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Dietary, Anticancer and Medicinal Properties of the Phytochemicals in Chili

Pepper (Capsicum spp.)

Article  in  Ceylon Journal of Science (Biological Sciences) · September 2016

DOI: 10.4038/cjs.v45i3.7396

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Ceylon Journal of Science 45(3) 2016: 5-20
DOI: http://doi.org/10.4038/cjs.v45i3.7396

REVIEW ARTICLE

Dietary, Anticancer and Medicinal Properties of the Phytochemicals in

Chili Pepper (Capsicum spp.)
M.D.M. Chamikara1,2, D.R.R.P. Dissanayake1, M. Ishan1,3 and
S.D.S.S. Sooriyapathirana1,*
1
Department of Molecular Biology and Biotechnology, Faculty of Science, University of Peradeniya,
Peradeniya, Sri Lanka
2
Current Address: Structural Biology and Biophysics Laboratory, Research School of Chemistry, Australian
National University, Pauline Griffin Building, [11], Canberra ACT 0200, Australia
3
Current Address: Regenerative Bioscience Center, Department of Animal and Dairy Science, University of
Georgia, Athens, GA-30602, USA

Received: 01/04/2016; Accepted: 15/09/2016

Abstract: Chili pepper (Capsicum spp.) is important dried fruit (FAO, 2015).Characteristic pungency
as a spice, flavour enhancer, vegetable and component and flavour of the chili pepper fruits provide
in herbal medicine. The numerous phytochemicals unique hotness to meal preparations and a wide
and their medicinally important properties present in variety of foods utilize this pungency in
diverse germplasm of chili pepper have been
combination with salt and other spices for
characterized and documented. Capsaicinoids,
carotenoids, vitamins, flavonoids such as flavour enhancement (Pino et al., 2007). The
anthocyanins are present as the major phytochemicals genus Capsicum is highly diverse and contains
in chili pepper fruits. Capsaicinoids, pungent 40 species (The Plant List, 2013). Of those, five
analogues of capsinoids, are the most important group species, C. annuum var. annuum, C. chinense, C.
of phytochemicals in which capsaicin and frutescens, C. baccatum varieties pendulum and
dihydrocapsaic in are prominent in providing the basis umbilicatum and C. pubescens are most
for pungency and medicinal properties. The detailed frequently consumed by humans (Moscone et al.,
studies conducted on the phytochemicals in chili 2007). The domestication of chili pepper has
pepper fruits using mouse models and human cell been dated to 6000 B.C., and archeological
lines have reported an array of anticancer effects on
evidence (genus specific starch-granule-
leukemia, myeloma and various carcinomas
associated with the digestive tract. In addition, chili morphotypes) found in the Bahamas and
pepper possesses anti-inflammatory, antidiabetic, Southern Peru imply that chili pepper had been a
antimicrobial, anticholesteremic, anticlotting and component in diets as early as in 7500 B.C.
antioxidant activities. Therefore, this review is (Perry, 2007).
compiled to provide a comprehensive assessment of
the phytochemical profile and medicinal values of Apart from the culinary uses, chili pepper
chili pepper. Collectively, numerous studies has also been used in medicinal preparations,
performed to date demonstrated the potential providing nutritional and health advantages such
medicinal significance of chili pepper for as anticancer, anti-inflammatory, antidiabetic,
development of herbal medicine and to plan further anticholesteremic, anticlotting, analgesic and
studies to elucidate other hitherto unknown medicinal antimicrobial effects. Mayans used chili pepper
values. to treat microbial diseases (Cichewicz and
Thorpe, 1996) and many reports from India
Keywords: Capsicum, Capsaicin, Capsaicinoids,
show that chili pepper was used to treat asthma
Phytochemicals, Anticancer activity
(even the chili root extracts were used),
INTRODUCTION gastrointestinal tract problems (Baruah et al.,
2014), extreme pain, toothache, wounds, ulcers,
Chili pepper, (Capsicum spp.), is an essential arthritis (Bhagowati and Changkija, 2009),
element in our daily cuisine. It is the most headaches and night blindness (Deorani and
highly consumed spice in the world with a mean Sharma, 2007). Treating hypersensitivity and
annual consumption of 3.5 million metric tons of rheumatism using chili pepper also was common

