Synthesis and In Vitro Antileishmanial Efficacy of Novel Ethylene Glycol Analogues of Benzothiadiazine-1,1-dioxide.

Leishmaniasis is a vector-borne, parasitic disease affecting millions of people and animals worldwide. Current therapeutic options have proven to be ineffective in both treating the disease and preventing its spread. As a result, new drugs must be developed to effectively combat this disease.

Hematoxylin, an Alternative Substrate of Tyrosinase.

Mushroom tyrosinase from (TYR) is often used during the development of tyrosinase inhibitors for medicinal and cosmetic purposes. In the search for novel tyrosinase inhibitors, this study identified hematoxylin as an alternative substrate for TYR. The interaction of hematoxylin with TYR was investigated through spectrophotometric and chromatographic analyses.

The effect of environmental stressors on the anticancer potential of aqueous extracts and fractions.

Some species have been shown to have pharmacological properties such as activity against cancer, and it is also used as a traditional herbal medicine in many rural parts of the world. The (3-(4,5-dimethylthiazol-2-Yl)-2,5-diphenyltetrazolium bromide assay was used as a screening tool to determine the approximate cell viability inhibitory concentrations of methanol and aqueous crude extracts of spp. The extracts were screened using small-cell lung cancer (H69V), hepatocellular carcinoma (HepG2/C3A) and non-cancerous kidney cells (Vero) cell lines.

Development of a HPLC Method for Analysis of a Combination of Clofazimine, Isoniazid, Pyrazinamide, and Rifampicin Incorporated into a Dermal Self-Double-Emulsifying Drug Delivery System.

We describe the development and validation of a new high performance liquid chromatography (HPLC) method for analysis of a combination of the first-line anti-tubercular drugs isoniazid, pyrazinamide, and rifampicin together with clofazimine. This is a unique challenge since clofazimine and rifampicin are relatively highly lipophilic drugs, whereas isoniazid and pyrazinamide are considerably more hydrophilic. Thus, clear separation of peaks and quantification of four individual drugs can present difficulties during the development of an analytical method.

2-Aroyl quinazolinone: Synthesis and in vitro anti-parasitic activity.

Trypanosomes and Leishmania are parasitic protozoans that affect millions of people globally. Herein we report the synthesis of 2-aroyl quinazolinones and their antiprotozoal efficacy against Trypanosoma brucei, Trypanosoma brucei rhodesiense, Trypanosoma cruzi, and Leishmania infantum. These compounds were counter-screened against a human cell line for cytotoxicity.

Influence of Drought and Heat Stress on Mineral Content, Antioxidant Activity and Bioactive Compound Accumulation in Four African Species.

Drought and heat stress is known to influence the accumulation of mineral content, antioxidant activity, phenolics, flavonoids and other bioactive compounds in many tolerant leafy vegetables. plants can tolerate adverse weather conditions, especially drought and heat. Therefore, evaluating the influence of drought and heat stress on commercially and medically important crop species like is important to grow the crop for optimal nutritional and medicinal properties.

In vitro and ex vivo experimental models for evaluation of intranasal systemic drug delivery as well as direct nose-to-brain drug delivery.

The intranasal route of administration provides a noninvasive method to deliver drugs into the systemic circulation and/or directly into the brain. Direct nose-to-brain drug delivery offers the possibility to treat central nervous system diseases more effectively, as it can evade the blood-brain barrier. In vitro and ex vivo intranasal models provide a means to investigate physiological and pharmaceutical factors that could play a role in drug delivery across the nasal epithelium as well as to determine the mechanisms involved in drug absorption from the nose.

Geographical and seasonal phytochemical variation of Artemisia afra Jacq. ex Willd.

Introduction: Artemisia afra Jacq. ex. Willd.

Validating a sensitive LCMS method for the quantitation of artemisinin in Artemisia spp. including material used in retracted clinical trials.

Two recent clinical trials reported that Artemisia afra contained significant amounts of the bioactive compound artemisinin. We suspected sample contamination and therefore obtained the A. afra material for testing.

6-Nitro-1-benzylquinolones exhibiting specific antitubercular activity.

In this study, we synthesized novel nitro quinolone-based compounds and tested them in vitro against a panel of Gram-positive and Gram-negative pathogens including Mycobacterium tuberculosis (MTB), Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumonia, Staphylococcus aureus, and Escherichia coli for antibacterial activities and also against HeLa cells for overt cytotoxicity. Compound 8e was identified as a non-toxic, potent hit with selective activity (MIC  ˂ 0.24 µm) against MTB.

Artemisia afra, a controversial herbal remedy or a treasure trove of new drugs?

Ethnoparmacological Relevance: Artemisia afra is one of the most widely used herbal remedies in South Africa. This highly aromatic shrub is used to treat various disorders including coughs, colds, influenza, and malaria. Due to the long tradition of use and popularity of A.

Anti-inflammatory activity of cinnamon (C. zeylanicum and C. cassia) extracts - identification of E-cinnamaldehyde and o-methoxy cinnamaldehyde as the most potent bioactive compounds.

Chronic inflammation is a contributing factor in many age-related diseases. In a previous study, we have shown that Sri Lankan cinnamon (C. zeylanicum) was one of the most potent anti-inflammatory foods out of 115 foods tested.

Effect of acute stresses on zebra fish (Danio rerio) metabolome measured by NMR-based metabolomics.

We applied an acute stress model to zebra fish in order to measure the changes in the metabolome due to biological stress. This was done by submitting the fish to fifteen minutes of acute confinement (netting) stress, and then five minutes for the open field and light/dark field tests. A polar extract of the zebra fish was then subjected to (1)H nuclear magnetic spectroscopy.

