Evidence-based Review of Medicinal Plants Used for the Treatment of Hemorrhoids
Hemorrhoidal disease is a common problem which is usually not managed properly with pharmacologic interventions and will eventually require surgery. However, there are many medicinal plants that were successfully used for the treatment of hemorrhoids in the traditional and folk medicine of different countries. In this study, these medicinal plants have been reviewed and their mechanism of action and their major chemical constituents responsible for their activities have been assessed individually. Among various herbal medicines, Aesculus hippocastanum, Boswellia species, Cissus quadrangularis, Euphorbia prostrata, Juniperus species, Melastoma malabathricum, Myrtus communis and Verbascum species have got higher support from scientific evidence. These medicinal plants may exert their beneficial effects in hemorrhoids by their anti-inflammatory, analgesic and venotonic activities. Several chemical constituents were identified in these plants which may be responsible for their pharmacological activities, of which, flavonoids, terpenoids, triterpenes and tannins are the majors.
Received: November 15, 2012;
Accepted: January 16, 2013;
Published: March 12, 2013
Hemorrhoids are vascular cushions with a thick submucosa involving
the smooth muscle, connective tissues and blood vessels around the anus. Any
enlargement, bleeding and protrusion of these cushions is responsible for pathologic
hemorrhoids (Thomson, 1975).
Many elements are involved in development of pathologic changes within the
hemorrhoidal cushions such as genetics, dysregulation in evacuation of the feces
like constipation or diarrhea, sustained strain due to several diseases or conditions
and aging. These issues lead to increased pressure within the submucosal arteriovenous
plexus and ultimately contribute to swelling of the cushions, laxity of the
supporting connective tissue and protrusion into and through the anal canal
(Sneider and Maykel, 2010; Lohsiriwat,
2012). Hemorrhoidal disease is a prevalent difficult, for instance, about
one million new cases are detected each year in the United States. The estimate
is that 5% of the general population is affected by symptoms from hemorrhoids,
with 50% of people over the age of 50 having experienced symptoms related to
hemorrhoids at some point in time (Sneider and Maykel,
2010). Current conventional treatment of hemorrhoids includes lifestyle
modification, pharmacologic therapies and surgery. Pharmacologic therapies include
drugs like calcium dobesilate as a venotonic agent, topical agents containing
anesthetics and corticosteroids and physical therapies such as ice and sitz
baths (Lohsiriwat, 2012). In the current years, medicinal
plants have been considered as potentially effective and more tolerable agents
for the treatment of different pathological conditions in the gastrointestinal
system from mouth to rectum (Rahimi and Abdollahi, 2012a;
Rahimi et al., 2009, 2010).
The medicinal plants with anti-bleeding, venotonic, anti-inflammatory and antinociceptive
activities may be useful for treatment of hemorrhoids. In this study, the medicinal
plants with any capacity used for the management of hemorrhoids have been criticized
and their possible mechanisms of action and their major chemical constituents
responsible for their activities have been appraised.
PLANTS FOR THE TREATMENT OF HEMORRHOIDS
Medicinal plants with antihemorrhagic activity and their possible mechanisms
of action and their components responsible for their activity have been discussed
below. Table 1-3 show in vitro, in
vivo and clinical studies related to their antihemorrhagic activity, respectively.
Aesculus hippocastanum L.: The seed of Aesculus hippocastanum
has been used in Europe to treat hemorrhoidal disease (Kucukkurt
et al., 2010; Anonymous, 2009).
|| In vitro studies on plants used in TIM for treatment
|Cox: Cyclooxygenase, ACh: Acetylcholine
|| In vivo studies on plants used in TIM for treatment
|EPP: Ethyl phenylpropiolate, TPA: 12-O-tetradecanoylphorbol-13-acetate
A clinical trial on A. hippocastanum confirmed that clinical and endoscopic
symptoms after average six days of administration to patients with acute symptomatic
hemorrhoids was improved (Pirard et al., 1976).
The key active component found in A. hippocastanum seed extract is aescin.
