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devance

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Everything posted by devance

  1. devance

    Hoodia patent look

    http://164.195.100.11/netacgi/nph-Parser?S...oodia&RS=hoodia This is a patent that comes up with the chemical strutures and more info./ It is known from International Patent Publication No. WO 98/46243 that extracts of certain plants of the genus Trichocaulon or Hoodia possess appetite suppressant properties. This document also discloses certain specific compounds which possess appetite suppressant activity. Among these is the compound 3-O-[-.beta.-D-thevetopyranosyl-(1.fwdarw.4)-.beta.-D-cymaropyranosyl-(1.f wdarw. 4)-.beta.-D-cymaropyranosyl]-12.beta.-O-tigloyloxy-14-hydroxy-14.beta.-pre gn-5-en-20-one; the structural formula of this compound is given as formula (1) in WO 98/46243. We have found that this compound is effective in reducing the secretion of gastric acid; accordingly, the compound finds application in the present invention. Derivatives of this compound are also effective in the present invention; such derivatives have the general formula ##STR2## In case you want to do your own patent search which is free go to http://www.uspto.gov/ and use hoodia as rhe search term. There are only two patents that come up.
  2. devance

    Hoodia patent look

    Dear Torsten, the rest of the patent is simply filled with vague scietific references and has no information as to chemical structure, extraction, or anything else of any worth what so ever. It doesn't even make reference to a glucose simulator molecule.
  3. devance

    free spyware for windows 95

    I have had norton firewall with eveything turned off but scripting but I found there was still an attack. After looking at what I hadn't turned off I found After blocking the {stealth port/ IP fragmented packet handling} stting by using the Norton interface works fine; there is probably a more direct way to do so as most security programs simply interface with the explorer browser. Anyway thought I would mention it as spyware removal may not do the job as there is a website infection redirector program that appeared a week ago as mentioned on world news. I think I ran into it a few days earlier than that which prompted me to look at my firewall settings which I thought was well blocking. One can always tell if there a trojun running program as it is memory draining and not compatible, as in freezing up a computer.
  4. devance

    myostatin

    I found a homemade enteric coating. Naturally only food quality ingredients should be used. It consists of using shellac flakes dissolved in ethanol to coat a gel capsule with a sprayer. The shellac will dissolve in the alkaline conditions of the lower intestine but not the acidic stomach. Shellac apparently is not only a fine wood varnish but is non toxic as it is produced by a insect for cocooning and is used on supermarket fruit along with wax as well as the pharmacuetical industry. Anyway this opens the door for extracting and using types of brown seaweed for various Sulfated polysaccharides of brown seaweed But perhaps an enema would serve even better.
  5. devance

    myostatin

    http://www.adn.com/24hour/healthscience/st...p-8836512c.html This is a interesting news item that relates to ethnobotany because of the brown seaweed called Cystoseira canariensis which some claim is effective if used with a enteric coating to reduce myostatin. Is there a homemade enteric coating? If so the medical benefits of the many types of brown seaweed,can be cautiously explored by the armchair herbal explorer. http://66.102.7.104/search?q=cache:NGTTCOq...&hl=en&ie=UTF-8
  6. devance

    myostatin

    The first link isn't working and I can not change it because of some type of problem in log in. So just go to google news for german superman baby for the news item.
  7. devance

    Asparagus pee

    I ate two pounds of fresh boiled asparagus long ago that permanently impressed me with the urine stench. But have never been able to reproduce the event when I have eaten fresh boiled asparagus and have always wondered about the biochemical dynamics.
  8. devance

    Seed Forming?

    I saw a interesting possible technique on the internet for getting seeds from difficult plants that are hard to seed. It simply consists of using pollen from whatever plant available to trigger a self pollination seed formation. I wonder If that works?
  9. devance

    Reagan's dead. good riddance

    All I smell is the smell of cooking steaks outside.
  10. devance

    Fun with spyware...

    I wouldn't be worried as my norton also detected three new adwares this week. So thats normal as I run my detection every week. Norton good.
  11. http://www.tropilab.com/black-cat.html one of these herbs works better than the other one although I can't remember which,NIRURI might be it. This is a interesting herb company that I actually used and recommend. Gallstone problems are typically shown by bags under the eyes, as a example Ashcroft who had his gallbladder recently removed surgically, a painful process. The herbal remedy is a muscle relaxer for the gallbladder, already patented by the ever alert pharmaceutical bioprospectors. But a more effective way is to increase citric acid intake which dissolves kidney and gallstone either by citric juices or by the pure chemical which can be added to buttermilk for enhancing flavor. Having been a lifetime sufferer who has found a nonsurgical alternative I am sure someone can benefit from the information of a condition which can be cured or advoided by eating alot of fruits that contain citric acid. [ 27. April 2004, 12:23: Message edited by: devance ]
  12. HOPS v2.0 Bryce 5 Some visual software programs for seeing and recognizing fractual forms which are mathematical builting bocks of the artistic forms of livings forms as in nature.
  13. devance

