Alkaline preparations of Inula for the control of fungal...

Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from compositeae

Reexamination Certificate

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C424S725000, C424S773000, C424S405000, C424S774000, C424S779000

Reexamination Certificate

active

06423352

ABSTRACT:

FIELD OF THE INVENTION
The subject invention relates an anti-fungal preparation for the control of fungal diseases in plants, more specifically, to alkaline extracts of Inula which are highly active in controlling diseases caused by fungi in crop plants.
BACKGROUND OF THE INVENTION
Extracts of plants which are members of the Inula species are effective against infections of plants caused by a variety of fungi. These extracts are typically prepared by dipping freshly cut Inula shoots in an organic solvent or by agitating freshly cut or dried Inula shoots in an organic solvent, removing the solvent to form a paste, and then dissolving the paste in an organic solvent or in water, possibly with an additive. Alternatively, suspensions of Inula can be prepared by grinding dried Inula shoots into a fine powder, adding an emulsifier, and then suspending the mixture in water. In both cases, the resultant preparation is then applied to plants resulting in the control of a wide variety of fungal diseases. Extracts of suspensions of Inula plants are effective at low concentrations, in the range of fractions of a single percent of extract, such that dilute concentrations have excellent fungal-control properties.
The plants which are the basis of these fungicidal extracts and suspensions are
Inula viscosa
and
Inula graveolens
(Family Compositae), perennial weeds widespread in the Mediterranean Basin.
Methods of preparing aqueous extracts from various parts of the Inula plant are well known in the literature. Additionally, organic extracts of the Inula plant are also well known in the art, e.g., U.S. Pat. No. 5,837,253. However, the prior art indicates that aqueous extracts of Inula shoots are poorly effective against fungal diseases of crop plants whereas extracts made with organic solvents are highly effective anti-fungal agents.
Methods have also been described for using organic solvents to extract Inula plants, but these are clearly distinguished from that disclosed in U.S. Pat. No. 5,837,253. Two of the prior art methods involved contacting the whole Inula plant, or the aerial parts thereof, with an organic solvent either by maceration of the plant in the organic solvent or by percolation of the solvent through the plant. Furthermore, U.S. Pat. No. 4,254,112 to Debat et al., (hereinafter referred to as “Debat”) describes the preparation of extracts of
Inula viscosa
and
Inula graveolens
using whole Inula plants which have been dried and ground and organic solvents, by using a Soxhlet apparatus. The yield of the paste obtained by this method was approximately 1.75-4%. U.S. Pat. No. 5,176,193 to Honerlagen et al. (hereinafter referred to as “Honerlagen”) describes a process for preparing a partial extract from roots of
Inula helenium
which involves contacting the plant material with an organic solvent, adding a drying agent to the solution to remove the water, removing the drying agent, and then distilling the dried organic phase. By contrast, the method disclosed in U.S. Pat. No. 5,837,753 disclosed either briefly dipping the leaves and stems of the shoots of
Inula viscosa
or
Inula graveolens
into an organic solvent or shaking the freshly cut or dried and ground leaves and stems of the shoots in an organic solvent for thirty minutes, and then evaporating the solvent to form a paste. The yield obtained by this method can be as much as 30%, in contrast to the low yields known in the literature and described above.
The medicinal properties of Inula extracts in humans are well known. For example, Debat disclosed the anti-microbial activity of extracts of Inula for use in human beings. However, the fungicidal effects of Inula extracts have only been demonstrated on fungi growing in Petri dishes or on post-harvest of fruits. For example, Qasem et al. (
Phytopathologia Mediterana,
34:7-14, 1995) demonstrated that the growth of certain fungi in Petri dishes was inhibited by aqueous extracts of
Inula viscosa
as well as by dried plant material added directly to the fungal growth media. By contrast, the method of the present invention uses Inula extracts prepared with alkaline aqueous solvents used against fungal infections of crop plants themselves.
Clearly, although Inula extracts have been shown to have fungicidal activity in the Petri dish (in vitro) and on plant (in vivo), the methods of preparation for these extracts have not been sufficient for large scale use directly on crop plants and have had other serious disadvantages. The true effectiveness of these extracts against fungal infections of plants is, therefore, unknown. Furthermore, there is a clear need for better methods to prepare Inula extracts. Qasem et al. (Ibid, page 13, 1995) concluded: “The diversity and the methodology of extraction and the differences in the results obtained . . . increased the need for developing more efficient, convenient, and cheaper methods of extraction to facilitate more extensive utilization of fungicidal extracts, especially if greater quantity of extracts must be prepared for large-scale production”.
Thus, there is a widely recognized need for and would be highly advantageous to have a method or methods for preparing extracts and/or suspensions of plants of Inula species which would facilitate the large-scale use of these extracts and suspensions which would simplify their preparation and use, be highly effective in controlling fungal infection in plants, as well as controlling fungal infections in crop plants.
SUMMARY OF THE INVENTION
According to the present invention, there is provided a method for preparing an aqueous extract from Inula species which comprises contacting shoots and/or portions thereof with an alkaline aqueous solvent to form a solution and debris, and removing the debris from the solution.
There is also provided a method for protecting plants against fungal infection comprising preparing a fungicidal extract of Inula species by contacting shoots and/or portions thereof with an alkaline aqueous solvent to form an extract solution and debris, and applying a fungicidally effective amount of the fungicidal extract to a plant for protecting the plant against fungal infection.
There is also provided in accordance with the present invention, a method for preparing a fungicide derived from Inula species which comprises combining a substantially powdered form of Inula shoots and/or portions thereof with a solid chemical to form a mixture which upon dissolution of the mixture in an aqueous solvent, forms an alkaline aqueous solution which can be directly applied to plants to prevent fungal infection.
Additionally, also in accordance with the present invention, there is provided an alkaline anti-fungal composition which comprises Inula shoots and/or portions thereof and a compound which when mixed with an aqueous solvent forms an alkaline solution, whereby the composition can be directly applied to plants to prevent fungal infection.
Accordingly, the subject invention provides a method for unexpectedly producing an anti-microbial extract from Inula plants which is not only active in vitro against fungi but also is active against diseases caused by fungi in crop plants while being safe to apply to the crop itself.
DETAILED DESCRIPTION OF THE INVENTION
The present invention provides a method for preparing an extract from Inula species including the steps of contacting shoots and/or portions thereof with an alkaline aqueous solvent to form a solution and debris and then removing the debris from the solution.
Preferably, the portion and/or portions of the Inula plant which are utilized in the present invention are the leaves and stem of the upper, younger parts of the shoots, and the upper part of the shoot extending from about 20-40 centimeters from the tip of the shoot. The flowers themselves are not used. As used herein, the term “shoot” is used to define the leaves and stem of the shoot of the Inula plant. In the methods of the present invention, the shoots or portions thereof can be either freshly cut or may be dried prior to the addition of the alkaline aqueous solvent.
Th

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