6. The Chlorin e6 Oral Agent Medicinal Product

Introduction

The main active principle of the preparation is the extract of water-soluble active chlorophyll which is extracted from natural raw material (microalgae Spirulina Platensis) in accordance with a special patented technology. The Russian patent №2183956 dated March 30, 2001, is based on the technology of extracting highly active elements (chlorin e6), which are able to penetrate into a damaged or foreign cell, from chlorophyll.

Due to the high clinical efficacy, chlorin e6 is popular in Russia, as well as in a number of foreign countries (like Holland, Germany, Great Britain, Ireland, the USA, Canada, Australia, Mexico, Korea, etc.).

The preparation underwent clinical studies in the Hematological Research Center of RAMS. The clinical studies carried out in specialized medical institutions, as well as rather long-time clinical examinations of individual patients showed an immunomodulatory effect which causes a number of positive changes in the body of a person suffering from chronic diseases. In particular, there was found a precise positive influence of chlorin e6 on the growth of the absolute number of neutrophils, lymphocytes and macrophagocytes of periferic blood, which afterwards was confirmed clinically in patients suffering from lymphogranuloma. The immunomodulatory activity of chlorin e6 is connected with increase of the enzymatic activity of macrophagocytes, with increase of production of active forms of oxygen and synthesis of cytokines. The latter ones, in their turn, under the principle of direct link and feedback, activate T- and B-systems of immunity. Chlorin e6 has the ability not only to enhance the formation of cytokines, but also, in small doses, to stimulate the synthesis of receptors to the tumor necrosis factor (TNF) and to interleukin-1 (IL-1) which are antagonists of these inflammatory cytokines. Therefore, chlorin e6 is also able to produce an inflammatory effect. This allows one to recommend it to treat patients suffering from diseases which go along with an inflammatory process against the background of a defect in the immune system. Life quality improvement for 85% of patients proves its positive influence on the general metabolism and processes of neurodynamics.

Mechanism of Action

Chlorin e6 (extract of active chlorophyll), as a photosensitizer, is able to be accumulated in ill-defined cells and tissues. The warmth of the body and light encourage activation of chlorophyll derivatives with energy transport on the cell oxygen. This leads to the formation of a highly active form of oxygen which causes a chain of oxidative reactions in ill-defined cells, which leads to their death. The immune system is activated and eliminates all foreign cells, including those which have a tendency for transformation into oncological cells.

Clinical studies showed high results of using chlorin e6 to treat such serious diseases as chronic hepatitises, psoriasis, chronic viral and bacterial infections, myomata, cysts, mastopathy, prostatitis, as well as malignant tumors which, in the process of using this preparation, decreased in size immensely and, in some cases, totally resolved.

According to the data of the clinical studies held in the Hematological Research Center of RAMS, chlorophyll derivatives fulfill their immunomodulatory properties on the cell and humor levels. And this happens both directly and indirectly, through suppression of pathological processes. Intake of chlorin e6 prevents development of immunodeficient diseases, including in oncological and oncohematological patients who are at the stage of anticancer chemotherapy. As a result of using chlorin e6, the rheological properties of blood improve, the microcirculation enhances, the aggregation of erythrocytes and thrombocytes decreases, which decreases the risk of thrombocytic complications development.

The ability of chlorophyll derivatives to link with low-density and very low-density lipoproteins (LDL and VLDL) decreases the risk of atherosclerosis development, which shows their antiatherogenic and vasoprotective properties and makes it effective to use chlorin e6 in patients suffering from atherosclerosis, ischemic heart disease (IHD), cerebrovascular diseases, diabetes, etc. Chlorin e6 improves life quality, which can be seen through enhancement of physical activity, labor ability, improvement of overall health condition.