The aescin is a combination of triterpene saponins existing in two forms of
α and β. Of these two forms, β-aescin is the active one. Aesin
has anti-inflammatory, venotonic and anti-edematous activities (Sirtori,
Boswellia species: Gum resins of Boswellia species, particularly
B. serrata Roxb. ex Colebr. and B. carterii Birdw. have been used
in traditional Iranian medicine for the management of hemorrhoids (Arzani,
2005). There are many reports about the anti-inflammatory action of gum
resin and its major constituents, boswellic acids (Siddiqui,
2011; Ammon, 2006). Boswellic acids are pentacyclic
triterpenes with anti-inflammatory and anti-cancer activities (Poeckel
and Werz, 2006).
Cestrum species: Cestrum auriculatum L'Hér. and
C. hediundinum have been used in Peruvian traditional medicine for treatment
of hemorrhoids. These two species have shown in vivo analgesic effects
and in vitro anti-inflammatory activity (Kawano
et al., 2009).
Cissus quadrangularis Linn.: The C. quadrangularis, a
medicinal plant indigenous to Asia and Africa, is used for treatment of hemorrhoids.
C. quadrangularis demonstrated analgesic, anti-inflammatory and venotonic
activities. The analgesic property of C. quadrangularis is because of
inhibition of some local mediators and nociceptors in charge for pain in central
nervous system and likewise anti-inflammatory effects in the peripheral tissue
by reduction of the release and synthesis of related mediators, principally
prostaglandins (Panthong et al., 2007). Administration
of C. quadrangularis to patients with hemorrhoids condensed the magnitude
of hemorrhoids and relieved inflammation and pain (Segsunviriya
and Choomprabutra, 1989).
||Clinical studies on plants used in TIM for treatment of hemorrhoids
Commiphora species: Gum resins from Commiphora mukul (Hook.
ex Stocks) Eng. and C. myrrha (Nees) Engler. have been used as efficacious
plant materials for the treatment of hemorrhoids in traditional Iranian medicine.
C. myrrha showed anti-inflammatory and antinociceptive activities (Su
et al., 2011, 2012). Anti-inflammatory
activity C. mukul was demonstrated in vitro (Francis
et al., 2004). Terpenoids and guggulusteroids from C. mukul
showed potent anti-inflammatory activity (Francis et
al., 2004; Kimura et al., 2001).
Euphorbia prostrata aiton: A preliminary study showed that Euphorbia
prostrata can be used for the treatment of grade I and II of hemorrhoids
with satisfactory efficacy and safety (Gupta, 2011).
The mechanisms of action of this plant in hemorrhoids include an increase in
lymphatic drainage, reduction in capillary permeability, improvement of venous
tone, protection of capillary bed microcirculation and inhibition of inflammatory
reactions. As reported, flavonoids in Euphorbia are robust inhibitors of thromboxane
A2, prostaglandin E2 and leukocyte stimulation, relocation and adhesion (MacKay,
2001). Studies with the standardized extract of E. prostrata, when
administered orally showed an inhibition of both carrageenan-induced paw edema
and histamine-induced edema (Singla and Pathak, 1990).
Ellagic acid is another major constituent of E. prostrata extract and
has been reported to suppress the histamine release (Choi
and Yan, 2009).
Ginkgo biloba L.: Ginkor-fort®, a commercial product
from Ginkgo biloba leave extract in combination with troxerutin (a flavonoid)
and heptaminol (a vasodilator) showed beneficial effects in patients with hemorrhoids
(Sumboonnanonda and Lertsithichai, 2004; Hep
et al., 2000; Soullard and Contou, 1978).
Ginkgo biloba may exert their beneficial effects in hemorrhoids by its
anti-inflammatory and venoprotective activity (Chan et
Juniperus species: Several juniperus species are used as a remedy
for hemorrhoids in Turkish folk medicine. Between 5 different species of Juniperus,
only methanol extracts of fruit and leaves from J. oxycedrus subsp. oxycedrus
and J. communis var. saxatilis showed significant antinociceptive
and anti-inflammatory activities (Akkol et al.,
2009). Among different compounds present in Juniperus species, diterpenoids
such as hinokiol isolated from J. polycarpos was shown to exert anti-inflammatory
activity (El-Sayed, 1998). Nevertheless, the active
antinociceptive and anti-inflammatory constituents in other Juniperus
species have not been deliberated yet.