    fractals

    [sorry I derailed your topic. [/qb] I derailed my topic by not placing it in the Creativity section. But fractals are more than simple artistic expression, but a fundamental shaping of nature, such as weather, terrain shaping, and gene expression, which is not a LINEAR series of random mutations but actually an expression of fractal predestination expression.. You definitely can see fractals in nature easy but it does take sophisticated educational software like I have mentioned. I don't have a imagination and have to be shown. The bryce program is a world generater. Very easy to use to create 3D mountains, seas, clouds,ect. I am artistically challenged or perhaps I haven't found my art yet. Wish I had been musically gifted or intertested. [ 21. April 2004, 10:38: Message edited by: devance ]
  14. devance

    fractals

    Both are fractual generators. As such they can produce amazing effects. Hops is a small application with parameters. More of a screen saver, but interesting. Bryce5 is a 70$ program, but one can use plugins for such as KTP7.. No software is going to see art.
  15. devance

    busted

    Stainless steel tanker trucks? [ 11. February 2004, 04:22: Message edited by: devance ]
  16. devance

    Funniest thing you ever did see.

    Is your washroom breeding Bolsheviks? http://historyproject.ucdavis.edu/imageapp...&SlideNum=47.00
  17. This is a nice site to learn basic pharmacuetical skills, such a dosage, compounding, extraction, etc. Apparently for prospective students of pharmacy. http://pharmlabs.unc.edu/exercise_list.htm#pceutics
  18. devance

    origin of your name!

    Mine is based on my favorite science fiction author. Jack Vance is a highly anthropological writer who can describe the high and lows of human existence in one book.
  19. devance

    psychoactive orchids?

    Stelis sp. Orchidaceae http://www.montana.com/manu/plants.html Heres a web site of a researcher who went to South America in search of plants for headache cures. There are a number of new plants mentioned including. Kemishitsa, tentatively Stelis sp. Orchidaceae. Oscar very excitedly brought us this specimen one day after he found it on the trail. Apparently, it was the plant that his master used to help him attain status as a seripegari, or shaman. He reports that it is very powerful, and we began calling it "the hallucinogen that falls from the sky". If corroborated, it will be the first such claim for this, the largest plant family, with some 30,000 species list of plants http://www.montana.com/manu/paper.html amusing travelogue http://www.montana.com/manu/log.html
  20. devance