The usage of chlorin e6 makes the immune system activate and eliminate not only its own ill–defined cells, but also foreign ones (mold, fungi, viruses, helminths, etc.), which actively use the substance for their nutrition. At that, active chlorophyll gets accumulated regardless of the type of a tumor, the size of the damaged area, the speed of disease development and the stage of its spread. Doctors are actively introducing chlorin e6 into their practice to treat the following diseases: cysts, polyps, myomata, thyroid nodules, mastopathy, prostatic adenoma, etc.

The usage of chlorin e6 is advised for primary and postprimary immunodeficient diseases; for prevention of thrombocytic complications in patients with a higher risk of their development (patients with IHD, thrombophlebitis, varicose vein disease in lower limbs, etc.); as an antiatherogenic means and a means to improve rheological properties of blood and microcirculation in patients with atherosclerosis, diabetes, ischemic heart disease, cerebrovascular diseases, arterial hypertension, both primary and symptomatic.

Description of the Chlorin e6 Oral Agent Medicinal Product

This is an absolutely non-toxic photosensitizer and, at the same time, an anticancer immunomodulator which immensely activates the system of cell immunity and, especially, K-cells (killer cells) which find and destroy tumor cells. The content of the active substance (Spirulina Platensis) in one capsule of the Chlorin e6 Oral Agent preparation is not less than 34 mg. Also, the Chlorin e6 Oral Agent preparation, in most cases, quickly improves life quality of oncological patients. It is extremely important that the Chlorin e6 Oral Agent preparation protects patients from side effects of chemotherapy (liver damage, hematosis, immune system functions decrease).

Oncological diseases nowadays are supposed to be the consequence of a failure in energetic balance of a stem (immortal) cell of a tissue or an organ. The energetic potential of a cell depends on a number of factors and defines the functioning of mechanisms of cell metabolism, organism adaptation, immune response. Preparations and treatment (including medical) which normalize some concrete damaged part of the immune system, are called «immunocorrectors». Similarly, the Chlorin e6 Oral Agent preparation can be called an «energocorrector». Thus, «energocorrectors» normalize the energetic potential of a cell which is generally connected with the activity of mitochondria – these are cell «healers» of pin-point target action. The Chlorin e6 Oral Agent preparation which contains chlorin e6 in high concentration, has a strong energo- and immunocorrecting activity. This is caused by its specific affinity to pathological cells and by its ability to create targeted suppression of atypical (precancerous, cancerous) cells and to change them for normal ones.

The usage of the Chlorin e6 Oral Agent preparation for the treatment of oncological and oncohematological patients at the stage of anticancer chemotherapy, softens the phenomenon of myelosuppression (suppression of proliferative activity of healthy cells of the bone marrow of myeloid range). A satisfying level of erythrocytes, leukocytes and thrombocytes in periferic blood reached after that, allows to decrease the risk of infectious and hemorrhagic complications, to hold courses of the main treatment in due time.

Results of Laboratory Research for the Chlorin e6 Oral Agent Medicinal Product

The research object is Spirulina Platensis. The content of the active substance (Spirulina Platensis) in one capsule of the Chlorin e6 Oral Agent preparation is 38.54 mg. The weight of the whole contents of a capsule is 310.5 mg. The concentration of the active substance is consequently 12.4 % by weight. The concentrations given below and the absorption coefficients were calculated due to the content of the active agent and not to the whole contents of a capsule.

The preparation used in the research for the purpose of comparison is Radachlorin (0.35 % water solution for intravenous administration) in a 10-ml vial which contains 35 mg (3.5 mg/ml) of the active chlorin substance which is Sodium Salt (Chlorin Sodium Salt).

1. The comparison of absorption coefficients

Pictures 1 – 3 give the absorption spectra of the solutions of the Chlorin e6 Oral Agent preparation and the Radachlorin preparation in 0.5 % chlorohydric acid solution with pH=1.5 – a model of gastric juice (picture 1), in distilled water with pH=7 (picture 2), and in sodium hydroxide solution with pH=9.5 – a model of small intestine medium (picture 3). The concentration of Spirulina Platensis in the solutions was 0.75 mg/ml, and that of Chlorin Sodium Salt was 0.05 mg/ml, e.i. the concentration of the active substance of the Radachlorin preparation was 15 times less than the concentration of the active substance of the Chlorin e6 Oral Agent preparation. Such concentrations were used for analysis in one optical density range. The behavior of the preparations in mediums with various pHs is illustrated in pictures 4 and 5.

