Water soluble fractions of rose-scented geranium (Pelargonium species) essential oil.

The essential oil of rose-scented geranium (Pelargonium species, family: Geraniaceae) obtained through steam or water plus steam distillation of shoot biomass is extensively used in the fragrance industry and in aromatherapy. During distillation, a part of the essential oil becomes dissolved in the distillation water (hydrosol) and is lost as this hydrosol is discarded. In this investigation, hydrosol was shaken for 30 min with hexane (10:1 proportion) and the hexane was distilled to yield 'secondary' or 'recovered' essential oil. The chemical composition of secondary oil was compared with that of 'primary' oil (obtained directly by distilling shoot biomass of the crop). Primary oil accounted for 93.0% and secondary oil 7.0% of the total oil yield (100.2 ml from 100 kg green shoot biomass). Fifty-two compounds making up 95.0-98.5% of the primary and the secondary oils were characterized through gas chromatography (GC) and gas chromatography-mass spectroscopy (GC--MS). Primary oil was richer in hydrocarbons (8.5-9.4%), citronellyl formate (6.2-7.5%), geranyl formate (4.1-4.7%), citronellyl propionate (1.0-1.2%), alpha-selinene (1.8-2.2%), citronellyl butyrate (1.4-1.7%), 10-epi-gamma-eudesmol (4.9-5.5%) and geranyl tiglate (1.8-2.1%). Recovered oil was richer in organoleptically important oxygenated compounds (88.9-93.9%), commercial rhodinol fraction (74.3-81.2%), sabinene (0.4-6.2%), cis-linool oxide (furanoid) (0.7-1.2%), linalool (14.7-19.6%), alpha-terpineol (3.3-4.8%) and geraniol (21.3-38.4%). Blending of recovered oil with primary oil is recommended to enhance the olfactory value of the primary oil of rose-scented geranium. Distillation water stripped of essential oil through hexane extraction can be recycled for distilling the next batch of rose-scented geranium.

Alternative medicine: herbal drugs and their critical appraisal--part II.

The availability of herbal products as "over-the-counter" drugs and their increasing usage in the US and Canada have caused concern at the US FDA, since these products are not currently monitored for their safety, efficacy and quality. Reliable information on these aspects of the products is not available. Most of the clinical trials carried out to date have been lacking in scientific design, data collection and interpretation, and systematic toxicological evaluation. A critical review of the existing data on three of the widely used herbs and their products is presented. Of the three herbs, garlic and ginger, through both experimental and clinical data, as well as their liberal consumption by man over millennia, appear to be very safe for therapeutic use. However, further and large-scale, well-designed clinical investigations are needed to establish their efficacy before they can enter the mainstream drug market of North America. It is hoped that this review will equip the physicians and interested biomedical scientists with a comprehensive summary of the total information available to date on the herbs described.

Alternative medicine: herbal drugs and their critical appraisal--Part I.

Among alternative therapeutic approaches that have shown global popularity during the past decades, herbal medicine stands out as a major concern in the countries where allopathic medicine prevails. The sales of herbal products as health care adjuvants in these countries have increased exponentially. Lack of quality control, commercial profiteering and exploitation leading to adulterations, lack of proper knowledge about the herbs and their contents that may exhibit drug-drug interactions and other adverse side-effects, and inappropriate usage of the herbal products have become a cause for concern in the health care professions, particularly in the United States. This review provides an incisive description of the known chemical, pharmacological, clinical and toxicological profiles of four of the most widely used herbal products.

Drug discovery: past, present and future.

New drug discovery from early on involved a trial-and-error approach on naturally derived materials and substances until the end of the nineteenth century. The first half of the twentieth century witnessed systematic pharmacological evaluations of both natural and synthetic compounds. However, most new drugs until the 1970s were discovered by serendipity. With the exponential development of molecular biology on one hand and computer technology on the other, it became possible from 1980 onwards to place drug discovery on a rational basis. Cloning of genes has led to the development of methodologies for specific receptor-directed and enzyme-directed drug discoveries. Advances in recombinant DNA and transgenic technologies have enabled the production of human hormonal and other endogenous biomolecules as new drugs. As we understand more about the co-ordinating and regulating powers of the cerebral cortex during the next century, especially of the frontal lobe, man may be able to use bio-feedback training to voluntarily regulate the release of neurotransmitters, hormones, and other molecules involved in the regulation of various physiological processes in health as well as in disease.