    sceletium

    7. A method according to any one of claims 4 to 6 wherein the serotonin-uptake inhibitor is (-)-mesembrine. United States Patent 6,288,104 Gericke , et al. September 11, 2001 Pharmaceutical compositions containing mesembrine and related compounds Abstract There is disclosed the use of mesembrine and related compounds (e.g. mesembranol, mesembranone) as scrotonin-uptake inhibitors, pharmaceutical compositions comprising such compounds or dry material or an extract of plants from the Mesembryanthemaceae family (e.g. Sceletium (Aizoaceae) tortuosum) containing a standardized content of said compounds, for use in the treatment of depressive states, psychological or psychiatric disorders with an anxiety component, alcohol and drug dependence, bulimia nervosa and obsessive-compulsive disorders. Also disclosed are new derivatives of mesembrine. Inventors: Gericke; Nigel Peter (Cape Town, ZA); Van Wyk; Ben-Erik (Johannesburg, ZA) Assignee: African Natural Health CC (Cape Town, ZA) Appl. No.: 194836Filed: March 22, 1999PCT Filed: June 3, 1997 PCT NO: PCT/GB97/01493 371 Date: March 22, 1999 102(e) Date: March 22, 1999 PCT PUB.NO.: WO97/46234PCT PUB. Date: December 11, 1997Foreign Application Priority Data Jun 04, 1996[ZA]06/4595 Current U.S. Class:514/421; 548/512 Intern'l Class: A61K 031/40Field of Search: 514/421 548/512 Foreign Patent Documents3604112A1Aug., 1987DE. 46-43538Dec., 1971JP. 46-43539Dec., 1971JP. Other References Taguchi et al., "Synthesis of Octahydroindole Derivatives," Tetrahedrom Letters, 55:5763-5766 (1968). Jeffs et al., "Total Syntheses of (.+-.)-Joubertinamine, and (.+-.)-N-Demethylmesembrenone," J. Org. Chem. 48:3861-3863 (1983). Capps et al., "Sceletium Alkaloids, Part 7..sup.1 Structure and Absolute Stereochemistry of (-)-Mesembrane and 3'-Methoxy-4'-O-methyljoubertiamine, Two Minor Bases from S. Namaquense L. Bolus: X-Ray Analysis of (-)-Mesembrane Hydrochloride Monohydrate," J. Chem. Soc. Perkins Trans. 8:1098-1104 (1977). Langlois et al., "Recherches Dans La Serie Des Aryl-3 Pyrrolidines-II, Syntheses de Produits Apparentes a la Mesembrine et a La Crinine," Tetrahedron 27:5641-5652 (1971). Taguchi et al., "Synthesis of Octhydroindole Derivatives," Chem. Pharm. Bull. 18:1008-1014 (1970). Kruger et al., "Minor Alkaloids from Sceletium Strictum L. Bol. The Structure of N-Demethylmesembrenol and N-Demthylmesembranol," Journal of the South African Chemical Institute XXIV:235-237 (1971). Jeffs et al., "Sceletium Alkaloids. VI. Minor Alkaloids of S. namaquense and S. strictum," J. Org. Chem. 39:2703-2710 (1974). Pfaffli et al., "Demethylierungen am Mesembrine," Helvetica Chimica Acta 56:347-355 (1973). Smith et al., "Psychoactive constituents of the genus Sceletium N.E.Br. and otehr Mesembryanthemaceae: a review," Journal of Ethnopharmacology 50:119-130 (1996). Hoshino et al., "Synthesis of Sceletium and Amaryllidaceae Alkaloids, (.+-.)-Mesembrine and (.+-.)-Dihydromaritidine, (.+-.)Epidihydromaritidine, (.+-.-Elwesine, and (.+-.)-Epielwesine.sup.1)," Chem. Pharm. Bull. 35:2734-2743 (1987). Primary Examiner: Jones; Dwayne C. Assistant Examiner: Delacroix-Muirheid; C. Attorney, Agent or Firm: Clark & Elbing LLP Claims What is claimed is: 1. A pharmaceutical composition in unit dosage form comprising a serotonin-uptake inhibitor having the formula I ##STR9## wherein the ring A is selected from the group consisting of: ##STR10## R.sub.1 and R.sub.2 are independently selected from H, OH, OCH.sub.3 and O(CH.sub.2).sub.n CH.sub.3 ; R.sub.3 is selected from H, CH.sub.3 and (CH.sub.2).sub.n CH.sub.3 ; n is an integer from 1 to 6; and Q.sub.1 and Q.sub.2 are independently selected from CH.sub.2, C.dbd.O and CHOH; in a dose of from 20 micrograms to 2 milligrams. 2. A pharmaceutical composition according to claim 1 comprising the serotonin-uptake inhibitor in a dose of from 50 micrograms to 500 micrograms. 3. A pharmaceutical composition according to claim 1 or 2 wherein the serotonin-uptake inhibitor is (-)-mesembrine. 4. A method of treating diseases that respond to treatment with a serotonin-uptake inhibitor comprising administering to a patient in need thereof an effective amount of a serotonin-uptake inhibitor having the formula I ##STR11## wherein the ring A is selected from the group consisting of: ##STR12## R.sub.1 and R.sub.2 are independently selected from H, OH, OCH.sub.3 and O(CH.sub.2).sub.n CH.sub.3 ; R.sub.3 is selected from H, CH.sub.3, and (CH.sub.2).sub.n CH.sub.3 ; n is an integer from 1 to 6; and Q.sub.1 and Q.sub.2 are independently selected from CH.sub.2, C.dbd.O and CHOH. 5. A method according to claim 4 wherein the scrotonin-uptake inhibitor is administered in a unit dose of from 20 micrograms to 2 milligrams. 6. A method according to claim 5 wherein the serotonin-uptake inhibitor is administered in a unit dose of from 50 micrograms to 500 micrograms. 8. A pharmaceutical composition comprising as an active ingredient plant material or an extract of a plant of the family Mesembryanthemaceae containing in each unit dose an amount of from 20 micrograms to 2 milligrams of a compound selected from the group consisting of mesembrine, mesembranol and mesembranone, or a mixture of two or more thereof. 9. A pharmaceutical composition according to claim 8 wherein each unit dose contains an amount of from 50 micrograms to 500 micrograms of the compound. 