*Corresponding Author’s Email: sunethss09@gmail.com

6 Ceylon Journal of Science 45(3) 2016: 5-20

in Italian indigenous medical practices (Pieroni reviews the medicinal values of chili pepper on
et al., 2004). diverse ailments including cancer, diabetics,
cholesteromia and microbial infections.
The indigenous uses of chili pepper in folk
medicinal applications and the safe and PHYTOCHEMICAL PROFILE
prolonged use of chili pepper as a spice in human
history enable us to think that the The phenolic compounds present in the chili
phytochemicals present in chili pepper fruits pepper are attributed to many medicinally
promote and maintain the good health of human important properties such as anti-diarrheal,
beings (Bosland, 1996). These phytochemicals antimicrobial, antioxidant, antihyperglycemic,
and their nutritional and medicinal values have anti-lithogenic and antimutagenic activities
been characterized in numerous studies. A few (Adefegha and Oboh, 2013). Chili pepper fruits
reviews have been published on metabolism and contain phenolic compounds such as flavonoids
bioavailability (Rollyson et al., 2014) and (Chu et al., 2002), β-catenin, capsaicinoids
anticancer effects (Cao et al., 2015; Pawar et al., (Vera-Guzman et al., 2011), carotenoids
2011) of capsaicin and nutraceutical benefits of (capsanthin, capsorubin and cryptocapsin),
chili pepper in general (Milind and Sushila, vitamins A, B, C and E (Kidmose et al., 2006;
2012). However, the array of medicinal Niizu and Rodriguez-Amaya, 2005; USDA
properties in chili pepper has not been reviewed Nutrient Data Laboratory, 2015), glycolipids,
together to realize it‟s multiple roles. This paper glycerolipids and esters (Bijttebier et al., 2014).

Figure 1: The structures of the common capsaicinoids in chili pepper.

M.D.M. Chamikara et al. 7

Chemical composition of chili pepper fruit Generally chili pepper has a higher amount of
extracts has been characterized using GC/MS vitamin C (ascorbic acid) than many other
spectrophotometry (Wesolowska et al., 2011) vegetables showing its significant nutritional
and liquid chromatography-photodiode array- value (Kumar and Tata, 2009). It is also
accurate mass mass spectrometry (LC-PDA- interesting to note that vitamin C is preserved
amMS) (Bijttebier et al., 2014). There are five during drying. The total phenolic and carotenoid
major capsaicinoids observed in chili pepper contents increase during ripening, where the total
(capsaicin, homocapsaicin, dihydrocapsaicin, phenolic content is doubled and the carotenoid
nordihydrocapsaicin, and homodihydrocapsaicin) content is increased by 10-fold. Although the
which contribute to the pungency (Baruah et al., total flavonoid content increases during initial
2014; Reyes-Escogido et al., 2011) (Figure 1). ripening (i.e. yellowing), it is later reduced as
Other capsaicinoids such as nonvamide and n- fruits turn red (i.e. at complete ripening) (Shaha
vanillyl decanamide are also present in et al., 2013). The content of ascorbic acid is
significant levels. The total capsaicinoid content increased during drying of green chili peppers,
is in the range of 58.8% to 84.5% in acetone and while total phenolic content is decreased,
hexane extracts of the fruits (Wesolowska et al., resulting in lowered overall antioxidant capacity
