| However, these herbs don't
address the fundamental problem: the actual increase in the volume of
the prostate gland itself. Despite what you hear, clinical trials have
repeatedly documented that saw palmetto has no effect on prostate
volume. The German Commission E Monographs are careful to spell this
out, if most supplement hawkers are not: saw palmetto "relieves only the
symptoms associated with an enlarged prostate without reducing the
enlargement." And it's the same with the others.
Because of this, the Monograph for saw palmetto advises users to
"Please consult a physician at regular intervals." The reason: even as
their symptoms are relieved, saw palmetto allows the prostate to
continue to grow, so that surgery may eventually become necessary.
Indeed, experience with drugs which relieve BPH symptoms without
addressing prostate volume (such as alpha 1 -adrenergic blockers (eg
Hytrin® or Flomax®)) has shown that, lacking any warning symptoms, men
often put off surgery for far too long, leading to concern that these
treatments may actually increase the complications of BPH.
By contrast, there is plenty of evidence that finasteride (Proscar®),
the most famous drug therapy for BPH, can reduce prostate volume.
Unfortunately, finasteride takes a long time to relieve symptoms, does
not work with several classes of patients, is very expensive, and has
significant side effects, including erectile dysfunction and loss of
libido. Furthermore, despite long-standing hopes that this drug would
reduce the risk of prostate cancer because of its ability to reduce
levels of the cancer marker prostate-specific antigen (PSA), the first
clinical trial to test this hypothesis has found that finasteride has
pretty muddled results: it decreases the overall risk of prostate cancer
- but increases the risk of the most aggressive, deadly forms of the
disease.
So men find themselves pinned on the horns of a serious dilemma:
symptomatic improvement with no halt to the loss of prostate health, or a
treatment which addresses the core problem, but causes problems of its
own.
The Real Prostate Health Alternative
Defined
pollen extract is different. While still new to Canadians, defined
pollen extract been used with success by two generations of European
men. Defined pollen extract is not bee pollen. Bee pollen is a mixture
of whatever pollens with which the insects happen to have come into
contact. Defined pollen extract, by contrast, is a mixture of several
specific pollen sources (primarily rye, but also including timothy
grass, corn, hazel, sallow, aspen, oxye, and pine pollens). Also, bee
pollen in its raw form is covered with a microscopic husk which prevents
its full assimilation by humans; by contrast, defined pollen extract
uses a precise process to isolate the key fractions from the pollen,
incorporating a specific 20:1 ratio of lipid- and water-soluble
components extracted under low-temperature conditions, bypassing the
pollen's protective sheath.
Proven in Controlled Trials
In contrast to saw
palmetto and the other standard prostate botanicals, four randomized,
double-blind, controlled clinical trials have shown that defined pollen
extract quickly improves prostate symptoms and reduces prostate volume.
In one of these studies, sixty men with symptomatic BPH received either
the pollen extract or placebo for six months. Sixty-nine percent of men
receiving the pollen extract experienced improved overall symptoms,
compared to less than a third of the placebo group. There were
statistically significant differences in the number of incidences of
nocturia, decreased leftover urine in the bladder after urination
("residual urine volume"). Compared to the placebo group, there were
also more improvements reported by men receiving the pollen extract in
hesitancy (inability to release urinary flow) and intermittency, but
these results were not strong enough, in this small a group over this
short a period, to be statistically meaningful.
But most importantly, this study reported that men using defined
pollen extract experience significant reductions in the volume of the
prostate as measured by ultrasound. In fact, every trial of defined
pollen extract in men with BPH, which has measured prostate volume,
size, or weight has reported significant reductions in the gland.
Proven More Effective than Other Botanicals
How
do these results stack up to the common prostate herbals? Very well,
thank you. In a head-to-head trial against Tadenan® (the best-studied
and most famous brand of Pygeum africanum in Europe), Dutkiewicz
reported that 78% of the men in the pollen extract group experienced
subjective improvements, versus "only" 55% of the Pygeum group. Another
trial compared it with Paraprost. Significant improvements in residual
urinary volume, flow rate, and (again, most importantly) prostatic
weight were seen in the pollen extract group as compared to the
Paraprost group; the lenth of time required to urinate was also better,
although the improvement did not meet the statistical test of significe.