The essential oil composition of Angelica glauca roots.

The essential oil of Angelica glauca roots was analysed by GC and GC/MS. Sixty-eight constituents representing about 92% of the oil were identified. The main constituents of the oil are beta-phellandrene (15.29%) and (Z)-ligustilide (31.55%).

Drug molecules of marine origin.

Somewhat accelerated developments in the chemistry and pharmacology of marine molecules during the eighties are a clear indication of the biomedical potential of marine organisms for the twenty-first century. Unfortunately, the overall effort toward the field is still insignificant. Both industry and governments are spending only a token share of R&D funds in pursuit of pharmacologically active substances from the sea. A critical appraisal of the literature reveals the existence of fascinating molecules with unusual and potent activities. The challenge of harnessing the clinical potential of these molecules is clearly evident. It is only awaiting the awakening of the academic, industrial, and federal researchers and resources. Only a concerted and a massive effort can shorten the time between now and the first clinical drug from the sea.

A method for the isolation of the caribbean palytoxin (C-PTX) from the coelenterate (zooanthid) Palythoa caribaeorum.

Chromatographically pure toxin was isolated from the zooanthid Palythoa caribaeorum. Toxin isolation was achieved by extraction with 50% ethanol from the homogenized specimens, gel filtration on Sephadex G-50 and ion exchange chromatography on QAE- and SP-Sephadex. Final purification was obtained by gel filtration on Biogel P-6. The LD50 tested on the shore crab Carcinus maenas was 62.5 ng/kg.

Compounds from the sea with actions on the cardiovascular and central nervous systems.

Recent efforts at probing into the oceans have produced evidence that marine invertebrates such as gorgonians and sponges offer a rich reserve of pharmacologically interesting molecules. Our investigations indicate that it is possible to obtain novel compounds both structurally and pharmacologically. For example, autonomium from a sponge is a dual adrenergic combined with cholinergic molecule, with a structure that may be considered a hybrid between a catecholamine and choline. Various terpenoids and indole derivatives from marine organisms have been found to possess activities on the central nervous system. Several peptides from sea anemones are cardiotonic and have initiated a new concept of chemical structure believed to be associated with cardiac activity. A number of closely related halogenated cyclic ethers are good inhibitors of drug metabolism. Thus, there seems little doubt that the sea warrants an extensive chemical and pharmacological examination.

Modification of drug-induced catatonia and tremors by quapazine in rats and mice.

Administration of perphenazine, tremorine, nicotine and harmine induced Parkinson-like symptoms in rats and mice. The efficacy of quipazine, a serotonin agonist, in antagonizing these drug-induced Parkinsonian symptoms was assessed. Combinations of this drug with other antiparkinsonian agents such as scopolamine, diphenhydramine and amantadine were also studied in the manifestation of Parkinson-like symptoms in the animal models. The results indicate that quipazine, a central serotonergic agent, counteracted some of the drug-induced symptoms of pseudoparkinsonism in laboratory animals. Cholinergic, dopaminergic and histaminergic receptors play an important role in the manifestations of these symptoms.

Modification by levo-propranolol of tremors induced by harmine in mice.

It has been recently reported that the levo isomer of propranolol possesses anti-serotonin properties in animals. Since harmine-induced behavioural changes in mice are reported to be mediated through central serotonergic receptors, an attempt was made to test whether 1-propranolol would also modify harmine-induced responses by virtue of its anti-serotonergic or anti-adrenergic property. The results indicated that l- and dl-propranolol inhibited central serotonin receptor mediated responses to harmine in mice, a finding that is analogous to other recent observations.

New drug metabolism inhibitor of marine origin.

Dactylyne, an acetylenic dibromochloro ether, was isolated from the sea hare Aplysia dactylomela and characterized pharmacologically. It had no direct effect on the cardiovascular, respiratory, and central nervous systems of mice, rats, and guinea pigs. However, a 25-mg/kg ip dose of dactylyne prolonged pentobarbital sleep time in mice by more than 10 hr. This potentiation was subsequently determined to be due to the inhibition of pentobarbital metabolism by dactylyne since the elimination half-life of pentobarbital in the dactylyne-treated mice increased several folds. Dactylyne was nontoxic up to 200 mg/kg iv. The unique structure, high potency, and relatively nontoxic nature of dactylyne make it an interesting pharmacological substance of marine origin.