampling represents conditions by which morels are produced (cultivated indoors, cultivated outdoors, and collected from natural habitats, respectively) for commercial markets. Both aqueous and methanolic extracts of all three morel species showed identical chromatographic and bioassay profiles, independent of their phylogenetic position or production method. In an antioxidant assay, aqueous and methanolic extracts of these mushrooms at 100 µg/mL inhibited lipid peroxidation (LPO) by 59%-62% and 33%-36%, respectively. In an anti-inflammatory assay using cyclooxygenase enzymes (COX-1 and COX-2), aqueous and methanolic extracts at 100 µg/mL showed COX-1 enzyme inhibition by 53%-57% and 30%-32% and COX-2 enzyme inhibition by 38%-44% and 16%-17%, respectively. Chromatographic purification and spectroscopic characterization of M. rufobrunnea extracts afforded five sugars (compounds 1-5), seven organic acids (compounds 6-13), three flavonoids (compounds 14-16), triglycerides, free fatty acids, and three sterols (compounds 17-19). This is the first report of COX-1 and COX-2 enzymes and LPO inhibitory activities of pure isolates (S)-morelid (compound 6), glutamic acid (compound 9), and brassicasterol (compound 19). This study also showed inhibitions of COX-1 (by 84%, 33%, and 37%), COX-2 (by 47%, 11%, and 22%), and LPO (by 74%, 48%, and 35%), respectively, at 25 µg/mL.

Nitrogenous compounds characterized in the deterrent skin extract of migratory adult sea lamprey from the Great Lakes region.

The sea lamprey (Petromzons marinus) is a devastating invasive species that represents a significant impediment to restoration of the Laurentian Great Lakes. There is substantial interest in developing environmentally benign control strategies for sea lamprey, and many other aquatic invasive species, that employ the manipulation of semiochemical information (pheromones and chemical cues) to guide the movements of invaders into control opportunities (e.g. traps, locations for safe pesticide application, etc.). A necessary precursor to the use of semiochemicals in conservation activities is the identification of the chemical constituents that compose the odors. Here, we characterize the major nitrogenous substances from the water-soluble fraction of a skin extract that contains the sea lamprey alarm cue, a powerful repellent that has proven effective in guiding the movements of migrating sea lamprey in rivers. Nitrogenous compounds are suspected components of fish alarm cues as the olfactory sensory neurons that mediate alarm responses transduce amino acids and related compounds. A laboratory assay confirmed the behavioral activity contained in the alarm cue resides in the water-soluble fraction of the skin extract. This water-soluble fraction consisted primarily of creatine (70%), heterocyclic nitrogenous compounds (4.3%) and free amino acids (18.4%), respectively. Among the free amino acids characterized in our study, essential amino acids constituted 13% of the water-soluble fraction. Free amino acids isolated from the water-soluble fraction composed of arginine, phenylalanine, threonine, and asparagine 3.9, 2.7, 2.6 and 2.4% of the water-soluble fraction, respectively. We discuss the implications of these findings for understanding the nature and use of the sea lamprey alarm cue in conservation activities.

Extraction and isolation of important bioactive compounds from the fruit of Physalis ixocarpa.

The current study investigates pharmaceutically important bioactive compounds in the fruits of Physalis ixocarpa. Two different extractions methods were used to study its effect on percent extract yield, recovery of bioactive compounds and antioxidant activity of the extracts. The data indicated that Soxhlet extraction had high efficiency of recovery than maceration method for extracting compounds; percent extract yield and antioxidant activity of the extracts. In maceration, the percent extract yield was found to be in order of water >methanol >ethyl acetate whereas in Soxhlet extraction, it was in order of methanol >water >ethyl acetate. Ethyl acetate extract produced by Soxhlet extraction showed strong antioxidant activity of 59.7% (250ppm) as compared to other extracts. Analysis of ethyl acetate extract showed the presence of Triglyceride. GC-MS study of triglyceride revealed the presence of trilinoleinic acid (9,12-Octadecdienoic acid), tripalmitin (hexadecanoic acid) and trioleinic acid (9-Octa decenoic acid). Four impure and three pure compounds were isolated from crude methanol extract of the fruit. The structure of pure compounds were identified by NMR and characterized as sugar, glucose and fructose.

Criteria for Postoperative Mechanical Ventilation After Thymectomy in Patients With Myasthenia Gravis: A Retrospective Analysis.