2011). The capsaicin [8-methyl-N-vaniloid-6- (Ozgur et al., 2011). However, Wangcharoen and
nonenamide] and dihydrocapsaicin [N-(4- Morasuk, (2008) reported that when chili pepper
hydroxy-3-methoxybenzyl)-8- was dried at a temperature more than 100 °C,
methylnonenamide] (Surh, 2002), present at higher amounts of phenolic compounds were
levels of 37% and 29% of the total capsaicinoids retained and hence resulting an increased
respectively (Wesolowska et al., 2011), provide antioxidant activity. It is also interesting to note
90% of the pungency of chili pepper (Giuffrida that the antioxidant activity of dried chili pepper
et al., 2013). was maintained for as long as 18 months after
harvesting (Ogiso et al., 2008).
Within the genus Capsicum, C. chinense
contains the highest level of capsaicin (Bosland ANTIOXIDANT ACTIVITY
and Baral, 2007). The contents of tannins,
flavonoids, saponins, terpenoids and carotenoids The phytochemicals present in chili pepper
are higher in C. annuum than those of other possess anticancer properties (Chung et al.,
species but C. frutescence contains the highest 2005), among them, vitamin C and phenolic
levels of flavonoids (Rahim and Mat, 2012) and compounds can act as antioxidants to counteract
anthraquinone (Emmanuel-Ikpeme et al., 2014) effects of reactive oxygen species (ROS)
compared to the other domesticated species. (Podsedek, 2007). ROS, which are generated
Although the mean vitamin E content in chili from cellular metabolic processes, have been
pepper ranges from 1.98% to 2.10% associated with several diseases such as cancer,
(Wesolowska et al., 2011), the species C. diabetes, cardiovascular and neurological
annuum contains a higher vitamin E content than disorders (Sun-Hwa et al., 2007). Detoxification
C. frutescence (Emmanuel-Ikpeme et al., 2014). of ROS can be done by several enzymes present
The well-known chili pepper cultivar, bell pepper in the body as well as antioxidants obtained
contains 20.73 g of dietary-fiber and 133 mg of through dietary components (Halliwell, 2006)
vitamin C per 100 g of fresh fruit weight such as chili pepper.The antioxidant activity of
(Durucasu and Tokusoglu, 2007). It has been chili pepper (Rosa et al., 2002) is only second to
revealed that C. annuum would be a good source spinach among commonly consumed fruits and
of Zn which is an essential micronutrient vegetables (Pellegrini et al., 2003). The
(Emmanuel-Ikpeme et al., 2014). antioxidant activity of chili pepper has been
measured and studied using several assaying
Effects of drying and ripening on systems such as DPPH (2,2-diphenyl-1-
phytochemicals picrylhydrazyl assay), ABTS (2,2'-azino-bis[3-
ethylbenzothiazoline-6-sulphonic acid] assay),
Conventional sun drying retains capsaicin in the DMPD (Dimethyl-4-phenylenediamine
chili pepper fruits (Magied et al., 2014), and it assay),CuPRAC (Cupric reducing antioxidant
has been confirmed that drying under low capacity assay) and FRAP (Ferric ion reducing
temperature assures the high quality of chili antioxidant power assay) (Krishna et al., 2010).
pepper by preserving the phenolic compounds Chili pepper contains both phenolic and
and vitamin C in the fruits (Moraes et al., 2013).
8 Ceylon Journal of Science 45(3) 2016: 5-20

