Basic Treatment: Establish a patent airway. Suction if necessary. Encourage patient to take deep breaths. Watch for signs of respiratory insufficiency and assist ventilations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with normal saline during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 ml/kg up to 200 ml of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . /Irritating materials/
Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in respiratory arrest. Early intubation at the first sign of upper airway obstruction may be necessary. Positive pressure ventilation techniques with a bag valve mask device may be beneficial. Monitor cardiac rhythm and treat arrhythmias if necessary ... . Start an IV with D5W /SRP: "To keep open", minimal flow rate/. Use lactated Ringer's if signs of hypovolemia are present. Watch for signs of fluid overload. Consider drug therapy for pulmonary edema ... . Treat seizures with diazepam (Valium) ... Use proparacaine hydrochloride to assist eye irrigation ... . /Irritating materials/
/HUMAN EXPOSURE STUDIES/ Skin: From the plant Schefflera arboricola, which has been reported to cause allergic contact dermatitis, ... the elicitor of allergic contact dermatitis /was isolated and determined to be/ falcarinol, heptadeca-1,9(Z)-diene-4,6-diyne-3-ol. Three polyacetylenes closely related to falcarinol, namely falcarindiol, falcarinone and dehydrofalcarinone were tested simultaneously. Falcarinol, but not falcarindiol, falcarinone and dehydrofalcarinone, elicited allergic contact dermatitis in a 38-year-old female plant-nursery worker.
/HUMAN EXPOSURE STUDIES/ Experimental and chemical investigations revealed that common ivy (Hedera helix susp. helix) contains 3 compounds which are powerful irritants and moderate sensitizers. Only 2 of these constituents, falcarinol and didehydrofalcarinol, are present in the plant during the whole year. Besides Panax ginseng and Schefflera arboricola, this is the third species of the Araliaceae in which these polyacetylenic sensitizers have been found. Falcarinol and didehydrofalcarinol also occur in Hedera helix subsp. canariensis. 4 patients have been patch tested. Even in low concentrations (0.03%), the main allergen falcarinol elicited strong reactions in all of them. One of the authors became sensitized during the investigations.
Differential Effects of Falcarinol and Related Aliphatic C17-Polyacetylenes on Intestinal Cell Proliferation
摘要：
Quantitative major polyacetylenes of carrots (falcarinol and falcarindiol) and American ginseng roots (falcarinol and panaxydol) were isolated and tested in human intestinal epithelial cells of normal (FHs 74 Int.) and cancer (Caco-2) origin. A hormesis effect was seen for all isolated polyacetylenes when added to Caco-2 cells in concentrations ranging from 1 ng/mL to 20 mu g/mL. The relative inhibitory potency was falcarinol > panaxydol > falcarindiol. No hormesis effect was observed when adding the polyacetylenes to FHs 74 Int. cells. Instead, an inhibitory growth response was observed above 1 mu g/mL. The relative inhibitory potency was panaxydol > falcarinol > falcarindiol. Maximal inhibition at 20 mu g/mL corresponded to approximately 95% and 80% inhibition of cell proliferation in normal and cancer cells, respectively. Combinations of falcarinol and falcarindiol added to normal and cancer cells showed a synergistic response for the inhibition of cell growth. Furthermore, the oxidized form of falcarinol, falcarinon, showed a significantly less growth inhibitory effect in intestinal cells of both normal and cancer origin; hence, a hydroxyl group at C-3 may be important for activity of falcarinol-type polyacetylenes. Extracts of carrots, containing different amounts of falcarinol, falcarindiol, and falcarindiol 3-acetate had significant inhibitory effects on both normal and cancer cell proliferation. In cancer cells, the extract containing the highest concentration of falcarinol tended to have the highest growth inhibitory effect, in accordance with a higher potency of falcarinol than falcarindiol. The present study demonstrates that aliphatic C-17-polyacetylenes are potential anticancer principles of carrots and related vegetables and that synergistic interaction between bioactive polyacetylenes may be important for their bioactivity.
