Anti-MRSA Constituents from Ruta chalepensis (Rutaceae) Grown in Iraq, and In Silico Studies on Two of Most Active Compounds, Chalepensin and 6-Hydroxy-rutin 3',7-Dimethyl ether.

Ruta chalepensis L. (Rutaceae), a perennial herb with wild and cultivated habitats, is well known for its traditional uses as an anti-inflammatory, analgesic, antipyretic agent, and in the treatment of rheumatism, nerve diseases, neuralgia, dropsy, convulsions and mental disorders. The antimicrobial activities of the crude extracts from the fruits, leaves, stem and roots of R. chalepensis were initially evaluated against two Gram-positive and two Gram-negative bacterial strains and a strain of the fungus Candida albicans. Phytochemical investigation afforded 19 compounds, including alkaloids, coumarins, flavonoid glycosides, a cinnamic acid derivative and a long-chain alkane. These compounds were tested against a panel of methicillin-resistant Staphylococcus aureus (MRSA) strains, i.e., ATCC 25923, SA-1199B, XU212, MRSA-274819 and EMRSA-15. The MIC values of the active compounds, chalepin (9), chalepensin (10), rutamarin (11), rutin 3'-methyl ether (14), rutin 7,4'-dimethyl ether (15), 6-hydroxy-rutin 3',7-dimethyl ether (16) and arborinine (18) were in the range of 32-128 µg/mL against the tested MRSA strains. Compounds 10 and 16 were the most active compounds from R. chalepensis, and were active against four out of six tested MRSA strains, and in silico studies were performed on these compounds. The anti-MRSA activity of compound 16 was comparable to that of the positive control norfloxacin (MICs 32 vs 16 µg/mL, respectively) against the MRSA strain XU212, which is a Kuwaiti hospital isolate that possesses the TetK tetracycline efflux pump. This is the first report on the anti-MRSA property of compounds isolated from R. chalepensis and relevant in silico studies on the most active compounds.

Naturally Occurring Calanolides: Occurrence, Biosynthesis, and Pharmacological Properties Including Therapeutic Potential.

Calanolides are tetracyclic 4-substituted dipyranocoumarins. Calanolide A, isolated from the leaves and twigs of Calophyllum lanigerum var. austrocoriaceum (Whitmore) P. F. Stevens, is the first member of this group of compounds with anti-HIV-1 activity mediated by reverse transcriptase inhibition. Calanolides are classified pharmacologically as non-nucleoside reverse transcriptase inhibitors (NNRTI). There are at least 15 naturally occurring calanolides distributed mainly within the genus Calophyllum, but some of them are also present in the genus Clausena. Besides significant anti-HIV properties, which have been exploited towards potential development of new NNRTIs for anti-HIV therapy, calanolides have also been found to possess anticancer, antimicrobial and antiparasitic potential. This review article provides a comprehensive update on all aspects of naturally occurring calanolides, including their chemistry, natural occurrence, biosynthesis, pharmacological and toxicological aspects including mechanism of action and structure activity relationships, pharmacokinetics, therapeutic potentials and available patents.

"Malancha" [Alternanthera philoxeroides (Mart.) Griseb.]: A Potential Therapeutic Option against Viral Diseases.

Alternanthera philoxeroides (Mart.) Griseb., commonly known as "Alligator weed" in English, and "Malancha" in Bengali, is a leafy vegetable from the family Amaranthaceae A. L. de Jussieu. This species is native to China, particularly to the provinces around the Yangtze River, other Far East and South-East Asian countries, and countries from other continents (e.g., South America). This plant also grows in certain areas in Australia, New Zealand, and the USA. While in Bangladesh the leaves of this plant are consumed as a vegetable, in China, this plant has been used widely as a traditional remedy for the treatment of various viral diseases (e.g., measles, influenza, and haemorrhagic fever). Flavonoids and saponins are the two largest groups of phytochemicals produced by this plant, and the antiviral property of this plant and its compounds has been studied extensively. This review article reviews all published literature on this plant and critically appraises its phytochemical profile linking to biomolecular interactions and therapeutic potential, particularly, against viral diseases.