10. A method of treating a patient suffering from a disease, said method comprising administering to said patient a composition comprising a plant material or an extract of a plant of the family Mesembryanthemaceae containing in each unit dose an amount of from 20 micrograms to 2 milligrams of a compound selected from the group consisting of mesembrine, mesembranol and mesembranone, or a mixture of two or more thereof wherein said disease is selected from the group consisting of mild to moderate depression, psychological and psychiatric disorders where anxiety is present, major depressive episodes, alcohol and drug dependence, bulimia nervosa, and obsessive-compulsive disorders. 11. The method of claim 10 wherein each unit dose contains an amount of from 50 micrograms to 500 micrograms of the compound. Description BACKGROUND OF THE INVENTION This invention relates to the use of mesembrine and related compounds as serotonin-uptake inhibitors, to pharmaceutical compositions comprising as an active ingredient dry material or an extract of a plant of the family Mesembryanthemaceae, standardised as to its active content, and to new compounds. It is known that the naturally occurring alkaloid mesembrine is useful as a medicament having CNS-stimulating action (see JP71043539 to Tanabe Seiyaku Company Limited). It is also known that a plant and plant products known colloquially as "kougoed", "channa" or "kanna" in the Cape of South Africa, are used traditionally by some communities as inebriants, sedatives and to elevate mood. The plants called "kougoed", "channa" or "kanna" are all members of the family Mesembryanthemaceae, and contains varying amounts of (-)-mesembrine and related alkaloids. An article entitled Psychoactive constituents of the genus Sceletium N.E.Br. and other Mesembryanthemaceae: a review, by Smith et al, in Journal of Ethnopharmacology, 50 (1996), Pages 119 to 130, reviews the historical data recorded over 300 year period of the use of Sceletium plants in psychoactive preparations, describes techniques for the preparation and use of "kougoed" from plants of Sceletium and documents the subjective experiences of a number of contemporary users. The alkaloid distribution in Sceletium and other members of the family Mesembryanthemaceae are also considered. Chemical studies have indicated as many as nine alkaloids in Sceletium, which fall into three distinct structural categories. SUMMARY OF THE INVENTION According to a first aspect of the invention there is provided the use of a compound having the formula I ##STR1## wherein the ring A is selected from the group consisting of: ##STR2## R.sub.1 and R.sub.2 are independently selected from H, OH, OCH.sub.3 and O(CH.sub.2).sub.n CH.sub.3 ; R.sub.3 is selected from H, CH.sub.3 and (CH.sub.2).sub.n CH.sub.3 ; n is an integer from 1 to 6; and Q.sub.1 and Q.sub.2 are independently selected from CH.sub.2, C.dbd.O and CHOH; in the manufacture of a medicament for the treatment of diseases that respond to treatment with a serotonin-uptake inhibitor. In their role as serotonin-uptake inhibitors, these compounds may be used in the treatment of mild to moderate depression, psychological and psychiatric disorders where anxiety is present, major depressive episodes, ie single episode and recurrent depression with associated anxiety, in alcohol and drug dependence, in the treatment of bulimia nervosa, and in the treatment of obsessive-compulsive disorders. According to a second aspect of the invention there is provided a pharmaceutical composition in unit dosage form comprising a serotonin-uptake inhibitor having the formula I as set out above, in a dose of from 20 micrograms to 2 milligrams inclusive, preferably in a dose of from 50 micrograms to 500 micrograms inclusive, more preferably in a dose of from 100 micrograms to 300 micrograms inclusive. According to a third aspect of the invention there is provided a method of treating diseases that respond to treatment with a serotonin-uptake inhibitor comprising administering to a patient in need thereof an effective amount of a compound having the formula I as set out above. According to a fourth aspect of the invention there is provided a pharmaceutical composition comprising as an active ingredient plant material or an extract of a plant of family Mesembryanthemaceae, containing in each unit dose an amount of from 20 micrograms to 2 milligrams inclusive, preferably from 50 micrograms to 500 micrograms inclusive, more preferably from 100 micrograms to 300 micrograms inclusive, of a compound selected from the group consisting of mesembrine, mesembranol and mesembranone, or a mixture of two or more thereof. The plant of the family Mesembryanthemaceae is preferably a plant of the genus Sceletium, more preferably a plant of the species Sceletium tortuosum(L.) N.E. Br. The pharmaceutical composition of the invention is also useful in the treatment of mild to moderate depression, psychological and psychiatric disorders where anxiety is present, major depressive episodes, ie single episode and recurrent depression with associated anxiety, in alcohol and drug dependence, in the treatment of bulimia nervosa, and in the treatment of obsessive-compulsive disorders. According to a fifth aspect of the invention there is provided a compound having the formula I ##STR3## wherein the ring A