anthocyanin compounds which possess apoptosis of malignant cells. Capsaicin elicits the
antioxidant activity (Borovsky et al., 2004; apoptosis pathway by repressing the plasma
Howard et al., 2000; Marín et al., 2004; Mennen membrane NADH oxidoreductase enzyme in
et al., 2005). Dietary phenolic compounds are mitochondria (Morre et al., 1995, 1996).
advantageous as they donate H atoms to free Capsaicin also binds with the ATP generating
radicals generated inside the body and neutralize coenzyme Q, inhibiting its activity and
them (Borovsky et al., 2004). The vitamins C destabilizing the electron flow in the
and E present in chili pepper are also effective mitochondria, thus producing ROS and
antioxidants (Sun-Hwa et al., 2007). Chili pepper triggering apoptosis (Macho et al., 1998, 1999,
is consumed in both dried and fresh forms, 2000; Wolvetang et al., 1996). The ROS have
potentially influencing antioxidant levels, been shown to disrupt the mitochondrial
although studies have provided conflicting membrane and induce apoptosis pathways in
results regarding the effect of drying pancreatic cancer cells (Zhang et al., 2008).
(Wangcharoen and Morasuk, 2008). Capsaicin triggered the apoptosis pathway in
human KB cancer cells (derived from HeLa cell
There are also differences for antioxidant line) by agitating the membrane potential of
capacity among different species and cultivars of mitochondria and subsequently activating the
chili pepper. Assessment of the antioxidant caspase signaling pathway (Lin et al., 2013).
activity in Turkish pepper cultivars revealed an However, capsaicin could also inhibit NF-ĸB
approximately 7-fold range in antioxidant (nuclear factor kappa-light-chain-enhancer of
activity (2.57 to 18.96 mmol of trolox per kg) activated B cells) pathway which can cause
(Frary et al., 2008). Out of the five chili pepper apoptosis and minimize carcinogenic effects
types tested, Bell and Caribe (a type of yellow (Han et al., 2001; Patel et al., 2002). The studies
fruited chili pepper) were reported to contain the on human cell cultures with exogenous capsaicin
highest antioxidant activity. The correlation exhibited apoptosis (Ghosh and Basu, 2010),
between the phenolic content and the antioxidant autophagy (Choi et al., 2009; Oh et al., 2010)
activity was estimated as 91.4% (Medina-Juarez and inhibition of cell metabolism (Arora et al.,
et al., 2012) indicating that majority of the 2011). The carotenoid pigments present in bell
antioxidant activity in chili pepper is due to the pepper such as capsanthin, capsorubin and
phenolic compounds. The highest level of cryptocapsin possess high free radical
phenolic content and the highest antioxidant scavenging activity (Matsufuji et al., 1998).
activity compared to other species and cultivars
were detected in bell pepper by Rahim and Mat, The experiments conducted using derived
(2012), which was verified by Nadeem et al., human cutaneous squamous cell carcinoma (SCC
(2011). C. chinense is also reported to contain cell lines) concluded that capsaicin has
higher levels of antioxidants such as carotenoids, prophylactic and therapeutic potentials to the
ascorbate and glutathione and the concentration skin cancers through the induction of apoptosis
of glutathione is increased during ripening (Hail and Lotan, 2002) and modulating the
(Castro-Concha et al., 2012). Glutathione and epidermal growth factor receptor (EGFR)
ascorbate are the major antioxidants which (Hwang et al., 2010). Capsaicin also down-
contribute to Halliwell Asada Cycle, where regulates the expression of Bcl-2 (B-cell
detoxification of H2O2 produced in chloroplast lymphoma 2) (Jun et al., 2007), and thereby
takes place without the involvement of enzyme induces the apoptosis in B16-F10 melanoma
catalase (Foyer and Noctor, 2009). cells (derived from Mus musculus skin
melanoma). Chemically induced skin cancers in
ANTICANCER ACTIVITY mouse models were also shown to be repressed
Application of C. chinense fruit extracts to the by capsaicin (Park and Surh, 1997).
HepG2 cell lines (derived from a hepatocellular Capsaicin is identified as a blocker for the
carcinoma) demonstrated the inhibition of cancer interleukin-6 induced transcription factor STAT3
cell proliferation. This inhibitory activity was [signal transducer and activator of transcription 3
independently verified by using methylthiazol (acute-phase response factor)] (Yu et al., 2009)
tetrazolium (MTT), lactate dehydrogenase which promotes tumor regenerative pathways.
leakage and nitrous oxide (NO) production Thus, capsaicin could be used as a preventive
assays (Amruthraj et al., 2014). The and treatment drug for myeloma and other
phytochemicals present in chili pepper trigger
M.D.M. Chamikara et al. 9