Melastoma malabathricum L.: The powdered leaves and roots have
been used to relieve the discomfort of hemorrhoids in Malay folk medicine. The
flower has been also used for hemorrhoidal bleeding. The antinociceptive, anti-inflammatory
and wound remedial activities of this plant were demonstrated by various in
vivo studies (Zakaria et al., 2006; Susanti
et al., 2008; Sulaiman et al., 2004;
Sunilson et al., 2008). The reported activities
may be attributed to different chemical constituents identified in this plant
such as flavonoids and tannins (Joffry et al., 2012).
Myrtus communis L.: Myrtus communis is a medicinal plant
used in traditional Iranian medicine for treatment of hemorrhoids (Aghili,
2009). Anti-inflammatory and antinociceptive activities of M. communis
have been evaluated in several studies (Al-Hindawi et
al., 1989; Hosseinzadeh et al., 2011;
Amira et al., 2012). Flavonoids are one of the
major components of this plant and may play the chief role in these pharmacological
properties of M. communis (Montoro et al.,
Onosma species: Onosma species are used for the treatment
of hemorrhoids in Turkish folk medicine. Screening of different Onosma species
for their anti-inflammatory and antinociceptive effects demonstrated significant
activity of O. isauricum, O. sericeum and O. aucheranum
(Tosun et al., 2008). Onosmins as flavonoid
type compounds in Onosma species were found to inhibit lipoxygenase enzyme
activity (Ahmad et al., 2005). Moreover, in the
root barks of several Onosma species accumulation of naphthaquinones
of alkannin and shikonin derivatives have been reported. These compounds possess
significant anti-inflammatory activity (Kundakovic et
al., 2006; Tanaka et al., 1986).
Phlomis species: Phlomis species has been used in Spanish
folk medicine for treatment of hemorrhoids (Limem-Ben Amor
et al., 2009). There are some reports on antinociceptive and vascular
protective effects of Phlomis species (Sarkhail et
al., 2003; Mohajer et al., 2005; Ismailoglu
et al., 2002). Two phenyl propanoid compounds including forsythoside
B and alyssonoside may play the major role in vascular protective activity of
this plant (Ismailoglu et al., 2002). These
species also contain a considerable amount of flavonoids, which show beneficial
effects in treatment of hemorrhoids (Limem-Ben Amor et
Plantago ovata Forssk: Results of clinical trials showed the
beneficial effects of seed husk from Plantago ovata on patients with
hemorrhoids (Webster et al., 1978; Moesgaard
et al., 1982; Perez-Miranda et al., 1996).
The seed husk of Plantago can reduce bleeding, improve the symptoms and
reduce hemorrhoidal cushions. Plantago was also used for posthemorrhoidectomy
complications. As reported, treatment of patients with P. ovata after
open hemorrhoidectomy diminished tenesmus rate, pain and markedly shortened
postoperative hospital halt (Kecmanovic et al.,
2006). P. ovata is a bulking laxative and causes softening of stool.
It also exerts its beneficial effects by producing fairly large amounts of short-chain
fatty acids. Anaerobic fermentation of the soluble non-starch polysaccharides
from Plantago seed results in the production of the propionate, butyrate
and acetate in the intestines. These fatty acids may play a critical role in
balancing of normal flora of colon and reducing inflammation of the anorectal
region (Anonymous, 2002).