is selected from the group consisting of: ##STR4## R.sub.1 and R.sub.2 are independently selected from H, OH, OCH.sub.3 and O(CH.sub.2).sub.n CH.sub.3; R.sub.3 is selected from H, CH.sub.3 and (CH.sub.2).sub.n CH.sub.3 ; n is an integer from 1 to 6; and Q.sub.1 and Q.sub.2 are independently selected from CH.sub.2, C.dbd.O and CHOH; with the provisos that: (1) when the ring A is ##STR5## R.sub.1 and R.sub.2 are OCH.sub.3, R.sub.3 is CH.sub.3, and Q.sub.1 is CH.sub.2, then Q.sub.2 is not C.dbd.O or CHOH; (2) when the ring A is ##STR6## R.sub.1 and R.sub.2 are OCH.sub.3 or R.sub.2 is OH and R.sub.2 is H, R.sub.3 is CH.sub.3, and Q.sub.1 is CH.sub.2, then Q.sub.2 is not C.dbd.O; and (3)when the ring A is ##STR7## R.sub.1 and R.sub.2 are OCH.sub.3, R.sub.3 is CH.sub.3, and Q.sub.1 is C.dbd.O, then Q.sub.2 is not C.dbd.O. BRIEF DESCRIPTION OF THE DRAWINGS FIG. 1 is a graph for a serotonin-uptake assay comparing (-)-mesembrine, identified by the code number 18532, as compared with the known serotonin-uptake inhibitor imipramine HCl; FIG. 2 is a graph for a serotonin-uptake assay of a whole plant extract of a plant from the family Mesembryanthemaceae, identified by the code number 18639, as well as some comparisons with the known serotonin-uptake inhibitor imipramine HCl; FIG. 3 is a graph for a serotonin-uptake assay for mesembranol, identified by the code number 18623, as well as some comparisons with the known serotonin-uptake inhibitor imipramine HCl; and FIG. 4 is a graph for a serotonin-uptake assay for mesembranone, identified by the code number 18622, as well as some comparisons with the known serotonin-uptake inhibitor imipramine HCl. DESCRIPTION OF EMBODIMENTS The first aspect of the invention is the use of compounds of the formula I as serotonin-uptake inhibitors. The compounds of the formula I may be utilised in either of their isomeric forms i.e as the (-)isomer or as the (+)isomer, or as the racemic mixture of the two isomers. The preferred form is the (-)isomer. The compounds of the formula I may be divided into three sub groups: ##STR8## In the compounds of the formula I, preferably R.sub.1 and R.sub.2 are both OCH.sub.3, R.sub.3 is CH.sub.3, Q.sub.1 is CH.sub.2 and Q.sub.2 is selected from C.dbd.O and CHOH. The preferred compound of formula I.1, is that in which R.sub.1 and R.sub.2 are OCH.sub.3, R.sub.3 is CH.sub.3, Q.sub.1 is CH.sub.2 and Q.sub.2 is C.dbd.O. This is the compound known as mesembrine. The structure of mesembrine, also known as 3a-(3,4-dimethoxyphenyl)-octahydro-1-methyl-6H-indol-6-one, has been reported by Popelak et al., Naturwiss.47,156 (1960), and the configuration by P W Jeffs et al., J.Am.Chem.Soc.91,3831 (1969). Mesembrine is preferably used as its (-)-isomer i.e (-)-mesembrine. Another preferred compound of the formula I.1 is that in which R.sub.1 and R.sub.2 are OCH.sub.3, R.sub.3 is CH.sub.3, Q.sub.1 is CH.sub.2 and Q.sub.2 is CHOH, i.e the compound known as mesembranol. Preferred compounds of the formula I.2 are those in which R.sub.1 is selected from OH and OCH.sub.3, R.sub.2 is selected from H and OCH.sub.3, R.sub.3 is CH.sub.3, Q.sub.1 is CH.sub.2 and Q.sub.2 is C.dbd.O. A particularly preferred compound of the formula I.2 is that in which R.sub.1 and R.sub.2 are OCH.sub.3, R.sub.3 is CH.sub.3, Q.sub.1 is CH.sub.2 and Q.sub.2 is C=O, i.e the compound known as mesembranone. The preferred compounds of the formula I.3 are those in which R.sub.1 and R.sub.2 are OCH.sub.3, R.sub.3 is CH.sub.3, and Q.sub.1 and Q.sub.2 are C.dbd.O. As stated above, it has been known that mesembrine is useful as a medicament having CNS stimulating action. However, it has now been discovered that the compounds of the invention have a totally different mode of action as serotonin-uptake inhibitors, and in specified doses act as anti-depressants, minor tranquilizers and anxiolytics. Thus, the compounds of the formula I are useful in the treatment of diseases selected from the group consisting of mild to moderate depression, psychological and psychiatric disorders where anxiety is present, major depressive episodes, alcohol and drug dependence, bulimia nervosa, and obsessive-compulsive disorders. The second aspect of the invention is a pharmaceutical composition in unit dosage form comprising a serotonin-uptake inhibitor having the formula I as set out above, in a unit dose of from 20 micrograms to 2 milligrams inclusive, preferably from 50 micrograms to 500 micrograms inclusive, more preferably from 100 micrograms to 300 micrograms inclusive, preferably as a once-a-day administration. The compounds of the formula I may be formulated in any suitable form for pharmaceutical administration, such as for example aqueous-ethanolic tinctures, tablets, capsules, nasal sprays and skin-patches. The formulations may be designed to be taken orally sublingually, intra-nasally and transdermally. The third aspect of the invention is a method of treating diseases that respond to treatment with a serotonin-uptake inhibitor comprising administering to a patient in need thereof an effective amount of a compound having the formula I, in the doses described above. The preferred compound for the pharmaceutical composition and for the method as described above is (-)-mesembrine, with mesembranol and mesembranone also being preferred. The fourth aspect of the invention is a pharmaceutical