OBJECTIVE: To determine the criteria for postoperative mechanical ventilation after thymectomy in patients with Myasthenia Gravis. DESIGN: Retrospective study. SETTING: Teritiary care centre. PARTICIPANTS: 77 Myasthenia gravis patients operated for thymectomy were studied. INTERVENTIONS: After obtaining clearance from Institutional ethics committee, medical records of 77 patients with MG, who were operated for thymectomy between January 2005 and December 2015 were reviewed in a retrospective manner. Perioperative variables collected from the patient records were demographic data, duration of the disease, Osserman and Genkin classification, Anti-acetylcholine antibody (AChR) positivity, preoperative daily dose of drug, history of preoperative myasthenic crisis, preoperative vital capacity, technique of anesthesia, drugs used for anesthesia, perioperative complications, and duration of postoperative mechanical ventilation. The patients were divided into two groups, group I and group II consisting of those who required postoperative ventilation for < 300 minutes and > 300 minutes, respectively. The determinants of prolonged postoperative ventilation were studied. MEASUREMENTS AND MAIN RESULTS: The requirement of mechanical ventilation was higher in patients with higher Osserman's grade of myasthenia gravis. Duration of the disease had no effect on the duration of mechanical ventilation in myasthenic patients post thymectomy (p = 0.89). The patients with a preoperative history of myasthenic crisis had a requirement for prolonged mechanical ventilation (p=0.03). Patients with preoperative vital capacity < 2.9 litres and preoperative CT scan showing thymoma had a requirement for prolonged mechanical ventilation with p values < 0.001 and 0.035, respectively. Patients who showed positivity for anti-acetylcholine antibodies had a prolonged mechanical ventilation (p=0.026). Preoperative dose of pyridostigmine and the choice of continuation or discontinuation of antcholinesterases on the day of surgery had no influence on the duration of mechanical ventilation (p value of 0.19 and 0.36 respectively). Epidural analgesia intra and postoperatively significantly reduced the requirement of mechanical ventilation (p=0.006). CONCLUSION: The predictors of postoperative ventilation in myasthenic patients undergoing thymectomy as per our study are: 1. Grade of myasthenia; 2. History of preoperative myasthenic crisis; 3. Anti-acetylcholine antibodies positivity; 4. Presence of thymoma; and 5. a vital capacity < 2.9 litres. Use of thoracic epidural as a part of combined anesthetic technique helps to reduce the need of mechanical ventilation in these patients.

Lipid Peroxidation and Cyclooxygenase Enzyme Inhibitory Compounds from Prangos haussknechtii.

Purification of extracts from Prangos haussknechtii Bioss afforded prenylated coumarins 1 and 2, monoterpenoid 3, amino acid derivative 4, and seven known compounds. Spectroscopic methods permitted establishment of the structures and relative configuration of these compounds. The pure isolates were tested for antioxidant and anti-inflammatory activities using lipid peroxidation (LPO), 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide (MTT), and cyclooxygenase (COX-1 and -2) enzyme inhibitory assays. Compounds 1-4 inhibited LPO with IC50 values between 43 and 114 µM and reduced MTT to formazan blue between 48 and 128 µM. In anti-inflammatory assays using cyclooxygenase enzymes, COX-1 and -2, these compounds showed inhibition, with IC50 values ranging from 34 to 56 µM.

Aflatoxin levels in sunflower seeds and cakes collected from micro- and small-scale sunflower oil processors in Tanzania.

Aflatoxin, a mycotoxin found commonly in maize and peanuts worldwide, is associated with liver cancer, acute toxicosis, and growth impairment in humans and animals. In Tanzania, sunflower seeds are a source of snacks, cooking oil, and animal feed. These seeds are a potential source of aflatoxin contamination. However, reports on aflatoxin contamination in sunflower seeds and cakes are scarce. The objective of the current study was to determine total aflatoxin concentrations in sunflower seeds and cakes from small-scale oil processors across Tanzania. Samples of sunflower seeds (n = 90) and cakes (n = 92) were collected across two years, and analyzed for total aflatoxin concentrations using a direct competitive enzyme-linked immunosorbent assay (ELISA). For seed samples collected June-August 2014, the highest aflatoxin concentrations were from Dodoma (1.7-280.6 ng/g), Singida (1.4-261.8 ng/g), and Babati-Manyara (1.8-162.0 ng/g). The highest concentrations for cakes were from Mbeya (2.8-97.7 ng/g), Dodoma (1.9-88.2 ng/g), and Singida (2.0-34.3 ng/g). For seed samples collected August-October 2015, the highest concentrations were from Morogoro (2.8-662.7 ng/g), Singida (1.6-217.6 ng/g) and Mbeya (1.4-174.2 ng/g). The highest concentrations for cakes were from Morogoro (2.7-536.0 ng/g), Dodoma (1.4-598.4 ng/g) and Singida (3.2-52.8 ng/g). In summary, humans and animals are potentially at high risk of exposure to aflatoxins through sunflower seeds and cakes from micro-scale millers in Tanzania; and location influences risk.

