Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Biocides; animal or insect repellents or attractants
Reexamination Certificate
2000-09-06
2002-04-16
Pryor, Alton (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Biocides; animal or insect repellents or attractants
C504S130000, C514S183000, C514S343000
Reexamination Certificate
active
06372239
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates to compositions and methods for controlling pest, and, more particularly, to pesticides that are derived from natural substances, such as plant alkaloids.
2. Description of Related Art
Infestation of pests continues to threaten the health of humans and animals, and causes damages to plants, wood structures and households. In particular, some 10,000 species of the more than 1 million species of insects are crop-eating, and of these, approximately 700 species worldwide cause most of the insect damage to man's crops, in the field and in storage.
Our ancestors have used a wide variety of natural materials to protect plants from insects since 1000 B.C. For example, the earliest records of insecticides pertain to the burning of “brimstone” (sulfur) as a fumigant. Even gall from green lizard was used to protect apples from worms and rot. Later, whitewash, lye, brine, vinegar, extracts of pepper and tobacco, and fish oil were used to control pests and repel biting and tickling insects.
Since the World War II (1940), attention has been focused on synthetic pesticidal chemicals that can be synthesized economically and used in large amounts to control insects on plants and in households. Thomson WT (1998) Agriculture Chemicals, Book I, “Insecticides”, Thomson Publications, Fresno, Calif. These synthetic organic insecticides can be classified into many types of chemicals, including organochlorines, organophosphates, organosulfurs, carbamates, formamidines, dinitrophenols, organotins, pyrethroids, nicotinoids, spinosyns, fiproles, pyrroles, pyrazoles, pyridazinones, quinazolines, and benzoylureas.
The organochlorines are insecticides that contain carbon, hydrogen, and chlorine. The oldest group of the organochlorines is the diphenyl aliphatics, which included DDT, DDD, dicofol, ethylan, chlorobenzilate, and methoxychlor. More than 4 billion pounds of DDT were used throughout the world, beginning in 1940, and ending essentially in 1973, when the U.S. Environmental Protection Agency canceled all uses. Other organochlorines include hexchlorocyclohexane (HCH), cyclodienes, and polychloroterpens.
The organophosphates (OPs) are the most widely used synthetic pesticidal chemicals. Other names that are known for this type of pesticide are organic phosphates, phosphorus insecticides, nerve gas relatives, and phosphoric acid esters. All organophosphates are derived from one of the phosphorus acids, and as a class are generally the most toxic of all pesticides to vertebrates. Because of the similarity of OP chemical structures to the “nerve gases”, their modes of action are also similar. Their insecticidal qualities were observed in Germany during World War II in the study of the extremely toxic OP nerve gases sarin, soman, and tabun.
The OPs have two distinctive features: they are generally much more toxic to vertebrates than other classes of insecticides, and most are chemically unstable or nonpersistent. It is this latter characteristic that brought them into agricultural use as substitutes for the persistent organochorines.
The OPs work by tying up or inhibiting certain important enzymes of the nervous system, namely cholinesterase (ChE). The enzyme is shown to be phosphorylated when it becomes attached to to the phosphorous moiety of the insecticide, a binding that is irreversible. This inhibition results in the accumulation of acetylcholine (ACh) at the neuron
euron and neuron/muscle (neuromuscular) junctions or synapses, causing rapid twitching of voluntary muscles and finally paralysis.
The OPs, originally developed as nerve gases during the World War II, can impose serious dangers to people exposed to this type of chemicals. The OPs attack the brain and nervous system, even short-term exposure can cause damage. Symptoms include headaches, nausea, dizziness, seizures, and in extreme cases can result in paralysis, coma, and death.
Safer pesticides have been derived from plants such as tobacco, pyrethrum, derris, hellebore, quassia, and camphor. In particular, pyrethroids, synthetic or extracted from chrysanthemum, are widely used as insecticides in many countries.
Unfortunately, long-term use of a single type of pesticides that have similar mechanisms of action can result in pesticide resistance and resurgence of pests. Resistance and resurgence of pests represents a major problem in agriculture. To date, more than 500 species, including rats, mice, German cockroaches, mosquitos, Drosphilia melanogaster, and tobacco bud worms, are known to have developed resistance to the toxic effects of a variety of pesticides. Pesticide resistance is characterized by multiple mechanisms including increased detoxification, reduced absorption of applied pesticides, increased tolerance of the pesticide by the targeted pest, and increased elimination by the pest of the applied pesticide. Such resistance interjects elements of uncertainty when applying pesticides to target pest and can require a regimen of increasing application rates or ever-changing pesticides to overcome or prevent the development of resistance. Increasing the amount, frequency or rate of pesticide application, in turn, can generate a more serious problem of accumulating residual pesticide on plants and environmental contamination as to soil, air, and water.
SUMMARY OF THE INVENTION
The present invention provides novel compositions and methods for controlling pests, in particular, for killing insects that cause harmful effects to plants, wood, and animals. The compositions of the present invention may be used as a pesticide to prevent and protect plants from damages caused by insects, to prevent and reduce damages caused by termite to wood structures, and to protect and cure animals infested with harmful insects and microorganisms.
The compositions of the present invention comprise cocktails of plant alkaloids that are combined to exert its insecticidal activity via multiple pathways of signal transduction. The alkaloids in the compositions possess a variety of structures and functions which may contribute to the synergistic lethal effects of the compositions on a broad spectrum of insects.
In one embodiment, the composition of the present invention comprises: anabasine; and one or more plant alkaloids selected from the group consisting of toosendanin, azadirachtin, tomatine, nicotine, matrine, oxymatrine, sophocarpine, N-oxysophocarpine, cytisine, and aloperine. Optionally, the composition comprises two, three, four or more members of this group.
According to the embodiment, the alkaloid anabasine may be chemically synthesized. Alternatively, anabasine may be extracted from plants such as Anabasis aphylla, Nicotiana acuminata, Duboisia myoporoides, Zinnia elegans, and Zollikoferia eliquiensis. When extracted, anabasine may be in a pure form, a semi-purified form, or may be a component of an unpurified plant extract.
Also according to the embodiment, the one or more plant alkaloids may be chemically synthesized. Alternatively, the one or more plant alkaloid may be extracted from plants. When extracted, they may be in a pure form, a semi-purified form, or may be a component of an unpurified plant extract.
For example, toosendanin may be extracted from the plants Melia toosendan Sieb. et Zucc. and Melia azedarach L. Azadirachtin may be extracted from the plant Melia azedarach L. Tomatine may be extracted from Lycopersicon esculentum. The alkaloids, matrine, oxymatrine, sophocarpine, and N-oxysophocarpine, may be extracted from the plants Sophora flavescens Ait., and Sophora alopecuroides L. Cytisine and aloperine may be extracted from Sophora alopecuroides L.
In a variation of the embodiment, the composition further comprises a plant alkaloid selected from the group consisting of ricinine, harmaline, stellerin, euphol, triptonide, tripdiolide, and triptolide.
According to the variation, the plant alkaloids may be synthesized chemically, or extracted from plants. For example, ricinine may extracted from Ricinus communis L. Harmaline may be extracted from Peganum
Lei Ling
Wu Chang-An
Wu Hong
GreenTech, Inc.
Pryor Alton
Wilson Sonsini Goodrich & Rosati
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