cancers (Bhutani et al., 2007). In vitro studies capsaicin also mediates ROS resulted
using T-cell leukemia cell cultures have reported mitochondrial damages and induces apoptosis.In
that capsaicin inhibits the growth of leukemia colorectal cancer cells capsaicin is known to
cells by degrading the TAX protein (human T- suppress the β-catenin dependent signaling
cell leukemia virus type 1 transcriptional pathway. Capsaicin restricts the expression of
transactivator) and increasing the NF-kB transcription factor 4 (TCF-4) and inhibits the
inhibitor alpha (Iĸ-Bα) which arrests the cell interaction between β-catenin and TCF-4
cycle and triggers apoptosis. This demonstrates suggesting the potential use of chili pepper as a
the possibility of using capsaicin as a chemo- treatment for colorectal cancers (Lee et al.,
preventive drug for leukemia (Zhang et al., 2012). Lee et al., (2010) also reported that
2003). Capsaicin is also known to induce the capsaicin represses the cell proliferation in
apoptosis pathway in leukemia cells through colorectal cancer cell lines.
oxidative stress (Ito et al., 2004).
The anticancer role of capsaicin is also
In glioma cancers of brain, capsaicin binds observed in lung associated carcinoma.
to the transient receptor potential vanilloid type I Capsaicin stabilizes the mitochondrial related
(TRPV I) receptor in glioma cells and induces enzymes in lungs which minimize the cancer risk
apoptosis (Amantini et al., 2007). Gil and Kang, induced by using benzopyrene in mouse models
(2008) have also reported that capsaicin induces (Anandakumar et al., 2007). Jang et al., (1989)
apoptosis in human glioma cells by down- have reported that capsaicin reduces the risk of
regulating Bcl-2 expression. Capsaicin is also lung tumor development induced by polycyclic
known to possess inhibitory effects against the aromatic hydrocarbons. According to Brown et
numerous cancers in the digestive system. al., (2010) capsaicin can be used to treat human
Capsaicin possesses anti carcinogenic activity small cell lung cancer since it has anti-
against tongue cancers (Tanaka et al., 2002) by proliferative activity in both cell culture
inducing apoptosis through the stimulation of the experiments and mouse models by inhibiting the
expression of caspase-3 and caspase-9 activities E2F (a family of transcription factor genesin
(Ip et al., 2012a). Wu et al., (2006) reported that higher eukaryotes) responses and proliferative
capsaicin triggers apoptosis via activating gene expression which triggers the anti-
caspase-3 and generating the ROS in CE proliferative activity. The apoptosis inducing
81T/VGH cells (derived from esophagus mechanisms in NPC cell lines (derived from
epidermoid carcinoma). It has also been reported human nasopharyngeal carcinoma) are reported
that capsaicin heightened the expression of in Ip et al., (2012b) and it was found that
proto-oncogenes (such as c-myc and c-Ha-ras), capsaicin induces endoplasmic reticulum stress,
which trigger the apoptosis pathway, and tumor caspase-3 activation and mitochondrial
suppressor gene p53 in SNU-1 cell line (derived depolarization. In addition capsaicin has an
from human stomach cancer cell) (Kim et al., inhibitory activity against the development of
1997). Jung et al., (2001) reported that capsaicin prostate cancer by down-regulating the
induces apoptosis by activating the caspase-3 and expression of prostate specific antigen (PSA)
down-regulating the Bcl-2 in hepatocarcinoma (Mori et al., 2006). The reported inhibitory
cells SK-Hep-1 human liver cell line (derived effects of the capsaicinoids on diverse cancer cell
from the ascetic fluid of a patient with lines are summarized in Table 1.
adenocarcinoma). In pancreatic cancer cells,
10 Ceylon Journal of Science 45(3) 2016: 5-20