Chemical Characterization of Lipophilic Constituents in the Skin of Migratory Adult Sea Lamprey from the Great Lakes Region.

The sea lamprey (Petromzons marinus) is an invasive ectoparasite of large-bodied fishes that adversely affects the fishing industry and ecology of the Laurentian Great Lakes. Lipid content in the whole sea lamprey and muscles, liver and kidney of metamorphosing larval stages has been reported. Similarly, the fatty acid profile of the rope tissues of sexually-mature male sea lampreys has also been reported. The average body weight of a sub-adult migratory sea lamprey is 250 g, which includes 14.4% skin (36 g). Our preliminary extraction data of an adult sea lamprey skin revealed that it contained approximately 8.5% of lipophilic compounds. Lamprey skin is home to a naturally aversive compound (an alarm cue) that is being developed into a repellent for use in pest management. As part of an ongoing investigation to identify the chemical structure of the sea lamprey alarm cue, we extracted the skin with water and methanol, respectively. The methanolic extract (1.55%) contained exclusively lipophilic compounds and did not include the alarm cue. We chemically characterized all compounds present in the methanolic extract as cholesterol esters (CE), tri- and di-glycerides (TG and DG), cholesterol, free fatty acids (FFA) and minor amounts of plasticizers. The free fatty acids fraction was composed of saturated (41.8%), monounsaturated (40.7%) and polyunsaturated (17.4%) fatty acids, respectively. The plasticizers characterized were phthalate and benzoate and found to be 0.95 mg and 2.54 mg, respectively, per adult sea lamprey skin. This is the first report of the chemical characterization of all the lipophilic constituents in the skin of sub-adult migratory sea lamprey. The CEs isolated and characterized from sea lamprey skin are also for the first time.

Sesquiterpenoid Lactones in Tanacetum huronense Inhibit Human Glioblastoma Cell Proliferation.

Tanacetum huronense (Lake Huron tansy), which is native to the upper Midwest region of USA and Canada, was examined for the presence of anticancer compounds using an in vitro human tumor cell proliferation inhibition assay, with glioblastoma derived cell line U-87 MG. Bioassay-directed purification of the ethyl acetate extract of the aerial portion of this plant identified six active sesquiterpenoid lactones (1-6). Among these, compounds 5 and 6 are new structural analogs. One of the most abundant isolates, tanacin (4), exhibited the greatest inhibition with an IC50 value of 4.5 µg/mL.

New antiinflammatory sucrose esters in the natural sticky coating of tomatillo (Physalis philadelphica), an important culinary fruit.

Tomatillo is a popular culinary fruit. The sticky material on its surface, consumed as part of the fruit, has never been investigated. Chemical characterization of sticky material on tomatillo fruits yielded five new sucrose esters, as confirmed by spectroscopic methods. The solvent extract of the sticky material from the whole fresh fruit and pure isolates showed antiinflammatory activity as confirmed by in vitro cyclooxygenase enzymes inhibitory assays. Five sucrose esters isolated at 100 µg/mL (153.8, 138.8, 136.2, 141.6 and 138.8 µM, respectively) inhibited cyclooxygenase-1 and -2 enzymes by 50%. The cyclooxygenase enzyme inhibitory activity of extract and isolates at 100 µg/mL was similar to non-steroidal antiinflammatory drugs aspirin, ibuprofen and naproxen, used as positive controls in the assay at 108, 12 and 15 µg/mL (600, 60 and 60 µM), respectively.

Phenanthrenes in Chinese Yam Peel Exhibit Antiinflammatory Activity, as Shown by Strong in Vitro Cyclooxygenase Enzyme Inhibition.

Chinese yam (Dioscorea opposita), peeled or whole, is a popular food item that is considered to be healthy. Often, the yam is peeled before cooking. However, it is also consumed with peel. Therefore, in this study, the peel of this yam was extracted sequentially with n-hexane, ethyl acetate and methanol, and studied for its health-benefits, using in vitro bioassays. Bioactivity-guided purifications of extracts of the peel afforded phenanthrenes (1-4), as characterized- by spectroscopic methods. Phenanthrene I is a novel analogue. The extracts and isolates were tested for antiinflammatory activity using cyclooxygenase enzyme (COX- I and -2) inhibitory assays. All phenanthrenes isolated from the yam peel showed higher inhibition of COX enzymes than the over-the-counter nonsteroidal anti-inflammatory drugs (NSAIDs) aspirin, ibuprofen and naproxen.