composition comprising as an active ingredient plant material or an extract of a plant of the family Mesembryanthemaceae, more preferably a plant of the genus Sceletium, most preferably a plant of the species Sceletium tortuosum(L.) N.E. Br., containing in each unit dose an amount of 20 micrograms to 2 milligrams inclusive, preferably from 50 micrograms to 500 micrograms inclusive, more preferably from 100 micrograms to 300 micrograms inclusive, of a compound selected from the group consisting of mesembrine, mesembranol and mesembranone, or a mixture of two or more thereof. In other words, this pharmaceutical composition, while derived from a natural plant material, must contain a known and specified content of the active component or components. The pharmaceutical composition of the invention may comprise fresh or dry portions of the plant, ground to a pulp or powder, or an aqueous or alcoholic extract of the plant, all containing amounts of mesembrine, mesembranol or mesembranone. Again, the pharmaceutical composition may be formulated for example as an aqueous-ethanolic tincture, tablet, capsule, nasal spray or skin-patch for oral, sublingual, intra-nasal and transdermal application. Methods for the extraction of (-)-mesembrine from a plant material containing the product, and methods of analysis thereof are set out below. 1 EXTRACTION METHODS Dry material: Material (or alcoholic extracts) are air-dried at maximum 40.degree. C. before analysis. Yield figures for mesembrine are variable but are typically between 15 and 35 mg per gram dry leaves (mean value around 15 mg per gram dry weight). Finely ground material (pestle and mortar) is mixed with 15 ml 0.05 M H.sub.2 SO.sub.4 and left standing at room temperature for 20 minutes. After filtration, the remaining solids are re-extracted with 5 ml 0.05 M H.sub.2 SO.sub.4. The aqueous phases are combined, applied to glass columns with a coarse grade celite (24 g), alkalinized with ammonia (4 ml) and extracted (1X) with 100 ml CH.sub.2 Cl.sub.2. The CH.sub.2 Cl.sub.2 extracts are dried with anhydrous Na.sub.2 SO.sub.4 and the solvent evaporated under reduced pressure to leave the alkaloid as a pale brown oil. The alkaloids can also be extracted with hot or cold water instead of H.sub.2 SO.sub.4, or with methanol, ethanol, acetonitrile, chloroform or dichloromethane. Fresh material: The leaf sap of fresh leaves (or alcoholic extracts) can be studied directly, or the alkaloids may be directly extracted in hot or cold water, ethanol, ethanol/acetonitrile, chloroform or dichloromethane or any other suitable solvent. For HPLC or GC, the sample has to be filtered (eg 0.45 .mu.m filter) in order to protect the columns from impurities. Yield figures for mesembrine are variable, but are typically between 0.8 and 6.5 mg per ml leaf sap (mean value around 3.3 mg per ml). 2 METHODS OF ANALYSIS 2.1 Thin-layer Chromatography This method can be used only for rough screening purposes, as there is a poor separation between mesembrine alkaloids with a 4.5 double bond (such as mesembrenone) and those without (such as mesembrine). For routine screening, the following system is suitable (Rf of mesembrine=0.6): Merck 60 F254 silica gel plates (0.25 mm layer thickness) developed in CHCl.sub.3 :cyclohexane:Et.sub.2 NH (4:5:1). The plates are dried at 100.degree. C. for 3 minutes, studied under UV254 and UV365 and then sprayed with iodoplatinate or dragendorff spray reagents. 2.2 Gas Chromatography (GC) Extracts are dissolved in minimum MeOH and studied by comparative GC and GC-MS. Authentic mesembrine should be used as external standard to quantify the alkaloid content. A Routine analyses for large numbers of samples (fast system): DB-1 fused silica capillary column (30 m.times.0.25 mm internal diameter; He as carrier gas at 4 ml min.sup.-1 ; column temperature 200.degree. C. to 300.degree. C. at 100 min.sup.-1, 15 minute isotherm; injector 230.degree. C.; FID (Flame Ionization Detector) detection 300.degree. C.; split ratio 30:1; injection volume 1 .mu.l ). B High resolution analyses (selected samples, slow): DB-1 fused silica capillary column (30 m.times.0.25 mm internal diameter; He as carrier gas at 4 ml min.sup.-1 ; column temperature 150.degree. to 320.degree. C. at 60 min.sup.-1 15 minute isotherm; injector 230.degree. C.; PND (Phosphorus-Nitrogen Detector) detection 300.degree. C.; split ratio 30:1; injection volume 1 .mu.l). C For GC-MS: Typical system such as DB-1 fused silica capillary column (30 m.times.0.32 mm internal diameter; He as carrier gas; column temperature 150.degree. to 300.degree. C. at 60 min.sup.-1, split ratio 20:1; injection volume 1 .mu.l). 2.3 High Performance Liquid Chromatography (HPLC) A phenomenex IB-Sil column is used (C18 reverse phase, 5 .mu.m particle size, 250 mm.times.4.6 mm internal diameter, flow rate 1 ml per minute, 20 .mu.l sample loop). An isocratic solvent system comprising 30% A in B (A=1% triethylamine in water; B=60% acetonitrile). Total run time is 10 minutes. Detection by diode array detector, using two channels (A set at 280.+-.30 nm, B set at 292.+-.10 nm). Results expressed in mg mesembrine per ml leaf sap (calculated from detector response, mean value of channels A and . For concentrations below 0.05 mg per ml, channel A is more accurate (lower detection limit of ca. 0.01 mg per ml leaf sap). The method depends on a calibration curve which was calculated using five different concentration levels of pure mesembrine, using the System Gold (Beckman) software package. For yield figures see `fresh material extraction`. 