Isolation and Characterization of Antibacterial Compounds from Aspergillus fumigatus: An Endophytic Fungus from a Mangrove Plant of the Sundarbans.

The Sundarbans, a UNESCO world heritage site, is one of the largest mangrove forests in one stretch. Mangrove plants from this forest are little studied for their endophytic fungi. In this study, we isolated fourteen endophytic fungi from the plants Ceriops decandra and Avicennia officinalis collected from the Sundarbans. Five of them were identified as Aspergillus sp. and one as Penicillium sp. by macroscopic and microscopic observation. Antibacterial activity of the crude extracts obtained from these endophytes was determined against Staphylococcus aureus, Micrococcus luteus, Escherichia coli, and Pseudomonas aeruginosa using resazurin-based microtiter assay. The isolated endophytes showed varying degrees of antibacterial activity with MICs ranging between 5 and 0.078 mg/mL. Molecular identification of the most active endophyte revealed its identity as Aspergillus fumigatus obtained from the leaves of C. decandra. Acute toxicity study of the ethyl acetate extract of A. fumigatus in mice revealed no mortality even at the highest dose of 2000 mg/kg bodyweight, though some opposing results are found in the subacute toxicity study. The extract was subjected to silica gel and Sephadex column chromatography resulting in the isolation of three pure compounds. LC-MS analysis of these pure compounds revealed their identity as fumigaclavine C, azaspirofuran B, and fraxetin. This is the first report of fraxetin from A. fumigatus. All three identified compounds were previously reported for their antibacterial activity against different strains of both Gram-positive and Gram-negative bacteria. Therefore, the observed antibacterial activity of the ethyl acetate (EtOAc) extract of A. fumigatus could be due to the presence of these compounds. These results support the notion of investigating fungal endophytes from the Sundarbans for new antimicrobial compounds.

Pesticidal Activity of Sundarban Mangrove Plant Extracts against Sitophilus Pests and Identification of Active Constituents Using LC-MS.

Plants act as a rich source of novel natural pesticides. In the backdrop of the recent revival of interest in developing plant-based insecticides, this study was carried out to investigate the pesticidal activity of Sundarban mangrove plants. A total of nine different plant parts from five plants, namely, Aegiceras corniculatum, Excoecaria agallocha, Heritiera fomes, Xylocarpus moluccensis, and Xylocarpus granatum, were extracted with methanol and tested for insecticidal activity against two common stored product pests Sitophilus oryzae and Sitophilus zeamais using direct contact feeding deterrent wafer disc method. Three bark extracts from A. corniculatum, E. agallocha, and H. fomes showed potent and statistically significant insecticidal activity against both S. oryzae and S. zeamais pests (80-100% mortality). All the active bark extracts were further fractionated using C-18 solid-phase extraction (SPE) columns and tested for their insecticidal activity against S. oryzae pest to identify the active fraction. Only the SPE4 fraction (100% MeOH) from all the three active plants showed the activity against S. oryzae pest with a lethal concentration 50% (LC50) value of 0.5, 1.0, and 1.5 mg/disc for A. corniculatum, E. agallocha, and H. fomes, respectively. The active fraction of A. corniculatum was further profiled for identification of active compounds using LC-ESI-MS and identified (along with some unknown peaks) two previously reported compounds at m/z 625.17630 (isorhamnetin 3-O-rutinoside) and 422.25346 (paspaline) as major constituents. Insecticidal activities of these plants are reported in this study for the first time and would be useful in promoting research aiming for the development of new biopesticides from mangrove plants.

Cicca acida L.: phytochemistry and pharmacological studies.