Verbascum species: Different species of Verbascum have
been used to treat hemorrhoids in traditional Turkish medicine. Aqueous extract
of the V. mucronatum flower has shown anti-inflammatory, antinociceptive
and wound healing activities. Fractionation of this extract demonstrated that
iridoid glycosides, especially verbascoside are responsible for these activities
(Akdemir et al., 2011). Besides V. mucronatum,
other species of Verbascum including V. latisepalum and V.
salviifolium, V. lasianthum, V. pterocalycinum var. mutense
and V. salviifolium displayed significant antinociceptive and anti-inflammatory
activities (Tatli et al., 2008a, b;
Kupeli et al., 2007a). Methanol extract of
V. lasianthum showed significant anti-inflammatory and antinociceptive activity.
Fractionation of these extract leads to isolation of different iridoid glycosides
of which, aucubin and ilwensisaponin A were found responsible for the mentioned
pharmacological activities (Kupeli et al., 2007b).
Traditional and folk medicines of different countries are an invaluable source
to discovery of effective drugs with lower incidence of side effects in modern
medicine (Rahimi et al., 2010, 2012;
Rahimi and Ardekani, 2013). Many of medicinal plants
discussed in this study for the management of hemorrhoids have historical backgrounds
in traditional medicine for this application. The medicinal plants can improve
the symptoms of hemorrhoids such as pain, bleeding, itching, heaviness and tenesmus,
rectal prolapse, number of hemorrhoidal cushions and recurrence and increase
the rate of wound healing. Their mechanisms of action include anti-inflammatory,
anti-nociceptive, venotonic and venoprotective activities or even stool softening
by absorption of water absorption as observed for Plantago ovata. As
shown in Table 4, different classes of compounds, especially
flavonoids, triterpenes, tannins and terpenoids may be responsible for anti-hemorrhoidal
activity. The chemical structures of some of the natural compounds which may
have a role in treatment of hemorrhoids have been shown in Fig.
1. There are some products from flavonoids in the market; the most popular
of them is Daflon, hesperidin in combination with diosmin. A meta-analysis of
14 clinical trials on the use of flavonoids for the treatment of hemorrhoids
indicated that flavonoids improve symptoms such as bleeding, persistent pain
and itching (Alonso-Coello et al., 2006). The
exact mechanisms of action of flavonoids remain unclear but the possible ones
are refining venous tone, boosting lymphatic drainage, dropping capillary hyperpermeability
along with anti-inflammatory activities (Meyer, 1994).
There are several plants in traditional Chinese medicine used for stopping
bleeding from hemorrhoids and their efficacy has been supported by some clinical
trials; but because their scientific names had not been determined in these
papers and only it has been implied in their Chinese names; we could not consider
them (Gan et al., 2010).
Medicinal plants used for treatment of hemorrhoids can also be used for post-hemorrhoidectomy
complications such as pain and bleeding thus reducing the use of chemical analgesics
and increasing wound healing rate (Rahimi and Abdollahi,
The problem of current medicinal plants in treatment of hemorrhoids is that
most of them although have traditional use history but lack enough evidence
needed for approval as a new drug in the current time. This means that most
of the studies have been in vitro or in vivo but in a systematic
manner and thus there are many gaps in their efficacy and safety profile. So
the first recommendation is to complete efficacy and safety profile of these
plants and then go through clinical trials to prove their efficacy. In the meantime,
mixture of these medicinal plants may be more useful by possible synergism that
needs to be elucidated.
||Chemical structures of some natural compounds found beneficial
in the treatment of hemorrhoids, (a) Aesin, (b) Beta-boswellic acid, (c)
Alpha-Boswellic acid, (d) Ellagic acid, (e) Hinokiol, (f) Shikonin, (g)
Forsythoside B, (h) Lamiide, (i)Alyssonoside, (j) Aucubin, (k) Hesperidin,
(l) Diosmin, (m) Troxerutin (n) Kaempferol-3-glucoside, (o) Alpha-Amyrin
and (p) Onosmin B
|| Chemical constituents of medicinal plants responsible for
their anti-hemorrhoidal activity
Final notice is that medicinal plants are the valuable source of preparing
new drugs for hemorrhoidal disease, but they need to be considered by scientists
to go through scientific efficacy and safety tests.
Authors acknowledge assistance of Iran National Science Foundation.
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