Chemoenzymatic Asymmetric Total Syntheses of Antitumor Agents (3R,9R,10R)- and (3S,9R,10R)-Panaxytriol and (R)- and (S)-Falcarinol from Panax ginseng Using an Enantioconvergent Enzyme-Triggered Cascade Reaction
摘要：
Total asymmetric synthesis of two components of Panax ginseng showing antitumor activity, i.e., (3R,9R,10R)- and (3S,9R,10R)-Panaxytriol and of both enantiomers of Falcarinol was accomplished. Due to the fact that the synthetic strategy was based on enantio-convergent biotransformations, the occurrence of any undesired stereoisomer was entirely avoided. The absolute configuration of naturally occurring Panaxytriol was confirmed to be (3R,9R,10R) on the basis of optical rotation values. It was shown that enzyme-triggered cascade reactions represent a valuable tool for the synthesis of natural products.
[EN] HUMANIZED ANTI-TN-MUC1 ANTIBODIES AND THEIR CONJUGATES<br/>[FR] ANTICORPS ANTI-TN-MUC1 HUMANISÉS ET LEURS CONJUGUÉS
申请人：CANCER REC TECH LTD
公开号：WO2015159076A1
公开（公告）日：2015-10-22
Humanized anti-Tn-MUC1 antibodies and conjugates thereof. Conjugates comprising pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker to the antibody are described.
[EN] METHOD AND MOLECULES<br/>[FR] MÉTHODE ET MOLÉCULES
申请人：MEDIMMUNE LLC
公开号：WO2018218093A1
公开（公告）日：2018-11-29
The present invention provides a bioconjugation method and compounds for use therein. The bioconjugation method comprises the step of conjugating a biological molecule containing a first unsaturated functional group with a payload comprising a second unsaturated functional group, wherein the first and second unsaturated functional groups are complementary to each other such that conjugation is a reaction of said functional groups via a Diels-Alder reaction which forms a cyclohexene ring.
The present invention is directed to a novel taste-masking composition comprising a taste-masking effective amount of an
Angelica
root extract, which shows unexpected effectiveness in reducing an undesirable taste in a food product (e.g., a beverage, broth, or whole grain food product), a dental product, an oral hygiene product or a medicinal product.
Two very important factors in human life—which play vital roles in promoting well being—includes returning the body to homeostasis and giving boost to body called lifeforce to get overall health free from diseases, i.e., its optimal balanced functioning ability. When the body is at homeostasis, there is no place for disease. It is only when the body is out of balance (something is deficient, in excess or stagnating) that pain, illness or disease can occur. The application described is based on returning the body to homeostasis (removing the problem and balancing the body) by providing lifeforce and not on dealing with the symptom (e.g., pain, vitamin deficiency). Imbalance results in various diseases and adverse health conditions (starting from aging to diabetes and cancers). This wonderful composition will interact with the body in a way that allows it to boost lifeforce and reach homeostasis no matter which direction it was. In this combination, in the form of liquid, all the 14 ingredients (
Lepidium meyenii
(Maca),
Croton planstigma
(Dragon's blood) tree sap,
Uncaria tomentosa
(Cat's Claw),
Morinda citrifolia
(Noni fruit) 4:1 PE, Lutein, Lycopene 5%, Flaxseed Oil (Omega-3-Fatty Acids), Vinpocetine, Phosphatidyl Serine 50%, Korean Ginseng 80%,
Bacopa monnieri
(Bacopin), CDP Choline (Cognizing), Guaranine (Guarana Seed PE 12%), Yerba Mate Ext. 8%) work as mixture for returning the body to homeostasis and give it lifeforce.
Site-specific antibody-drug conjugates are described, in particular conjugates comprising an antibody which binds PSMA, and which comprises an amino acid substitution of an interchain cysteine residue by an amino acid that is not cysteine and pyrrolobenzodiazepines (PBDs) having a labile protecting group in the form of a linker. The site of conjugation, along with modification of the antiobody moiety, allows for improved safety and efficacy of the ADC.