OBJECTIVES: Cicca acida L., is reported with traditional and pharmacological uses, and a good number of pure compounds have been isolated from its different parts. But published information is sporadic and fragmentary in nature. Therefore, it is imperative to have a comprehensive account of all of its medicinal potentialities with critical analysis. In this review, the traditional reports, phytochemical and pharmacology studies associated with Cicca acida have been compiled to figure out the net possibilities for its application in modern medicine. KEY FINDINGS: Careful scrutiny reveals that the plant possesses a huge range of medicinal properties, but published report analysis suggests that the plant is effectively used as antibacterial, hepatoprotective, anticonceptive and antidiabetic purposes. The published papers revealed the bioactivity of only 04 compounds. This indicates that a good number of isolated major compounds of this plant are yet to be pharmacologically investigated. CONCLUSION: Intensive study of Cicca acida showed that despite of its plentiful isolated molecules, the effort leading to final product stage seems to be less. Therefore, the plant and its compounds need concentrated effort towards establishment of its therapeutic potentialities.

Antidiabetic plants used among the ethnic communities of Unakoti district of Tripura, India.

ETHNOPHARMACOLOGICAL RELEVANCE: A large group of ethnic communities living in Unakoti district of Tripura, India is still dependent on traditional herbal remedies for treatment of diabetes. Valuable information collected from these communities in the present investigation is important in maintaining their indigenous knowledge of folklore medicine. METHODS: Systematic and extensive field surveys were conducted during 2011-2013 among the ethnic inhabitants of Unokati district, Tripura, India covering all the seasons to collect information on their traditional herbal medication system for treatment of diabetes. Obtained data were analysed through fidelity level (FL), use value (UV) and relative frequency of citation (RFC) to authenticate the uniqueness of the species being used for diabetes treatment. RESULTS: In this current study a total of 39 medicinal plant species belonging to 37 genera and 28 families were presented, used by the traditional healers of Unakoti district, Tripura, India for diabetes treatment. FL, UV and RFC values of collected plants for the selected study area ranges between 06% and 100%, 0.07% and 2.64% and 0.02% and 0.51% respectively. Out of 39 collected plants, 11, 5 and 3 plant species have showed significant (<50%) FL, UV and RFC values respectively. CONCLUSION: Like many other ethnic communities of the world, inhabitants of Unakoti district depend on a traditional medication system to treat diabetes. Documented floras are locally available and need proper further pharmacological validation to endorse their traditional use in a modern health care system. This will help in the development of effective herbal antidiabetic medicines in near future.

Male contraceptive efficacy of Ricinus communis L. extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Ricinus communis L. (Rc), of Euphorbiaceae family is a widespread plant in tropical regions and it is used in traditional medicines as an antifertility agent in India and different parts of the world. AIM OF THE STUDY: The aim of the present study is to revalidate the ethnobotanical knowledge by evaluating the activity of only crude stem bark extracts of Rc. In this study, effects of extracts on male contraceptive efficacy were experimented in vitro with human sperm sample. The work is based on primordial and contemporary therapeutic uses of this plant. MATERIALS AND METHODS: In this study, dose of petroleum ether extract, ethyl acetate extract, acetone extract and lyophilised aqueous extract of Rc were added to fresh human semen in 1:1 volumetric ratio. As the aqueous extract showed a promising result in 1:1 ratio, therefore, the Hypo-osmotic swelling test (HOS), Nuclear chromatin decondensation test (NCD) and Acrosomal status and function test (AFT) were also carried out with the aqueous extract of Rc. RESULTS: The sperm immobilisation effects of the extract appeared immediately in a dose-dependent manner when the samples were treated with four different extracts of this plant. At a concentration of 100mg/mL, 100% (p<0.001 and p<0.05) sperms lost their progressive motility. At a concentration of 300 mg/mL, 100% (p<0.001 and p<0.05) became immotile when treated with aqueous extract. There was 88% (p<0.001 and p<0.05) morphological deformities in sperm sample due the effect of aqueous extract when they were tested for HOS and 91% (p<0.05) sperms behaved against NCD as compared to control group. Also there was a distinct decline (p<0.05) in AFT with increase in dosage concentration. CONCLUSION: The findings of the study revealed that aqueous stem bark extract of the plant showed dose dependent loss of sperm motility by influencing the morphological deformation, blockage in nuclear envelope and distinct declination in acrosomal status of spermatozoa. This research, thus, opens up scope for future exploration of bark of the plant as commercial source of new male contraceptive.