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Compounds of phorbol esters and methods of use

A technology of phorbol ester and composition, applied in the field of cell pathology, can solve severe nausea, decreased bone marrow function, toxicity and other problems

Inactive Publication Date: 2016-05-25
BIOSUCCESS BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, it can be difficult to obtain a clear border around a tumor, leaving some residual tumor tissue and increasing the chance of disease recurrence
Almost all current chemotherapy agents are toxic, and chemotherapy causes significant side effects, including severe nausea, decreased bone marrow function, and immune suppression

Method used

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  • Compounds of phorbol esters and methods of use
  • Compounds of phorbol esters and methods of use
  • Compounds of phorbol esters and methods of use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Effects of TPA on the number of peripheral white blood cells (WBC) and hemoglobin (Hb) in mice injected with S180 cells:

[0107] Sarcoma 180 (S180) cells were injected into Kunming (Kwen-Ming) mice. On day three, mice were given 50, 100 or 200 μg / kg / day of TPA intraperitoneally (i.p.) for 7 days. The day after completion of treatment, blood samples were taken from the tails of treated mice for WBC and Hb analysis. The WBC counts in the treatment groups (50, 100, or 200 μg / kg / day for 7 days) were 16.1±7.4, 18.7±3.0, and 20.7±3.4x10 per liter, respectively. 9 ; while the WBC count in the control group was 13.6±1.8x10 per liter 9 . The Hb in the treatment group was 136±11, 149±12 and 149±10 grams per liter, while the Hb in the control group was 134±15 grams / liter. The results indicate that the i.p. injection of TPA can increase the number of peripheral white blood cells (WBC) in the mice according to the degree of dose. However, after comparing with the mice in the co...

Embodiment 2

[0109] Dose Ranging Studies

[0110] Due to the strong local irritation caused by TPA, TPA is administered to patients by intravenous (i.v.) injection. The TPA solution in the sterile syringe was injected into 200 ml of sterile normal saline and mixed well for i.v. injection.

[0111] Clinical toxicity and side effects of different TPA dosages:

[0112] (1) Dosing at a dose of 1 mg of TPA per patient per week:

[0113] One milligram of TPA in solvent was mixed well with 200 milliliters of sterile saline for intravenous injection at a rate of 16 micrograms per minute over 1 hour. One hour after TPA administration, the patient began to have chills lasting 30 minutes, followed by fever (the patient's body temperature reached 37.5-39.5°C and lasted for 3-5 hours, and then returned to normal), accompanied by varying degrees of sweating . The above symptoms can be alleviated by giving patients glucocorticoid. TPA at this dose caused a small number of patients to bleed, while se...

Embodiment 3

[0119] Phase 1 clinical trial of HIV+patients treated with TPA

[0120] Twelve symptomatic patients (five men and seven women) were treated with TPA, aged 35 to 52, all of whom were HIV-infected by blood transfusion in 1995, And are resistant to standard HIV treatment. Each patient was administered intravenously (i.v.) a weight-adjusted dose of TPA (75 μg / sqm) in 200 mL of sterile saline over 1 hour. This dose is given once daily for the first to three days of treatment. Each patient was then given this dose every two days from day 4 to day 8, followed by a 6-month rest period before the second phase of treatment according to the same program.

[0121] Blood samples were collected prior to the first dose and on Days 4 and 40 of the treatment cycle. The amount of CD3, CD4 and CD8 in peripheral blood was measured by monoclonal antibody (Becton Dickson Scientific Co., Franklin Lakes, NJ) and flow cytometer (B.D. Bioscience, San Diego, CA).

[0122] As shown in Table 1, no con...

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Abstract

The present invention provides methods and compositions comprising crotyl esters or crotyl ester derivatives for the treatment of cytopathic diseases. Cytopathic diseases can be caused by various means, for example, viral infection, such as HIV and AIDS, or the development of neoplastic lesions in mammalian subjects. The methods and compositions of the present invention are effective for inhibiting new HIV infection, upregulating viral expression from latent provirus, inhibiting HIV-induced cytopathic effects, downregulating HIV receptors, and increasing Th1 cytokine expression , reducing Th2 cytokine expression, increasing ERK phosphorylation, inducing apoptosis in malignant tumor cells, remission induction, remission maintenance, use as a chemotherapeutic agent, and for alleviating the symptoms of cytopathic diseases and the opportunistic infections that accompany these diseases. The present invention provides additional compositions and methods employing crotyl esters or derivatives thereof in combination with at least one additional agent, such as an agent for a course of HAART, a therapeutic agent for treating opportunistic infections due to HIV, or is a chemotherapeutic agent to generate a more effective therapeutic tool against cytopathic diseases in mammalian subjects.

Description

[0001] 【Related application】 [0002] This application claims priority to US Provisional Patent Application Serial No. 60 / 898,810, filed January 31, 2007, which is hereby incorporated by reference in its entirety. 【Technical field】 [0003] The present invention relates generally to the field of cytopathic diseases. More specifically, the present invention relates to a compound comprising a phorbol ester and a method of using a phorbol ester for the treatment of a cytopathic condition and the disease causing the cytopathic condition. 【Background technique】 [0004] Phorbol is a naturally occurring organic compound from plants, which belongs to diterpenes. Phorbol was first isolated in 1934 as a hydrolyzate of croton oil produced from the seeds of croton (cortontiglium), a leafy shrub native to Southeast Asia in the Euphorbiaceae family. Various esters of phorbol have important biological properties, including the well-known diacylglycerols and the ability to initiate prote...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N43/00A01N43/46A61K31/55
CPCA01N43/46A01N63/00A61K31/225A61K31/23A61K31/55A61K31/573A61K31/60A61K31/606A61K31/618A61K45/06C07C69/013C07C69/22C07C69/33C07C2603/40A61P31/18A61P35/02A61P35/00Y02A50/30A61K31/222
Inventor 张立才韩正涛
Owner BIOSUCCESS BIOTECH CO LTD
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