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CN-121987688-A - Loquat leaf extract, preparation method thereof and application thereof in preparation of medicines with breast cancer resisting effect

CN121987688ACN 121987688 ACN121987688 ACN 121987688ACN-121987688-A

Abstract

The invention relates to the technical field of pharmaceutical chemistry, and further discloses a loquat leaf extract, a preparation method thereof and application thereof in preparing medicines with an anti-breast cancer effect. The preparation method of the loquat leaf extract comprises the steps of taking loquat leaves, adding an ethanol aqueous solution according to a feed liquid ratio of 1g to 80-120mL for ultrasonic extraction, separating an extracting solution after extraction is finished, concentrating and drying to obtain the loquat leaf ultrasonic extract, and taking the loquat leaf ultrasonic extract to obtain the loquat leaf extract. Studies show that the loquat leaf extract prepared by the method has an inhibition effect on topoisomerase I. Therefore, the loquat leaf extract provided by the invention has potential application value in preparing medicines with the effect of resisting breast cancer.

Inventors

  • Pan Zengfeng
  • ZENG HUANG
  • LIU XIAOMIN
  • XIE ZHIHAO

Assignees

  • 梅州市人民医院(梅州市医学科学院)

Dates

Publication Date
20260508
Application Date
20260327

Claims (10)

  1. 1. A preparation method of a loquat leaf extract is characterized by comprising the steps of taking loquat leaves, adding an ethanol aqueous solution according to a feed liquid ratio of 1g to 80-120mL for ultrasonic extraction, separating an extracting solution after extraction is finished, concentrating and drying to obtain the loquat leaf ultrasonic extract, and taking the loquat leaf ultrasonic extract to obtain the loquat leaf extract.
  2. 2. The method for preparing the loquat leaf extract according to claim 1, wherein the ultrasonic extraction is performed by adding an aqueous ethanol solution at a feed liquid ratio of 1g to 100 ml.
  3. 3. The method for preparing the loquat leaf extract according to claim 1, wherein the volume fraction of ethanol in the aqueous ethanol solution is 70-95%.
  4. 4. The method for preparing the loquat leaf extract as recited in claim 1, wherein the volume fraction of ethanol in the aqueous ethanol solution is 80%.
  5. 5. The method for preparing the loquat leaf extract according to claim 1, wherein the condition of ultrasonic extraction is that the power is 70-100W, the ultrasonic temperature is 55-65 ℃ and the ultrasonic time is 20-40 min.
  6. 6. The method for preparing the loquat leaf extract according to claim 1, wherein the condition of ultrasonic extraction is that the power is 80W, the ultrasonic temperature is 59 ℃, and the ultrasonic time is 30min.
  7. 7. The loquat leaf extract prepared by the preparation method of any one of claims 1 to 6.
  8. 8. Use of the loquat leaf extract of claim 7 for preparing a medicament having an inhibitory effect on topoisomerase I.
  9. 9. Use of the loquat leaf extract of claim 8 in the preparation of a medicament with an anti-breast cancer effect.
  10. 10. The use according to claim 8 or 9, wherein the pharmaceutical dosage form is a tablet, capsule, oral liquid dosage form, granule, injection or ointment.

Description

Loquat leaf extract, preparation method thereof and application thereof in preparation of medicines with breast cancer resisting effect Technical Field The invention relates to the technical field of pharmaceutical chemistry, and further relates to a loquat leaf extract, a preparation method thereof and application thereof in preparing medicaments with an anti-breast cancer effect. Background Breast cancer is the most frequently occurring malignancy among women worldwide and has become a serious public health challenge. Despite significant advances in early diagnosis, surgical techniques, radiation therapy, and systemic therapy in recent years, treatment of patients with advanced breast cancer remains a significant challenge. Especially refractory subtypes such as triple negative breast cancer, hormone receptor positive endocrine drug resistance and the like, have limited treatment means and generally have poor prognosis for patients. Meanwhile, the traditional chemotherapy drugs often have obvious toxic and side effects and drug resistance problems, and seriously influence the life quality and the treatment effect of patients. Therefore, the development of novel high-efficiency low-toxicity novel antitumor drugs not only has important clinical practical significance, but also provides a key scientific direction for improving the current situation of breast cancer treatment. Topoisomerase I (Topoisomerase I, TOP 1) is an essential nuclease, and has the core function of solving the problem of DNA topology entanglement through a specific mechanism and maintaining normal operation of key physiological processes such as intracellular DNA replication, recombination, transcription, repair and the like. Specifically, TOP1 attacks the 3' end of the DNA single strand through its Tyr723 residue, forming a reversible DNA-TOP1 covalent complex (TOP 1 cc) that breaks the DNA strand, and then the broken strand rotates around the complete strand releasing the torsional tension, eventually TOP1 breaks away and completes the ligation of the DNA strand. Given that TOP1 expression levels are significantly elevated in proliferation-active cells, it has become an important target for anti-tumor drug development. At present, camptothecin derivatives represented by irinotecan and topotecan are typical representatives of the drugs, and have been approved for the treatment of various malignant tumors such as colorectal cancer, ovarian cancer, cervical cancer, small cell lung cancer and the like. TOP1 shows remarkable high expression in breast cancer tissues, but TOP1 inhibitors are easy to cause DNA damage to normal cells in the process of treating breast cancer, cause serious toxic and side effects such as bone marrow suppression, neutropenia, diarrhea and the like, and limit the application of the medicines in breast cancer. Natural products have been an important source for the development of antitumor drugs due to their structural diversity and good biocompatibility. It was counted that about 34% of antitumor drugs approved by the U.S. food and drug administration were directly derived from natural products or derivatives thereof in the 1981-2010. Under the background, the traditional Chinese medicinal materials with the characteristic of homology of medicine and food become an important resource treasury for development of anti-tumor medicines due to the long safe eating history and rich pharmacological activity. Loquat leaf (Eriobotrya japonica (thunder) Lindl.) is used as a traditional Chinese medicinal material, and is originally carried in Ming Yi Bie Lu (miscellaneous records of famous physicians) and is used for treating cough due to lung heat, vomiting due to stomach heat, and the like. Modern phytochemistry research shows that loquat leaves are rich in various bioactive components such as triterpenes, flavonoids, phenolic acids and the like. Pharmacological studies further reveal that the loquat leaf extract has various biological activities such as anti-inflammatory, antioxidant, blood sugar reducing and anti-tumor activities. Therefore, the loquat leaf is used as a raw material to develop an active site with an inhibition effect on topoisomerase I (Topoisomerase I, TOP 1), and has potential application value for the development and application of breast cancer medicaments. Disclosure of Invention In order to overcome the technical problems in the prior art, the invention provides a loquat leaf extract, a preparation method thereof and application thereof in preparing medicines with the effect of resisting breast cancer. The technical scheme of the invention is as follows: The invention provides a preparation method of a loquat leaf extract, which comprises the following steps of adding an ethanol aqueous solution into loquat leaves according to a feed liquid ratio of 1g:80-120mL for ultrasonic extraction, separating an extracting solution after the extraction is finished, concentrating and drying to obtain the loquat