The most impressive comparison is that with beta-sitosterol - both
because beta-sitosterol is perhaps the most rigorously studied of all
the common prostate health herbals, and because of the unique insight
the trial yielded about the power of the pollen extract. The trial found
that greater relief was experienced by men in the pollen extract group
in their subjective symptoms, painful urination, and frequent urination,
while the two groups demonstrated equal improvements in straining,
urinary volume, residual volume, and intermittency.
Also important was the fact that this trial was the first to measure
the effect of these two supplements on levels of prostate-specific
antigen (PSA - a marker used to detect prostate cancer) and prostatic
acid phosphatase (PAP - an enzyme which is elevated in many prostatic
dysfunctions). Men supplementing with defined pollen extract experienced
significant reductions in both PAP and PSA, whereas no significant
change was reported in the beta-sitosterol group. In still another
trial, defined pollen extract demonstrated its superiority to the amino
acid mixture Paraprost.
Other Prostate Health Concerns
BPH, of course, is
not the only prostate disorder that men may face. Others include
chronic prostatitis (CP) and prostatodynia. Because the symptoms of
these disorders sound similar, many men with CP or prostatodynia
mistakenly self-medicate with saw palmetto. And unfortunately, the
relative ignorance of many mainstream MDs about the herbal pharmacy
leads them to give the go-ahead for this useless course of action -
useless, because there is no evidence that saw palmetto or the other
common herbals for BPH are helpful for these conditions. By contrast,
several open trials have found that defined pollen extract is helpful in
chronic prostatitis and prostatodynia.
Hope for Prostate Cancer
An even graver prostate
health concern for many men is prostate cancer. Autopsy studies show
that 15 to 30% of men over 50, and 60 to 70 percent of men over the age
of 80, have latent, undiagnosed prostate cancer. There has been exciting
progress made in the last few years in the discovery of natural ways of
reducing the risk of prostate cancer, including successful
double-blind, placebo-controlled trials with selenium, and extremely
promising preliminary result with the carotenoid lycopene.
While it's far too soon to be sure, preliminary evidence suggests the
possibility that defined pollen extract may yet prove to be a safe,
natural herb to help the fight against the second greatest cause of
cancer death in men. Much of this evidence comes from studies in
isolated prostate cancer cells, which have found that fractions of the
pollen extract selectively inhibit the growth of human prostate cancer
cells.
Another hint that defined pollen extract may protect men from this
scourge is the finding - from the controlled clinical trial mentioned
earlier - that defined pollen extract lowers PSA, considered a marker of
prostate cancer risk. As the results with finasteride have shown, the
reduction in PSA does not itself guarantee a corresponding reduction in
risk; however, the results are certainly promising, and many men are
taking these preliminary results into account when considering which
prostate botanical to use.
How Does it Work?
The mechanism of action of
defined pollen extract remains elusive. Molecular, experimental,and
clinical studies suggest that defined pollen extract may reduce
inflammation and balance the muscle tone of the urethra and bladder -
effects which might help to explain some of the extract's effects on the
symptoms of BPH.
But the exact method by which the defined pollen extract exerts its
most exciting influence on the prostate - namely, its ability to reduce
the actual volume of the prostate - remains unknown. Proscar,® the most
successful drug therapy for BPH, reduces prostate volume by inhibiting
5-a-reductase (5AR), the enzyme which converts testosterone into the
much more prostate-stimulating dihydrotestosterone (DHT). In test-tube
studies, defined pollen extracts do inhibit 5AR; however, they also
inhibit the less-known hydroxysteroid oxioreductase (HSORred) enzymes,
which convert DHT to the less-stimulating 3-alpha- and 3-beta-diol. In
other words, the pollen extract directly decreases both the synthesis
and the clearance of DHT. What the end result of this would be is
unclear, but the net effect on DHT activity levels in the prostate could
very well be zero. Clearly, more studies are needed, but direct
inhibition of DHT may not be a key mechanism of the pollen's activity.