Antioxidant and Antiinflammatory Compounds in Nutmeg (Myristicafragrans) Pericarp as Determined by in vitro Assays.

Nutmeg, Myristicafragrans, is known for its culinary and medicinal values. The nutmeg pericarp, abundant during the production of the seed, is also used in food and beverage preparations. In this study, the pericarp of M. fragrans was evaluated for its bioactive components using in vitro antioxidant and antiinflammatory assays. The hexane, ethyl acetate and methanolic extracts inhibited lipid peroxidation (LPO) by 82.5, 70.1 and 73.2%, and cyclooxygenase enzymes COX-1 by 44, 44 and 42% and COX-2 by 47, 41 and 36%, respectively, at 100 microg/mL. The bioassay-guided purifications of extracts yielded 20 compounds belonged to neolignans (0.13%), phenylpropanoids (0.28%), phenolic aldehyde (0.35%), triterpenoids (0.06%), triglycerides (0.20%), sugars (10.2%) and steroids (0.49%). Pure isolates 1-5 inhibited LPO by 70-99% and 3-12 inhibited COX-1 and -2 enzymes by 37-49%. This is the first report on the bioassay-guided characterization of constituents in nutmeg pericarp. Our results support the medicinal claims of nutmeg pericarp.

Evaluation of coriander spice as a functional food by using in vitro bioassays.

Coriander leaves and seeds are widely used as a condiment and spice. The use of roasted coriander seeds in food and beverage is very common. In this study, we investigated raw and roasted coriander seeds for their functional food quality using antioxidant, anti-inflammatory and human tumour cell proliferation inhibitory assays. The hexane and methanolic extracts of raw and roasted coriander seeds showed identical chromatographic and bioassay profiles. Chromatographic purification of the roasted seed extracts afforded tripetroselinin as the predominant component. Other isolates were petroselinic acid, 1,3-dipetroselinin, 2-C-methyl-d-erythritol, 2-C-methyl-d-erythritol 4-O-ß-d-glucopyranoside and linalool. Hexane and methanolic extracts of both raw and roasted seeds and pure isolates from them showed comparable antioxidant and anti-inflammatory activities to the positive controls used in the assays, and inhibited the growth of human tumour cells AGS (gastric carcinoma), DU-145 and LNCaP (prostate carcinoma), HCT-116 (colon carcinoma), MCF-7 (breast carcinoma) and NCI-H460 (lung carcinoma) by 4-34%, respectively.

Blood-brain barrier permeability of bioactive withanamides present in Withania somnifera fruit extract.

The neuroprotective effect of Withania somnifera L. Dunal fruit extract, in rodent models, is known. Withanamides, the primary active constituents in W.somnifera fruit extract exhibited neuroprotective effects against ß-amyloid-induced cytotoxicity in neuronal cell culture studies. Therefore, we investigated the blood-brain barrier permeability of withanamides in W.somnifera fruit extract in mice using HPLC coupled with high resolution quadrupole time of flight mass spectrometer (Q-TOF/MS) detection. Mice were administered with 250 mg/kg of W.somnifera extract by intraperitoneal injection, and the blood and brain samples analyzed by Q-TOF/MS detection. Four major withanamides were detected in brain and blood of mice administered with W.somnifera extract. The results suggested that the withanamides crossed the blood-brain barrier. These results may help to develop W.somnifera fruit extract as a preventive or therapeutic botanical drug for stress-induced neurological disorders.

Major constituents of Boswellia carteri resin exhibit cyclooxygenase enzyme inhibition and antiproliferative activity.

Aromatic gum from Boswellia carteri (olibanum oleogum) has long been used in Egyptian traditional medicine. Cyclooxygenase-1 (COX-1) enzyme inhibitory assay guided purification of the extracts of this resin resulted in five bioactive compounds, 3alpha-O-acetyl-8,24-dien-tirucallic acid (1), verticilla-4(20),7,11-triene (2), cembrene A (3), incensole acetate (4), and incensole (5). The pure isolates were investigated for their inhibitory effects on COX-1 and -2 enzymes and human tumor cell lines Hep-G2, MCF-7 and RAW 264.7. Compounds 1-5 inhibited COX-2 enzyme by 39.0, 32.7, 60.0, 46.3, and 49.8%, respectively. Furthermore, compound 2 showed an inhibitory concentration of 50% (IC50) at 9 microg/mL against Hep-G2 tumor cell line. This is the first report of COX-1 and -2 enzyme and tumor cell proliferation inhibitory effects of compounds 1 and 2.