3 IDENTIFICATION OF MESEMBRINE BY MASS SPECTROMETRY AND 1H NMR SPECTROSCOPY In the two populations of Sceletium tortuosum studied, mesembrine occurs in leaves as virtually the only compound (small but negligible amounts of mesembrenone and mesembrenol may sometimes be present). The alkaloid was isolated from the leaves using the methods described above and fully identified by mass spectrometry (relative structure) and 1H NMR spectroscopy (absolute configuration). The optical rotation was measured, which confirmed that the natural product is the (-)-form. Mesembranol and mesembranone may be extracted from suitable plant material, analysed and identified as set out above for mesembrine. Derivatives of mesembrine, mesembranol and mesembranone, within the group of compounds of formula I, may be prepared from these starting compounds by methods known in the art. Higher order alkyl ethers of mesembrine, mesembranone or mesembranol may be prepared by acidolytic cleavage of the methoxy methyl groups (for example using anhydrous hydrogen fluoride) which gives the corresponding hydroxyl compound (R.sub.1.2.dbd.OH) followed by alkylation using the appropriate alkyl halide (for example CH.sub.3 (CH.sub.2).sub.n Br). The hydroxyl compounds above may be reduced to the corresponding benzyl compound (R.sub.1.2.dbd.H) by catalytic hydrogenation (for example over palladium). Mesembranol may be prepared from mesembrine by catalytic hydrogenation (for example over palladium). Compounds of formula I.3 may be prepared from the appropriate mesembrine derivatives described above by dehydrogenation with mecuric acetate. Compounds of formulas I.2 and I.3 may be prepared from mesembrine by oxidation using selenium dioxide (SeO.sub.2) in tertiary butanol with subsequent purification of the desired positional isomer. The isolated pure compound (-)-mesembrine was screened for biological activity by the National Institute of Mental Health in the United States of America, through a contract with Novascreen, a division of Oceanix Biosciences Corporation. As illustrated in FIG. 1, in comparison to the tricyclic anti-depressant imipramine HCl, (-)-mesembrine was found to be a highly potent serotonin-uptake inhibitor with an IC50 in nano-molar concentrations. This testing of (-)-mesembrine also gave the following results set out in Table 1, and below. TABLE 1 Percent Inhibition (Average: N = 2) Receptor Concentration 5,0E1 GABA B -0,6% Serotonin-uptake 96,5% The inhibitory constant (Ki) of (-)-mesembrine, with reference to imipramine HCl was found to be Ki=3.6E-8. In addition, the whole plant extract of Sceletium N.E.Br., mesembranol and mesembranone were screened for biological activity by the National Institute of Mental Health in the United States of America through the contract with Novascreen. The results of these assays are illustrated in FIGS. 2 to 4. These assays show that the whole plant extract, as well as mesembranol and mesembranone are highly potent serotonin-uptake inhibitors. Various in vitro studies of the effects of the compounds of the invention were carried out in adult volunteers as follows: Study 1. N=3 Healthy Adult Volunteers, All Health Professionals Sep. 13, 1996. A single dose of standardised preparation of dried whole plant, standardised to contain 400 micrograms of mesembrine was taken sublingually. Rapid onset of action (10-15 minutes) noted by all. Anxiolytic effect noted by all. Sustained elevation of mood noted by all. Duration of anxiolytic action ranged from five hours to eight hours. Study 2. N=2 Healthy Adult Volunteers, All Health Professionals Sep. 21, 1996. A single 200 microgram dose of pure (-)-mesembrine dissolved in 1 ml of 60% ethanol was taken sublingually. Rapid onset of action (7 and 12 minutes, respectively) noted by both. Anxiolytic effect noted by both. Sustained elevation of mood noted by both (for approximately eight hours and eleven hours respectively) Duration of anxiolytic action ranged from five hours to eight hours. Study 3. N=2 Adult Volunteers, Both Self-confessed Alcoholics and Polysubstance Abusers Sep. 21, 1996. A single 5 ml dose of a whole-plant aqueous-ethanolic extract containing 100 micrograms of mesembrine per ml of extract (60% ethanol) was administered orally (total dose of mesembrine 500 micrograms). Rapid onset of action (15-20 minutes) noted by both. Anxiolytic effect noted by both. Neither volunteer imbibed alcohol or used any illicit or other drug for a twenty-four hour period following the administration of the single dose. Examples of pharmaceutical compositions of the invention will now be given. EXAMPLE 1 A liquid composition comprises a 60% ethanol/water solvent containing about 200 .mu.g/ml of (-)-mesembrine. A typical dose of the liquid composition is from 1 ml to 5 ml inclusive daily. EXAMPLE 2 A sublingual tablet contains a spray-dried 30% aqueous-ethanolic extract of Sceletium tortuosum, containing 200 micrograms of (-)-mesembrine, and conventional pharmaceutical excipients. EXAMPLE 3 An oral tablet contains 200 micrograms of pure (-)-mesembrine, and conventional pharmaceutical excipients. * * * * *
  21. devance