Further studies are clearly needed. All we can say with certainty,
from existing evidence, is that defined pollen extract works, relieving
the symptoms of BPH and reducing prostate volume. How it works is a
question for continued scientific investigations.
Not Just for the Prostate... And Not Just for Men!
Most
people taking the pollen extract are using it for the health of their
prostate, which is by far the best-backed usage for this botanical. Yet
there are hints in the literature of a broad range of other applications
which get much less attention. One such property is detoxification and
hepatoprotection. Animal studies have found that the defined pollen
extract provides protection against a variety of liver toxins, including
as ammonium fluoride, paracetamol, organic solvents, allyl alcohol, the
deadly carbon tetrachloride, cadmium, and galctosamine.
Finally, although we emphasize that the evidence is purely anecdotal,
in some parts of the world more women buy defined pollen extracts than
men, because they have found that the pollen extract helps with urinary
incontinence - which, although unproven by clinical trials, is
consistent with the improved bladder and urethral smooth muscle tone
balance, which the pollen extract is known to afford. Funding is
presently being sought to run a controlled trial on this application.
The Future of Prostate Care
Proscar® and other
drugs for BPH are effective, but come with side effects and a cost which
make drug therapy unattractive to many men. The natural alternatives
commonly found on health food store shelves may help relieve symptoms,
but do not ultimately address the underlying cause. Defined pollen
extract has been effectively helping European men with many prostate
health problems for decades now, and is proven to do what no other
herbal can: shrink swollen prostates. As the pollen itself is golden, so
defined pollen extract may open up a golden age for safe, natural
therapy for the most personal of male health concerns.
References
Buck AC, Cox R, Rees RW,
Ebeling L, John A. Treatment of outflow tract obstruction due to benign
prostatic hyperplasia with the pollen extract, cernilton. A
double-blind, placebo-controlled study. Br J Urol. 1990 Oct; 66(4):
398-404.
Dutkiewicz S. Usefulness of Cernilton in the treatment of benign prostatic hyperplasia. Int Urol Nephrol. 1996; 28(1): 49-53.
Maekawa M, Kishimoto T,
Yasumoto R, Wada S, Harada T, Ohara T, Okajima E, Hirao Y, Ohzono S,
Shimada K, et al. Clinical evaluation of cernilton on benign prostatic
hypertrophy - a multiple center double-blind study with Paraprost.
Hinyokika Kiyo. 1990 Apr; 36(4): 495-516.
Ebeling L. Therapeutic results
of defined pollen-extract in patients with chronic prostatis or BPH
accompanied by chronic prostatitis. In , Schmiedt E, Alken JE, Bauer HW
(eds). Therapy of Prostatitis. Munich: Zuckerschwerdt Verlag, 1986;
154-60.
Brauer H. The treatment of
benign prostatic hyperplasia with phytopharmata: a comparative study of
cernilton vs. beta-sitosterol. Therapiewoche. 1986; 36: 1686-96.
Yasumoto R, Kawanishi H,
Tsujino T, Tsujita M, Nishisaka N, Horii A, Kishimoto T. Clinical
evaluation of long-term treatment using cernitin pollen extract in
patients with benign prostatic hyperplasia. Clin Ther. 1995 Jan-Feb;
17(1): 82-7.
Becker H, Ebeling L.
Phytotherapy of BPH with cernilton N - results of a controlled
prospective study. Urologe (B) 1991; 31: 113-6.
Roberts KP, Iyer RA, Prasad G,
Liu LT, Lind RE, Hanna PE. Cyclic hydroxamic acid inhibitors of
prostate cancer cell growth: selectivity and structure activity
relationships. Prostate. 1998 Feb 1; 34(2): 92-9.
Jaton JC, Roulin K, Rose K,
Sirotnak FM, Lewenstein A, Brunner G, Fankhauser CP, Burger U. The
secalosides, novel tumor cell growth inhibitory glycosides from a pollen
extract. J Nat Prod. 1997 Apr; 60(4): 356-60.
