DESCRIPTION
Chlorophyll is the green pigment found in
higher plants, as well as algae. Chlorophyll is the principal
photoreceptor in photosynthesis, the light-driven process in which
carbon dioxide is "fixed" to yield carbohydrates and oxygen. Chlorophyll
is a cyclic tetrapyrolle, similar in structure to the heme group of
globins (hemoglobin, myoglobin) and cytochromes. Chlorophyll differs
from heme in a few major respects, most notably that the central metal
ion in chlorophyll is magnesium while that in heme is iron.
There are a few types of chlorophyll.
Higher plants and green algae, such as chlorella (see Chlorella) contain
chlorophyll a and chlorophyll b in the approximate ratio of 3:1. The
molecular formula of chlorophyll a is C55H72MgN4O5;
the molecular formula of chlorophyll b is C55H70MgN4O6.
The difference between the two chlorophylls is that a methyl side-chain
in chlorophyll a is replaced by a formyl group in chlorophyll b.
Chlorophyll a is found with chlorophyll c in many types of marine algae.
Red algae contain principally chlorophyll a and also chlorophyll d.
Chlorophyllin is a semi-synthetic
sodium/copper derivative of chlorophyll. In contrast to chlorophyll,
chlorophyllin is water-soluble. Chlorophyllin, like chlorophyll, has
deodorizing activity. It is used as an aid to reduce odor from a
colostomy or ileostomy and also as an aid to reduce fecal odor due to
incontinence. A topical ointment of chlorophyllin is used to reduce
malodors in wounds and surface ulcers.
Chlorophyll and chlorophyllin are
available as nutritional supplements. Preliminary evidence from in
vitro and animal studies suggests that these substances may have
anticarcinogenic activity.
ACTIONS AND PHARMACOLOGY
ACTIONS
Chlorophyll and chlorophyllin may have
antimutagenic and anticarcinogenic activities.
MECHANISM OF ACTION
Chlorophyll and its metabolites
pheophytin, pyropheophytin and pheophorbide, as well as chlorophyllin,
have demonstrated antimutagenic effects in vitro against such
mutagens as 3-methylcholanthrene, N-methyl-N'-nitro-N'-nitrosoguanidine
(MNNG) and aflatoxin B1. Chlorophyll and chlorophyllin have also
demonstrated anticarcinogenic effects in animal models against such
carcinogens as aflatoxin B1, 1,2-dimethylhydrazine and dibenzo[a,1]pyrene.
The mechanism of the antimutagenic and
anticarcinogenic activities of chlorophyll and chlorophyllin are
unknown. It is speculated that antioxidant activity of chlorophyll/chlorophyllin
may play a role in these activities. Another possible mechanism is the
formation of complexes between the mutagen/carcinogen with chlorophyll/chlorophyllin
through strong interactions between their planar unsaturated cyclic
rings. The complexes would effectively inactivate the
mutagens/carcinogens.
PHARMACOKINETICS
There is little on the pharmacokinetics
of chlorophyll and its derivative chlorophyllin in humans. Some older
studies showed that chlorophyll, following absorption, is converted into
pheophytin, pyropheophytin and pheophorbide. These three derivatives of
chlorophyll are tetrapyrolles.
INDICATIONS AND USAGE
Some experimental data suggests that
chlorophyll and chlorophyllin may have some antimutagenic and
anticarcinogenic potential, may help protect against some toxins, and
may ameliorate some drug side effects. They are useful in reducing
urinary and fecal odor in some circumstances. They may help ease
constipation in some. There is some preliminary indication that they
could be beneficial in the treatment of calcium oxalate stone disease
and that they may have some anti-atherogenic activity.
RESEARCH SUMMARY
In one in vitro test,
chlorophyllin demonstrated significant inhibition of several mutagens,
including cigarette smoke, coal dust and diesel emission particles. Its
antioxidant activity may have accounted for this effect. In another
assay, chlorophyllin proved a more effective antimutagen than retinol,
beta-carotene, vitamin C and vitamin E. In an animal study,
chlorophyllin demonstrated both antimutagenic and anticarcinogenic
activity, inhibiting 1,2-dimethylhydrazine-induced nuclear damage in rat
colonic epithelium.
In another animal study, chlorophyllin
significantly inhibited aflatoxin B1 hepatocacinogenesis. In a rainbow
trout multi-organ tumor model, chlorophyllin markedly reduced liver,
stomach and swimbladder cancer incidence.
Chlorophyllin has been used to reduce
some of the side effects of cyclophosphamide. Chlorophyll consumption
has been associated, in an animal study, with increased fecal excretion
of polychlorinated dibenzo-p-dioxin (PCDD) congeners and polychlorinated
dibenzofuran (PCDF). The researchers suggested that green vegetables
rich in chlorophyll might be helpful in humans exposed to PCDD and PCDF
congeners.