Phytochemistry of the carnivorous sundew genus Drosera (Droseraceae) - future perspectives and ethnopharmacological relevance.

Species of the carnivorous genus Drosera L. have long been a source of valuable natural products. The various phytochemicals characteristic of these species, particularly 1,4-naphthoquinones and flavonoids, have contributed to the diverse utilization of sundews in traditional medicine systems worldwide.

The complexity of medicinal plants: the traditional Artemisia annua formulation, current status and future perspectives.

Ethnopharmacological Relevance: Artemisia annua has a long tradition of use for the treatment of intermittent fevers which we now relate to malarial infections. The active principle artemisinin has been isolated from Artemisia annua and today forms the backbone of the global fight against malaria. The traditionally prepared Artemisia annua formulation is however still being used on a global scale for the treatment of malaria, and it is claimed that its action is superior to the single purified drug.

Developmental effects of cannabinoids on zebrafish larvae.

Cannabinoids are natural or synthetic compounds related chemically to (-)-(6aR,10aR)-6,6,9-trimethyl-3-pentyl-6a,7,8,10a-tetrahydro-6H-benzo[c]chromen-1-ol (Δ(9)-THC), the principle psychotropic constituent of the hemp plant, Cannabis sativa L. Here we examine the effects of the cannabinoids Δ(9)-THC, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo [1,2,3-de]-1,4-benzoxazin-6-yl]-1-napthalenylmethanone and 2-[(1R,2R,5R)-5-hydroxy-2-(3-hydroxypropyl) cyclohexyl]-5-(2-methyloctan-2-yl)phenol, and the cannabinoid antagonist (AM 251). Exposures were either acute (1-12-h exposure at 108 hours of postfertilization [hpf]) or chronic (96-h exposure starting at 24 hpf).

The use of bio-guided fractionation to explore the use of leftover biomass in Dutch flower bulb production as allelochemicals against weeds.

A major problem in flower bulb cultivation is weed control. Synthetic herbicides are mainly used, although they cause a range of problems, and integrated weed control through application of naturally occurring allelochemicals would be highly desirable. Flower bulb production creates large amounts of leftover biomass.

Is artemisinin the only antiplasmodial compound in the Artemisia annua tea infusion? An in vitro study.

In our ongoing investigation into Artemisia annua for the treatment of malaria, we decided to study the possibility that synergism might enhance the efficacy of artemisinin. Our main objective was to test tea infusions and nonpolar extracts prepared from different A. annua varieties against Plasmodium falciparum in vitro in order to determine if synergism will increase the effectiveness of artemisinin in the samples as compared to pure artemisinin.

Coproduction and ecological significance of naphthoquinones in carnivorous sundews (Drosera).

While the 1,4-naphthoquinone derivatives 7-methyljuglone (1) and plumbagin (2) possess a diverse and well documented array of biological activities, relatively little remains known about the functional significance of these compounds in planta and, in particular, their possible relation to carnivorous syndromes. In addition, the chemotaxonomic distribution of naphthoquinones (NQs) amongst species of Drosera L. is of phytopharmaceutical interest.

Ethnopharmacology in overdrive: the remarkable anti-HIV activity of Artemisia annua.

Ethnopharmacological Relevance: Artemisia annua contains the well-known antimalarial compound artemisinin, which forms the backbone of the global malaria treatment regime. In African countries a tea infusion prepared from Artemisia annua has been used for the treatment of malaria only for the past 10-20 years. Several informal claims in Africa exist that the Artemisia annua tea infusions are also able to inhibit HIV.

Renewable energy from Cyanobacteria: energy production optimization by metabolic pathway engineering.

The need to develop and improve sustainable energy resources is of eminent importance due to the finite nature of our fossil fuels. This review paper deals with a third generation renewable energy resource which does not compete with our food resources, cyanobacteria. We discuss the current state of the art in developing different types of bioenergy (ethanol, biodiesel, hydrogen, etc.

The content of artemisinin in the Artemisia annua tea infusion.

The traditional use of the medicinal plant Artemisia annua for the treatment of malaria entails the preparation of a tea infusion. In the scientific literature there have been some discrepancies on the quantity of the active principle, artemisinin, in the tea infusion. Due to these discrepancies, we decided to quantify artemisinin in tea infusions prepared according to different methods.

Comparative quantitative analysis of artemisinin by chromatography and qNMR.

Introduction: Since the discovery of artemisinin in the 1970s, many techniques based on diverse chromatography techniques have been developed to detect and quantify this important antiplasmodial compound. The accurate quantification of this compound in the Artemisia annua plant material is mainly needed for breeding purposes in order to cultivate higher yielding varieties. It is also important for the quality control of herbal preparations containing A.

Cannabinoid receptor 1 binding activity and quantitative analysis of Cannabis sativa L. smoke and vapor.

Cannabis sativa L. (cannabis) extracts, vapor produced by the Volcano vaporizer and smoke made from burning cannabis joints were analyzed by GC-flame ionization detecter (FID), GC-MS and HPLC. Three different medicinal cannabis varieties were investigated Bedrocan, Bedrobinol and Bediol.

Metabolomic investigation of the ethnopharmacological use of Artemisia afra with NMR spectroscopy and multivariate data analysis.

Ethnopharmacological Relevance: Artemisia afra has been used as an infusion to treat malaria throughout the southern parts of Africa, in much the same way as the antimalarial plant Artemisia annua in China. The antiplasmodial activity of purified components from an apolar fraction of Artemisia afra has been shown in the past. No data on the efficacy of the tea infusion prepared from Artemisia afra are however available.