Zhang X, Habib FK, Ross M,
Burger U, Lewenstein A, Rose K, Jaton JC. Isolation and characterization
of a cyclic hydroxamic acid from a pollen extract, which inhibits
cancerous cell growth in vitro. J Med Chem. 1995 Feb 17; 38(4): 735-8.
Blumenthal M (ed). The
Complete German Commission E Monographs. Therapeutic Guide to Herbal
Medicines. Austin, TX: American Botanical Council, 1998.
Treatment of outflow tract obstruction due to benign
prostatic hyperplasia with the pollen extract, cernilton. A
double-blind, placebo-controlled study.
Br J Urol 1990 Oct; 66(4): 398-404.
Buck AC, Cox R, Rees RW, Ebeling L, John A.
Whilst prostatectomy remains the "gold standard" for the treatment of
outflow tract obstruction due to benign prostatic hyperplasia, medical
treatment-if only for symptomatic relief--appears to be an attractive
alternative. Most of the pharmacological agents in use block the
hormonal or the sympathetic neurological pathways that influence
prostate growth and function. All of these drugs are known to have side
effects. Sixty patients with outflow obstruction due to benign prostatic
hyperplasia (BPH) were entered into a double-blind, placebo-controlled
study to evaluate the effect of a 6-month course of the pollen extract,
Cernilton. There was a statistically significant subjective improvement
with Cernilton (69% of the patients) compared with placebo (30%). There
was a significant decrease in residual urine in the patients treated
with Cernilton and in the antero-posterior (A-P) diameter of the
prostate on ultrasound. However, differences in respect of flow rate and
voided volume were not statistically significant. It is concluded that
Cernilton has a beneficial effect in BPH and may have a place in the
treatment of patients with mild or moderate symptoms of outflow
obstruction.
Usefulness of Cernilton in the treatment of benign prostatic hyperplasia.
Int Urol Nephrol 1996; 28(1): 49-53.
Dutkiewicz S.
A total of 89 patients with benign prostatic hyperplasia (BPH) were
treated pharmacologically for 4 months: 51 received Cernilton and 38
Tadenan [Pygeum africanum] (controls). Significant subjective
improvement was found in 78% of the patients in the Cernilton group
compared to only 55% of the Tadenan-treated patients. The obstructive
and irritative symptoms responded best to the therapy. In the
Cernilton-treated patients a significant improvement in the uroflow
rate, decrease in residual urine and in prostate volume were found. This
study shows that Cernilton is an effective therapy for patients with
BPH.
Clinical evaluation of cernilton on benign prostatic hypertrophy--a multiple center double-blind study with
Paraprost.
Hinyokika Kiyo 1990 Apr; 36(4): 495-516.
Maekawa M, Kishimoto T, Yasumoto R, Wada S, Harada T, Ohara T, Okajima E, Hirao Y, Ohzono S, Shimada K, et al.
A multiple center double blind study was performed to study the
effectiveness of Cernilton (CN) on benign prostatic hypertrophy in
comparison to Paraprost (PP). Among a total of 192 patients, overall
effect was studied on 159 patients, overall safety rate on 178 patients
and rate of effectiveness on 159 patients. There were no differences
between the two groups in the selected patients, criteria for exclusion
and drop out cases or background data of the patients. Impression of
patients and overall effect by committee and physician judgment were
slightly higher in the CN group compared to the PP group, but there was
no significant difference between the two groups. For the improvement in
subjective symptoms, the rate of moderate improvement or more after 4
weeks by committee judgement was higher in the CN group compared to the
PP group. The rate of improvement in protracted miction, which is an
effective marker of urinary disturbance, was also higher in the CN group
compared to the PP group. An analysis of objective symptoms showed a
significant improvement in residual urinary volume, average flow rate,
maximum flow rate and prostatic weight in the CN group. A significant
improvement in the phased change of residual urinary volume was also
seen in the CN group. No side effects or abnormalities in clinical test
levels were noted in the CN group. By committee judgement, the rate of
more than moderate effectiveness was 49.1% in the CN group compared to
41.2% in the PP group, but there was no significant difference between
the two groups. By physician's judgment, the rate of more than moderate
effectiveness was 49.4% in the CN group compared to 46.3% in the PP
group, but there was also no significant difference between the two
groups. These results suggested that Cernilton was an effective drug for
benign prostatic hypertrophy.