Table 1: The inhibitory effects of capsaicinoids on diverse cell lines mimicking the anticancer activity.

Cancer Cell line Effect/s Reference

HPB-ATL-T (adult T-cell leukemia) Inhibit growth. Zhang et al., (2003)
NB4 –PL (neuroblastoma promyelocytic leukemia) and
Leukemia Induce apoptosis by oxidative stress. Ito et al., (2004)
Kasumi-1 (myeloid leukemia)
HL-60 (human myelocytic leukemia) Induce apoptosis by caspase-3-dependent mechanism. Tsou et al., (2006)
U266 (human multiple myeloma) and MM.1S (immunoglobulin Inhibit the tumorigenesis by blocking STAT3 [signal transducer and activator of
Multiple myeloma Bhutani et al., (2007)
A lambda myeloma) transcription 3 (acute-phase response factor)].
SRB-12 (scavenger receptor class B type 12 derived from an
Cutaneous cell Arrest cell cycle at G1 stage and induce apoptosis by mitochondrial
epidermal lesion of a patient) and COLO 16 (squamous-cell Hail and Lotan, (2002)
carcinoma depolarization.
carcinoma)
A172 (human glioblastoma) Induce apoptosis by generating ROS. Lee et al., (2000)
Glioma
FLS (fibroblast-like synoviocyte) and FC1 (glioblastoma) Induce apoptosis by mitochondrial depolarization. Amantini et al., (2007)
Tongue cancer SCC-4 (squamous-cell carcinoma) human tongue cancer cells Induce apoptosis by mitochondria dependent and independent mechanisms Ip et al., (2012a)
Nasopharyngeal Induce apoptosis by endoplasmic reticulum stress and mitochondrial
NPC-TW 039 (human nasopharyngeal carcinoma) Ip et al., (2012b)
carcinoma depolarization.
Esophageal
CE 81T/VGH (human esophagus epidermoid carcinoma) Arrest cell cycle at G0-G1 phase. Wu et al., (2006)
carcinoma
Gastric cancer SNU-1. NIH/3T3 (a Korean stomach cancer) Alter the expression of tumor forming genes and induce the apoptosis. Kim et al., (1997)
Induce apoptosis by generating ROS. Zhang et al., (2008)
Pancreatic cancer AsPC-1 and BxPC-3 (human pancreatic cancer)
Induce apoptosis by oxidative stress and mitochondrial damage. Pramanik et al., (2011)
SK-Hep-1 (sloan kettering hepatocarcinoma) Induce apoptosis by caspase-3-dependent mechanism. Jung et al., (2001)
Hepato carcinoma
HepG2 (human hepatoma) Induce apoptosis by ROS disruption. Huang et al., (2009)
Induce apoptosis by activating the peroxisome proliferator-activated receptor
HT-29 (human colon cancer) Kim et al., (2004)
Colon carcinoma gamma.
Colo 205 (human colon cancer) Induce apoptosis by caspase-8 dependent mechanism. Lu et al., (2010)
Lung cancer NCI-H69, NCI-H82 (small cell lung cancer) Arrest cell cycle at G1. Brown et al., (2010)
MCF-7 (Michigan Cancer Foundation-7) (human breast cancer) Induce apoptosis by caspase-independent pathway. Chou et al., (2009)
Breast cancer MCF-7 (Michigan Cancer Foundation-7), T47D, BT-474, Thoennissen et al.,
Arrest cell cycle and induce apoptosis by altering the EGFR/HER-2 pathway.
SKBR-3 and MDA-MB231 (breast cancer) (2010)
LNCaP (lymph node carcinoma of the prostate), PC-3 and DU-
Confer anti- proliferative activity by downregulating PSA. Mori et al., (2006)
Prostate cancer 145 (prostate cancer)
PC-3 (prostate cancer) Induce apoptosis by ROS generation. Sanchez et al., (2007)
Human KB
KB (derived from HeLa cell line) Arrest cell cycle at G2/M phase and induce apoptosis. Lin et al., (2013)
carcinoma
M.D.M. Chamikara et al. 11

