1.

ABSTRACT

Black pepper (Piper nigrum L.) is an important healthy food owing to its antioxidant,
antimicrobial potential and gastro-protective modules. Black pepper, with piperine as an active
ingredient, holds rich phytochemistry that also includes volatile oil, oleoresins, and alkaloids.
It has also been extensively explored for its biological properties and its bioactive phyto-
compounds. In addition to its culinary uses, pepper has important medicinal and preservative
properties, and, more recently, piperine has been shown to have fundamental effects on p-
glycoprotein and many enzyme systems, leading to biotransformative effects including
chemoprevention, detoxification, and enhancement of the absorption and bioavailability of
herbal and conventional drugs The alkaloid piperine improves the therapeutic value of several
drugs, vaccines and nutrients by enhancing bioavailability through inhibiting numerous
digestive enzymes. Piperine also aids in digestion through stimulating pancreatic and intestinal
enzymes, and enriches cognitive skills and fertility. Furthermore, piperine is recognized as
delivering several therapeutic activities distinct from other chemical components. This study
endeavors to systematically review précised data on the traditional uses and pharmacological
properties of black pepper. Besides, this review presents a summary of the data on the chemical
composition of black pepper, including minerals, vitamins, carotenoids and flavonoids, and
various therapeutic benefits. Up to date existing information, various metabolites have been
isolated from P. nigrum. Among them, biologically active alkaloid piperine and the main
essential oils constituents including β-caryophyllene, limonene, sabinene, α-pinene, β-
bisabolene and α-copaene can serve as a new natural source for use in food, aroma, cosmetics
and pharmaceutical industries.

1
 2. INTRODUCTION

Black pepper (Piper nigrum L.) is a widely utilized spice renowned for its pungent aroma and
valued for its strong pungency and medicinal potency. Native to southern India, this perennial
shrub has been extensively cultivated in tropical regions. Piper nigrum is a woody climbing
vine growing up to 30 feet, with grayish stems reaching 1.2 cm in diameter, and numerous
rootlets emerging from swollen stem nodes.
The leaves are dark green above and pale green beneath, glossy, ovate, and acutely tipped,
measuring 13-25 cm in length. Elongated, slender spikes or catkins bear minute, white flowers,
producing 50-60 single-seeded dark red berries approximately 5 mm in diameter. Different
plant parts are used medicinally, with the cooked and dried unripe berry being the most
common.
Black pepper's bioactive phytochemical compounds include piperine, a potent alkaloid, as well
as piperanine, piperettine, piperylin A, piperolein B, and pipericine. Notably, black pepper
contains more polyphenols than white pepper, which undergoes fermentation and skin removal,
altering its flavor and heat component. Research has established black pepper's therapeutic
efficacy in antioxidant activity, anti-inflammatory properties, antimicrobial effects, and
digestive aid.
Black pepper is highly valued in traditional systems of medicine, including Unani and
Ayurvedic. Recent scientific researchers have identified many active compounds with specific
pharmacological properties. The spice's aromatic features are susceptible to loss during regular
grinding, resulting in deterioration of quality. However, black pepper's bioactive compounds
remain effective, with piperine hydrolyzing in the gut and liberating bound polyphenols.
Studies have analyzed black pepper's volatile oils using column chromatography, high-
resolution gas chromatography, and gas chromatography-mass spectrometry (GC-MS),
identifying up to 46 compounds. Five phenolic amides isolated from black pepper
demonstrated high antioxidant activity, surpassing some naturally occurring antioxidants.
Experimental and clinical studies have confirmed black pepper's therapeutic efficacy for
specific pharmacological actions.
Common Names:
Kali mirch (Urdu, Hindi)
Marich (Nepali)
Pippali (Sanskrit)
Milagu (Tamil)

2
 3. TAXONOMICAL CLASSIFICATION

Kingdom Plantae

Division Manoliophyta

Class Magnoliopsida

Order Piperales

Family Piperaceae

Genus Piper

Species nigrum

3
 4. Bioactive chemical compounds

Black pepper is rich in minerals, vitamins and nutrients. The chemical

composition of 100 g of black pepper seeds includes carbohydrate 66.5 g, protein
10 g, and fat 10.2 g, as well as a relatively high concentration of minerals such as
calcium (400 mg), magnesium (235.8-249.8 mg), potassium (1200 mg),
phosphorus (160 mg), and the lower concentration of sodium, iron and zinc. These
minerals are essential elements for day-to-day activities of humans. Besides, black
pepper also has a significant concentration of vitamins such as Vitamin C, B1, B2
and B3. Nine accessions of Nigeria grown black pepper had a concentration of
tannin ranging from 2.11 to 2.80 mg /100 g. In a recent study on black pepper,
catechin, Quercetin, myricetin, and carotenoids, namely lutein and βcarotene have
also been detected in significant concentration. Several researchers evaluated
essential oils (EO), oleoresin and piperine in various parts of black pepper. The
EO yield of black pepper berries and leaves have varied from 1.24 to 5.06 %, and
0.15–0.35 %, respectively. It has been observed that variability of volatile oil and
oleoresin content in 14 black pepper accessions ranged from 2.7 − 5.1 % and 7.6
− 9.4 %, respectively. The oleoresin content of black pepper ranged between 4.27
and 12.73 % and the characteristic natural alkaloid of black pepper “piperine”
ranged from 2.13 − 5.80 % and 0.12 − 20.86 %, in seeds and leaves
correspondingly.