Therapeutic results of defined pollen-extract in patients with chronic prostatis or BPH accompanied by chronic prostatitis.
In Schmiedt E, Alken JE, Bauer HW (eds). Therapy of Prostatitis. Munich: Zuckerschwerdt Verlag, 1986; 154-60.
Ebeling L.
Objective(s): The purpose of this study was to
control the acceptance and effectiveness of pollen-extract on patients
with chronic prostatic complaints.
Study Population: 2,289 total patients prostatitis; 1,116 with BPH, 590 with BPH and prostatitis, 583 with chronic prostatitis alone
Study Design:
Open field study. The subjects were divided into three groups, 583
cases chronic prostatitis (P), 590 cases BPH accompanied by prostatitis
(BP), and 1116 cases BPH (B). The pollen-extract treatment was provided
in 84% of the cases with a dosage of 3x2 tablets/day in the first week
and continued in 78.5% with 3x2 tablets/day for up to 12-weeks.
Palpation, residual urine volume, peak urine flow, urine volume voided,
flow time and leukocytes in the prostatic secretions were performed
before and after treatment.
Test Results: The
palpated size of the prostate greatly disappeared in the BP-group and
the B-group's and the P-group's reduction was 55.9%. The leukocytes in
the pro-static secretion decreased significantly in all groups. The
residual urine volume decreased in all stages and showed a continuous
drop in the course of treatment. The peak urine flow rate increased in
all groups with the urine volume flow voided increased and flow time was
reduced. The general assessment of the patients and physicians was good
to very good.
Side Effects: There was a mild and temporary GI tract upset in 66 cases and in 1.2% of the cases treatment was stopped.
Conclusion(s):
The results of this study suggest the logical use of the pollen-extract
in the treatment of nonpathogen dependent chronic prostatitis,
prostatodynia. prostatic congestion. BPH with and without concomitant
prostatitis and TURP-prostatitis.
The treatment of benign prostatic hyperplasia with phytopharmata: a comparative study of cernilton vs. beta-sitosterol.
Therapiewoche. 1986; 36: 1686-96.
Brauer H.
The conservative tretment of benign prostatic hyperplasia (BPH) has
gained increasingly in significance in view of the increased life
expectancy. In a controlled comparative study (n-39) with Cernilton and
beta-sitosterol the course of treatment was objectified by
clinical-chemical findings. The results demonstrate the marked
improvement of symptoms and signs, whereas the regression of complaints
was more pronounced under Cernilton. The significant decrease of
prostate alkaline phosphatase (PAP) and prostate specific antigen (PSA)
serum levels shows the reduction of cell lesions in BPH under the
treatment with Cernilton. A comparable effect of beta-sitosterol could
not be demonstrated. The relative lack of toxicity of both drugs can be
confirmed by the biochemical data.
Clinical evaluation of long-term treatment using cernitin pollen extract in patients with benign prostatic hyperplasia.
Clin Ther 1995 Jan-Feb; 17(1): 82-7.
Yasumoto R, Kawanishi H, Tsujino T, Tsujita M, Nishisaka N, Horii A, Kishimoto T
Seventy-nine patients with benign prostatic hyperplasia (BPH) were
treated with cernitin pollen extract. Patient ages ranged from 62 to 89
years (mean, 68 years). Mean baseline prostatic volume was 33.2 cm3.
Cernitin pollen extract was administered in a dosage of 126 mg (2
tablets, 63 mg each), three times a day, for more than 12 weeks. Symptom
scores, based on a modified Boyarsky scoring scale, uroflowmetry,
prostatic volume, residual urine volume, and urinalysis results were
examined before and after administration of cernitin pollen extract.