In a study of geriatric patients,
chlorophyllin was said to be effective in helping control body and fecal
odors and helped ease chronic constipation. It also reduced excessive
flatus is some. In another study, this one involving incontinent
geriatric patients, subjects received 100 mg of chlorophyllin daily or
placebo for two weeks. A non-significant decrease in urinary odor was
noted in those receiving chlorophyllin, compared with those on placebo.
One preliminary study indicated that
chlorophyllin can inhibit the crystallisation and growth kinetics of
calcium oxalate dihydrate in normal urine and that it might be helpful
in the treatment of calcium oxalate stone disease.
Finally, chlorophyllin significantly
decreased serum cholesterol and triglycerides in a study using rats with
experimental atherogenesis. Followup is needed.
CONTRAINDICATIONS, PRECAUTIONS, ADVERSE
REACTIONS
CONTRAINDICATIONS
Chlorophyll and chlorophyllin are
contraindicated in those who are hypersensitive to any component in a
chlorophyll-containing or chlorophyllin-containing preparation.
PRECAUTIONS
Supplemental chlorophyll and supplemental
chlorophyllin should be avoided by pregnant women and nursing mothers.
ADVERSE REACTIONS
Use of chlorophyll and chlorophyllin
supplements may cause discoloration of the urine (green urine), the
feces (green stool) and the tongue (yellow to black tongue). There are
occasional reports of diarrhea with use of these substances.
INTERACTIONS
In a mouse model, chlorophyllin
ameliorated some of the side effects of cyclophosphamide.
OVERDOSAGE
No reports of overdosage.
DOSAGE AND ADMINISTRATION
There are a few chlorophyll and
chlorophyllin nutritional supplements. Chlorophyllin is available as a
liquid supplement. A typical dose is 100 mg daily. Those who use
chlorophyllin to reduce fecal odor due to incontinence or to reduce odor
from a colostomy or ileostomy typically take 100 mg daily.
HOW SUPPLIED
Capsules — 50 mg, 60 mg, 100 mg
Liquid — 45 mg/15 ml, 75 mg/5 ml
Tablets — 20 mg, 200 mg
LITERATURE
Breinholt V, Arbogast D, Loveland P, et
al. Chlorophyllin chemoprevention: an evaluation of reduced
bioavailability vs. target organ protective mechanisms. Toxicol Appl
Pharmacol. 1999; 158:141-151.
Breinholt V, Hendricks J, Pereira C, et
al. Dietary chlorophyllin is a potent inhibitor of aflatoxin B1
hepatocarcinogenesis in rainbow trout. Cancer Res. 1995;
55:57-62.
Chernomorsky S, Segelman A, Poretz RD.
Effect of dietary chlorophyll derivatives on mutagenesis and tumor cell
growth. Teratogen Carcinogen Mutagen. 1999; 19:313-322.
Dashwood RH, Breinholt V, Bailey GS.
Chemopreventive properties of chlorophyllin: inhibition of aflatoxin B1
(AFB1)-DNA binding in vivo and antimutagenic activity against
AFB1 and two heterocyclic amines in the Salmonella mutagenicity assay.
Carcinogenesis. 1991; 12:939-942.
Nahata MC, Slencsak CA, Kamp J. Effect of
chlorophyllin on urinary odor in incontinent geriartric patients.
Drug Intell Clin Pharm. 1983; 17:732-734.
Ong TM, Whong WZ, Stewart J, Brockman HE.
Chlorophyllin: a potent antimutagen against environmental and dietary
complex mixtures. Mutat Res. 1986; 173:111-115.
Reddy AP, Harttig U, Barth MC, et al.
Inhibition of dibenzo[a,l]pyrene-induced multi-organ
carcinogenesis by dietary chlorophyllin in rainbow trout.
Carcinogenesis. 1999; 20:1919-1926.
Robins EW, Nelson RL. Inhibition of
1,2-dimethylhydrazine-induced nuclear damage in rat colonic epithelium
by chlorophyllin. Anticancer Res. 1989; 9:981-985.
Te C, Gentile JM, Baguley BC, et al.
In vivo effects of chlorophyllin on the antitumot agent
cyclophosphamide. Int J Cancer. 1997; 70:84-89.
Vlad M, Bordas E, Caseanu E, et al.
Effect of cuprofilm on experimental atherosclerosis. Biol Trace Elem
Res. 1995; 48:99-109.
Young RW, Beregi JS Jr. Use of
chlorophyllin in the care of geriatric patients. J Am Geriatr Soc.
1980; 28:46-47.