ANTI-INFLAMMATORY AND PAIN Chili pepper, with a significant potential as a

RELIEVING ACTIVITIES candidate plant for new drugs, has shown to
possess promising antidiabetic activity (Okumura
Chili pepper extracts contain anti-inflammatory et al., 2012) as it contains inhibitors for α-
(Kim et al., 2003; Lee et al., 2005) and anti- amylase and α-glucosidase which are required
allergic properties (Lee et al., 2005). Out of the for the degradation of polysaccharides and
numerous phytochemicals in chili pepper, disaccharides. Chili pepper is also reported to
capsaicin is reported mainly to confer the anti- lower the absorption of D-glucose in the
inflammatory activity (Kim et al., 2003) but the intestine, thus it can be used to control
colour pigment anthocyanin has also been carbohydrate digestion and post-prandial glucose
reported to possess significant anti-inflammatory level rise (Kwon et al., 2007) (reviewed in
activity (Wang et al., 1999). Capsaicin Adefegha and Oboh, 2013). The effect of
overwhelmed the obesity induced inflammatory capsaicin on carbohydrate metabolism in
responses from macrophages in adipose tissue exercising and resting states were determined
(Kang et al., 2007) indicating the potential using human subjects and it was found that
applications as an analgesic. Inhibition of the capsaicin increases the plasma epinephrine and
expression of pro-inflammatory cytokines such norepinephrine by increasing O2 consumption.
as tumor necrosis factor-α (TNF-α) and This implies an increase of carbohydrate
interleukin 1β (IL-1β) by capsaicin reduces the oxidation due to capsaicin (Lim et al., 1997).
inflammatory responses induced by antigens Domotor et al., (2006) further confirmed using
(Spiller et al., 2008). It was also found that anti- human subjects, that capsaicin increases the
inflammatory activity was not triggered by glucose adsorption and increases the level of
vanilloid receptor-1 but by inhibiting the IkB-a, blood glucagon concentration. The obesity
which degrades the lipopolysaccharide induced insulin resistance which is a metabolic
stimulated peritoneal macrophages (Kim et al., disorder that can be minimized by using
2003). Capsaicin and nordihydrocapsiate (a type capsaicin reducing the risk of having type-2
of capsinoid) inhibit the early T cell activation diabetes in the future. Capsaicin alters the gene
events such as NF-ĸB activation (Sancho et al., expression, lessens the glucose intolerance
2002). Capsaicin can be used to treat rheumatoid (hyperglycemia) and reduces the fasting glucose
arthritis, osteoarthritis and peripheral arthritis levels in mouse models (Kang et al., 2010).
(Cordell and Araujo, 1993) as it reduces the Capsaicin is known to increase the rate of
inflammatory heat. It can be used to relieve the carbohydrate metabolism in human subjects and
pain from noxious chemical hyperalgesia as well in addition, the rat models were used to gain a
(Arora et al., 2011; Fraenkel et al., 2004) deep insight on the antidiabetic effects of chili
because it has an ability to control the secretion pepper. Administration of chili pepper to rats
of neurotransmitter relating to the pain (Lynn, reduces blood glucose levels (Magied et al.,
1990). The analgesic activity of capsaicin can be 2014; Okumura et al., 2012) through the
used to minimize neuropathic pain conditions induction of thermogenesis reactions such as
(Sindrup and Jensen, 1999). When recovering lipid and glucose metabolism leading to the
from cancer treatments, capsaicin can be used as lowering of fatty acid storage in the body.
a temporary pain relieving agent for oral Induction of thermogenesis reactions are
mucositis which results from chemo and achieved by activating the sympathetic nervous
radiation therapies (Berger et al., 1995). Cruz, system which promotes thermogenesis reactions
(2004) reported that capsaicin can reduce the (Okumura et al., 2012). C. frutescence is always
bladder pain associated with patients who have a center of attraction in this regard as it was
hypersensitive disorders. shown to increase the blood insulin level in type-
2 diabetes of rats (Islam and Choi, 2008).
Furthermore C. frutescence was found to
ANTIDIABETIC/ANTIHYPERGLYCEMIC increase the affinity of insulin towards its
ACTIVITIES receptor (glucose) implying the potential of using
chili pepper as a treatment for diabetes (Anthony
It is estimated that by 2025, the number of
et al., 2013; Patel et al., 2012).
diabetic patients in the world could go up to 300
million (Sy et al., 2005) and therefore more
efficient and economical treatments are needed.
12 Ceylon Journal of Science 45(3) 2016: 5-20