Symptom scores significantly decreased from baseline, and the favorable
results continued during the treatment period. Urine maximum flow rate
and average flow rate increased significantly from 9.3 mL/s to 11 mL/s
and from 5.1 mL/s to 6 mL/s, respectively. Residual urine volume
decreased significantly from 54.2 mL to less than 30 mL. There was no
change in prostatic volume. However, 28 patients treated for more than 1
year showed a mean decrease of prostatic volume to 26.5 cm3. No adverse
reactions were observed. Clinical efficacy at 12 weeks was rated
excellent, good, satisfactory, and poor in 11%, 39%, 35%, and 15% of
patients, respectively. Overall clinical efficacy was 85%. In
conclusion, cernitin pollen extract showed a mild beneficial effect on
prostatic volume and urination variables in patients with symptomatic
BPH.
Phytotherapy of BPH with cernilton N - results of a controlled prospective study.
Urologe (B) 1991; 31: 113-6.
Becker H, Ebeling L.
The efficacy and tolerance of the pollen extract preparation,
Cernilton N, were investigated in a double blind, placebo-controlled
study carried out over a treatment period of 12 weeks in 6 urological
practices, in a total of 103 patients suffering from benign prostatic
hyperplasia (BPH) in stages II and III. The investigational parameters
were the disturbances of micturition classified according to the FDA
recommendation, residual urine volume, palpation findings, uroflow as
well as the global assessment of the therapy by the physician and by the
patient. Under the pollen extract, nocturia, the principal symptom of
BPH, improved in 68.8% of the cases, compared with 37.2% under the
placebo medication (p<0.005). Notable differences were observed in
frequency and in sensation of residual urine, which were statistically
significant as regards absence of these symptoms after the treatment,
between the active treatment (AT) and placebo (Pl) (p=0.010 and p=0.016,
respectively). Observation of the course of the symptoms after 6 weeks
and 12 weeks showed higher rates of improvement under the active
treatment, for all the individual symptoms. In the case of the
urodynamic study parameters, similar changes were observed in the
findings for all the uroflow parameters, whereby the differences between
the comparative groups were unremarkable. At the control examination
after 6 weeks a continuous increase in the peak urine flow was observed,
averaging 3.3ml/sec under active treatment and 0.9ml/sec under placebo
(p=0.060). The difference in the average decrease in the residual urine
volume in the course of the treatment was statistically significant
(AT/Pl: 24.3ml/3.7ml; p=0.006). The pollen extract led to a continuous
reduction, whereas in the placebo group the residual urine after 12
weeks had increased in comparison with the value recorded after 6 weeks.
Significant differences in the residual urine volumes before and after
the treatment, in favor of the pollen extract, were observed also in the
patients in BPH stage III (p=0.042). Prostate size and congestion
showed higher response rates, in the sense of reduction in size and
decongestion, as detected by palpitation, under the active treatment,
with a marked trend (AT/Pl: 88.5%/69.0%; p=0.155). Nausea was recorded
under active treatment in one case. In accordance with their positive
experiences with the treatment, the investigating physicians and the
patients assessed the therapeutic result under the pollen extract as
very good or good significantly more often than that obtained under
placebo (p=0.001). The results of the study prove the efficacy of the
pollen extract in patients with BPH in stages II and III, in regard to
clinical symptomatology, urodynamics and global assessment, and
demonstrate the good tolerability of the drug, which permits long-term
therapy with little risk of side effects.
Cyclic hydroxamic acid inhibitors of prostate cancer cell growth: selectivity and structure activity relationships.
Prostate 1998 Feb 1; 34(2): 92-9.
Roberts KP, Iyer RA, Prasad G, Liu LT, Lind RE, Hanna PE.
BACKGROUND: Clinical symptoms of prostatitis,
prostatodynia, and benign prostatic hyperplasia are relieved by the
pollen extract cernilton, and the water-soluble fraction of this extract
selectively inhibits growth of some prostate cancer cells. A cyclic
hydroxamic acid, DIBOA, has been isolated from this extract and mimics
its cell growth-inhibitory properties, but the specificity of DIBOA for
inhibition of prostate cell growth has not been reported.