As it seen from the given pictures, in acid medium the Chlorin e6 Oral Agent preparation makes aggregates, which influences its absorption spectrum. A similar thing happens to the Radachlorin preparation. This reaction is however reversible: alkalization of the acid solution of Chlorin e6 Oral Agent or Radachlorin makes the preparation dissolve and demonstrate absorption which is similar to that one of the preparation which initially was put into the alkaline medium.

The absorption coefficients of the Chlorin e6 Oral Agent and the Radachlorin preparations were calculated due to their absorption spectra in neutral and alkaline media. The maximum absorption of the Chlorin e6 Oral Agent preparation in the red range of the spectrum is ε=1.2 ml/mg*cm in neutral medium, and ε=1.9 ml/mg*cm in alkaline medium. The maximum absorption of the Radachlorin preparation in the red range is ε=37.1 ml/mg*cm in neutral medium, and ε=41.7 ml/mg*cm in alkaline medium.

Picture 1. Absorption spectra of the solutions of the Chlorin e6 Oral Agent preparation (the concentration of the active substance is 0.75 mg/ml) and the Radachlorin preparation (the concentration of the active substance is 0.05 mg/ml) in acid medium. The thickness of the sample is 1.0 cm.

Picture 2. Absorption spectra of the solutions of the Chlorin e6 Oral Agent preparation (the concentration of the active substance is 0.75 mg/ml) and the Radachlorin preparation (the concentration of the active substance is 0.05 mg/ml) in neutral medium. The thickness of the sample is 1.0 cm.

Picture 3. Absorption spectra of the solutions of the Chlorin e6 Oral Agent preparation (the concentration of the active substance is 0.75 mg/ml) and the Radachlorin preparation (the concentration of the active substance is 0.05 mg/ml) in alkaline medium. The thickness of the sample is 1.0 cm.

Picture 4. The Chlorin e6 Oral Agent preparation with the concentration of the active substance of 0.75 mg/ml in acid medium (pH=1.5), in neutral medium (pH=7.0) and in alkaline medium (pH=9.5) (from left to right).

Picture 5. The Radachlorin preparation with the concentration of the active substance of 0.05 mg/ml in acid medium (pH=1.5), in neutral medium (pH=7.0) and in alkaline medium (pH=9.5) (from left to right).

2. The comparison of fluorescence intensity

Picture 6 gives the fluorescence spectra of the solutions of the Chlorin e6 Oral Agent preparation and of the Radachlorin preparation in 0.5 % hydrochloric acid solution with pH=1.5 – a model of gastric juice, in distilled water with pH=7, and in sodium hydroxide solution with pH=9.5 – a model of small intestine medium. The concentration of Spirulina Platensis in the solutions was 0.75 mg/ml, and that of Chlorin Sodium Salt was 0.05 mg/ml, e.i. the concentration of the active substance of the Radachlorin preparation was 15 times less than the concentration of the active substance of the Chlorin e6 Oral Agent preparation. Such concentrations were used for analysis in one fluorescence range. The given diagrams show how the fluorescence intensity changes due to the changing pH of the solution.

Picture 6. Fluorescence spectra of the solutions of the Radachlorin preparation with the concentration of the active substance of 0.05 mg/ml in alkaline medium (the red spectrum), in neutral medium (the blue spectrum) and in acid medium (the dark blue spectrum), and fluorescence spectra of the solutions of the Chlorin e6 Oral Agent preparation with the concentration of the active substance of 0.75 mg/ml in alkaline medium (the yellow spectrum), in neutral medium (the purple spectrum) and in acid medium (the violet spectrum).