ANTICHOLESTEREMIC ACTIVITY AND in rodents (Ogunlade et al., 2012). Experiments

THE EFFECTS ON LIPID METABOLISM conducted using rat models suggested that chili
pepper can reduce the risk of cardiovascular
Chili pepper is reported to possess diseases and arthritis (Kritchevsky, 1992).
hypocholesteremic and hypolipidemic activities, Capsaicin was shown to inhibit platelet
thus it can be used to treat and prevent aggregation (Adams, 2009; Hogaboam and
cardiovascular diseases (Kempaiah and Wallace, 1991) by stabilizing the membranes of
Srinivasan, 2002; Srinivasan et al., 2004). red blood cells via interfering with the enzyme
Capsaicin can induce the thermogenesis and lipid phospholipase A2 (PLA2) (Wang et al., 1984).
metabolism pathways (Ahuja et al., 2006) by Mouse model studies revealed that capsaicin,
inhibiting the fatty acid storage in the body which inhibits platelet formation by inhibiting
(Okumura et al., 2012; Yoshioka et al., 1998) the clotting factors VIII: C and IX (Adams et al.,
showing its potential to use as a treatment to 2009), is more effective than aspirin in averting
control obesity. Capsaicin stimulates the acute pulmonary thromboembolism (Wang et
catecholamine secretion leading to the release of al., 1985). Therefore, capsaicin may have the
β3 adrenergic stimulation which generates potential to be developed as a therapeutic and
thermogenesis reaction (Kawada et al., 1986; preventive agent of cardiovascular diseases.
Jimenez et al., 2002; Watanabe et al., 1987).
Capsaicin specifically alters the lipid metabolism ANTIMICROBIAL ACTIVITY
by lipid oxidation of the high fat diets in the
gastrointestinal tract. Kempaiah et al., (2005) Herbal materials have long been appreciated
reported that capsaicin inhibits low density because of their proven antimicrobial effects
lipoprotein oxidation induced by copper (in (Alavijeh et al., 2012). In addition to the use of
vitro) and ferrous (in vivo) ions. Ahuja et al., chili pepper as a spice, it has been widely used as
(2006) reported that capsaicin and an agent to preserve food (Omolo et al., 2014).
dihydrocapsaicin inhibit the copper-induced The antimicrobial activity of the compounds
serum lipoprotein oxidation. Capsaicin has present in Capsicum species were reported in
proven protective effects on hepatic lipid many studies (Careaga et al., 2003; Cichewicz
peroxidation in rats (Kempaiah et al., 2005). and Thorpe, 1996; Omolo et al., 2014). In
Another study on rats revealed that administering addition to the pungency related phytochemicals,
chili pepper along with high fat diet affects HDL the pigment anthocyanin in chili pepper also
and LDL cholesterol, total glyceroids and total possesses antimicrobial activity (Zhao et al.,
lipid contents, and thereby reduces serum 2009). The antibacterial activities of chili pepper
cholesterols significantly compared to that of were reported against the noxious pathogens
control treatments (Magied et al., 2014). Bacillus cereus, B. subtilis, Clostridium
Similarly, the serum lipoprotein content was sporogenes, C. tetani, Streptococcus pyogenes
reported to be reduced in human subjects who (Cichewicz and Thorpe, 1996), Staphylococcus
had daily chili pepper diets (Ahuja and Ball, aureus (Molina-Torres et al., 1999), Escherichia
2006). Chili pepper can be used to control lipid coli, Pseudomonas aeruginosa, Sarcina lutea,
oxidation since it possesses higher antioxidant Candida albicans (Soetarno et al., 1997) and
activity than most of the other vegetables Vibrio cholera (Chatterjee et al., 2010). The
(Embuscado, 2015). Experiments with human bactericidal activity of capsaicin against the
subjects also have shown that dietary capsaicin gastric pathogen Helicobacter pyroli was
induces abdominal fat loss by increasing fat evaluated and the minimum inhibitory
oxidation (Snitker et al., 2009). Further studies concentration (MIC) was found to be 10 μg/ml
with human subjects with higher Body Mass (Jones et al., 1997) and confirmed by Zeyrek and
Index (BMI) demonstrated that consumption of Oguz, (2005). Similarly MIC values of 25 μg/ml
capsaicinoids increased fat oxidation rate and against B. subtilis, 200-300 μg/ml against E. coli
energy expenditure in the body, suggesting it (Molina-Torres et al., 1999), 15 µl/g against
may be valuable to facilitate reduction in BMI Salmonella typhimurium and5-15 µl/g against P.
(Inoue et al., 2007). aeruginosa (Careaga et al., 2003) were reported.
Capsaicin also possesses inhibitory activity
ANTICLOTTING EFFECT against numerous antibiotic resistant microbial
strains (Zeyrek and Oguz, 2005). The acetonitrile
The phytochemicals present in chili pepper have extracts of phytochemicals chrysoeriol,
proven healing effects on cardiovascular diseases
M.D.M. Chamikara et al. 13

dihydrocapsaicin and capsaicin from C. pepper were also reported. The healing effects of
frutescence were found to have antimicrobial chili pepper on other disease conditions such as
activity against Enterococcus faecalis, B. strokes, hypercholesterolemia, aging, obesity,
subtillis, S. aureus, P. aeruginosa, Klebsiella and ulcers associated with the digestive tract
pneumoniae, E. coli and C. albicans were well studied. The underlying
(Nascimento et al., 2014). The mechanism of phytochemicals and their associated molecular
antimicrobial activity of capsaicin was evaluated pathways have been characterized to show the
through DNA microarray technology and it was mechanisms of action. The inter-genera diversity
found that capsaicin has a toxic effect against of the medicinal properties have been studied
yeast cells and induces their pleiotrophic drug though mainly limited to the fruits of two main
resistance network which expresses genes related species, C. annuum and C. frutescence and, the
to osmotic stress and membrane biosynthesis famous cultivar bell pepper which is also a C.
(Kurita et al., 2002). annuum. Further studies are essential to explore
and characterize more efficient bio-active
OTHER MISCELLANEOUS MEDICINAL compounds from the underutilized Capsicum
VALUES spp. in diverse geographical locations. The
It has long been believed that chili pepper wealth of information that is currently available
promotes proper functioning and good health of regarding the medicinal properties of chili pepper
digestive tract. Capsaicin stimulates the secretion can be used to develop novel drugs to combat
of saliva and gastric juice which is vital for cancers and other important ailments mentioned.
efficient digestion of food and to overcome
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