METHODS:
The in vitro growth inhibitory effects of DIBOA and nine structurally
related compounds on DU-145 prostate cancer cells, MCF-7 breast cancer
cells, and COS-7 monkey kidney cells were determined by treatment of the
cells with various concentrations of the compounds for 2-6 days.
RESULTS:
The compounds exhibited a wide range of potencies, but none of them
exhibited selective inhibition of DU-145 cell growth. MCF-7 cells were
more sensitive to DIBOA than either DU-145 cells or COS-7 cells.
3,4-dihydroquinoline 2(1H)-one, compound (4), and
1-hydroxy-6-chloro-3,4-dihydroquinolin-2(1H)-one, compound (7),
selectively inhibited MCF-7 cell growth at a concentration of 10
micrograms/ml. 1-hydroxy-3,4-dihydroquinolin-2(1H)-one, compound (3),
and compound 7 were the most potent inhibitors of DU-145 cell growth.
Treatment of DU-145 cells with 3 (100 micrograms/ml) substantially
decreased the number of viable cells within 2 days, and no viable cells
remained in the culture by day 4.
CONCLUSIONS: It
is unlikely that DIBOA, compound (1), is responsible for the selective
growth inhibition of prostate cancer cells by the water-soluble fraction
of the pollen extract cernilton. Cell morphology results indicate that
the growth-inhibitory effects of DIBOA and structurally related agents
on DU-145 cells are due to their ability to cause cell death.
The secalosides, novel tumor cell growth inhibitory glycosides from a pollen extract.
J Nat Prod 1997 Apr; 60(4): 356-60.
Jaton JC, Roulin K, Rose K, Sirotnak FM, Lewenstein A, Brunner G, Fankhauser CP, Burger U.
The pollen of rye (Secale cereale) was shown to contain a
biologically highly active family of glycosides called the secalosides.
Secalosides A and B (1), both of molecular formula C46H51-NO24, were
found to be epimeric esters of (2-oxo-3-indolyl)acetic acid (4). They
are made up, in addition to this heterocyclic aglycon I (4), of three
hexose building blocks and a carbocyclic aglycon II, which is an
indan-derived dicarboxylic acid (5). In aqueous solution, secalosides A
and B interchanged by epimerization at the chiral center of 4. A further
epimeric pair, secalosides C and D (2), contain one additional glucose
building block. Secalosides A and B, the racemic aglycon I (4), and
2-oxo-1,2,3, 4-tetrahydroquinoline-4-carboxylic acid (3), which results
from 4 by hydrolytic rearrangement, exhibited significant antitumor
activity against S180 sarcoma in vivo. IC50 values obtained were about 5
micrograms/mouse for the secalosides and 1 microgram/mouse for 3 and 4.
Isolation and characterization of a cyclic hydroxamic acid from a pollen extract, which inhibits cancerous cell growth in vitro.
J Med Chem 1995 Feb 17; 38(4): 735-8.
Zhang X, Habib FK, Ross M, Burger U, Lewenstein A, Rose K, Jaton JC.
One fraction, designated FV-7, in the water soluble ingredient of the
pollen extract cernilton was found to be inhibitory to the growth of a
prostate cancer cell line. Characterization of FV-7 by high-resolution
mass spectrometry and nuclear magnetic resonance identified the fraction
as hydroxamic acid, 2,4-dihydroxy-2H-1,4-benzoxazin-3(4H)-one (DIBOA).
To confirm this further, we synthesized an authentic sample of DIBOA and
found subsequently that the synthetic DIBOA was structurally
indistinguishable from FV-7. Furthermore, in a separate experiment we
compared the in vitro effects of FV-7 and DIBOA on the growth of a
prostate cancer cell line and found that in both cases the effect was
inhibitory and that the inhibition curves obtained for both compounds
were virtually identical.
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