    sceletium

    The oxyalic acid in it causes the problems. Microwaving the fresh plant crushed material on low does dry it and get rid of oxyalic acid in a gaseous form but causes the fresh plant: crushed material; to electrically discharge, in a starting electrical display and also burn it, as in charcoaling it, which is not desirable. Another way is to dry it in a food, forced air-fan, dehydrator. The home gerky making type. Gets rid of the rather caustic chemical at a low temperature after a couple of days if the fresh matrial is squished to make it more dehydratable. . Another way is to use baking soda on the dried material. This eliminates the acrid biting acid chemical which gets rid of the acrid taste. Seems to change the biochemical experience into a more sedative, sleep indusive type. For smoking or snuffing, drying the wet material is necessary after baking soda treatment is necessary.
  22. devance

    Study shows pot OK.

    An analysis of research studies with long-term, recreational users of marijuana has failed to reveal a substantial, systematic effect on the neurocognitive functioning of users. According to researchers at the University of California, San Diego (UCSD) School of Medicine, the only deleterious side effect found was a minimal malfunction in the domains of learning and forgetting. http://www.sciencedaily.com/releases/2003/...30630112652.htm
  23. devance

    saving amazonian rainforests

    http://www.alternet.org/issues/index.html?...?IssueAreaID=18 this is a good site. I been studying the problem and it has levels of complexity that I am just starting to appreciate. They are complex because they aren't apparent, deliberately obscured.
  24. http://www.alternativescience.com/no_brainer.htm I can't seem to edit my above post so I'll just add a post. It would have been added to. This is your brain on There is this college mathematics student who has no brain and is supposedly functioning because of the above hypothesis. On the other hand he might have his brain at home getting high and using the above hypothess to send his body to college. The student in question was academically bright, had a reported IQ of 126 and was expected to graduate. When he was examined by CAT-scan, however, Lorber discovered that he had virtually no brain at all. Instead of two hemispheres filling the cranial cavity, some 4.5 centimetres deep, the student had less than 1 millimetre of cerebral tissue covering the top of his spinal column. They don't mention if he can get stoned which would bring up other questions if he could.
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