PIPERINE

4
 5. CHEMICAL COMPOSITION
The chemical constituents of pepper can be classified into three major groups:
a) compounds that contribute to its spiciness (spicy taste);
b) compounds that give a characteristic aroma;
c) compounds that make the pre-dominant ingredients (starch), and other compounds.
The aroma of pepper comes from the essential oil present in the fruit, while the presence of the
alkaloids, mainly piperine, is important for its spiciness. Pepper extracts in the form of
oleoresins, also containing phenolic compounds, can also be found commercially . Starch may
contribute to the cooking and nutritional quality of black peppers. Plant quality is the most
important criterion in cultivation when it comes to spices, and pepper is no exception. The
quality of pepper is mainly determined by the amounts of piperine, essential oil, or oleoresin.

Piperine - the main pungent compound of pepper.Black pepper has a characteristic aroma and
spicy taste, which is attributed to piperine the main alkaloid found in peppercorns. The amount
of piperine can be affected by modifcations of growing conditions, such as climate or drying
conditions and the place of origin. The fruit of black pepper contains piperine in the amount of
2-9% . There are different methods for the isolation of piperine. This yellow-brown substance
can be found in the form of crystals and obtained by polar organic solvents by maceration
and/or Soxhlet extraction of black pepper fruit .

Black pepper oleoresin- Spice oleoresins range from viscous oils to thick, tacky pastes. They
are composed of various components such as essential oils, fixed oils, pigments, pungent
constituents such as alkaloids, etc. The components of oleoresin, each in particular, cannot be
added directly to food. Oleoresins have high stability and can be stored for a minimum of one
year, without any loss in quality. Controlled-atmosphere storage (temperature and humidity) is
not required .Oleoresin constitutes around 6% to 13% of black pepper . It is obtained by
extraction of black pepper fruit with volatile organic solvents, such as ethanol, acetone, ether,
dichloroethane, etc., and subsequent removal of the solvent under reduced pressure to trace
levels. The organoleptic properties of black pepper oleoresin are determined by its volatile oil
and piperine contents whose abundance depends on the type of pepper and its maturity stage,
the used extraction solvent, and the extraction condition. Typically, oleoresin contains 15% to
20% of volatile oil and 35% to 55% of piperine .

Essential oil- The black pepper contains about 1%-3% of essen-tial oil, but some studies have
shown values of 9% . The essential oil of black pepper is a colorless to yellow-greenish
liquid,with a spicy aroma and characteristic odour. The essential oil is obtained by distillation
of the dried immature fruits. This essential oil has a specific gravity of 0.860-0.884 and a
refractive index of 1.478-1.488 at 20 °C, and the optical rotation range between - 1 ° to - 23 °
so it is characterized as levorotatory . The most abundant compounds in the essential oil of
black pepper are monoterpene hydrocarbons, then sesquiterpene hydrocarbons, and also small
quantities of oxygenated monoterpenoids and oxygenated sesquiterpenoids.

5
6. NUTRITIONAL COMPOSITION

6
 7. PROCESSING

Post Harvesting Primary Treatment :

Harvesting

First Drying

Transport

Primary processing Secondary processing

Reception Processing

Cleaning and Drying Packaging

Storage
1. Post Harvesting Primary Treatment
Harvesting - The harvesting of the black pepper should be manually accomplished. As it is
known, the pepper is offered in the market under two types: black pepper and white pepper.
The type one wants to produce will determine the maturation point at which the bunches should
be harvested. When the objective is to prepare black pepper, the harvest should be
accomplished when the fruits are completely developed and at the beginning of the maturation
stage, as presenting yellowish coloration. In India, the harvest begins on January and extends
until March, and the Brazilian harvest comes soon after. In Vietnam, the harvest coincides with
the India, since it extends from February to April. In Malaysia, from which the main producing
region is Sarawak, the harvest is began soon after that of Vietnam and extends over the period
from May to July.
First Drying -The first drying is accomplished in order to reduce the moisture content of the
raw material and to darken the fruits. The decreased activity of the water within the fruits is
important for their conservation during transportation, as well as until they are properly
processed. After harvesting, the bunches taken to dry in boards in the sun or properly fenced
terrain. During the drying process, the dry fruits get loose from the axis of the bunches. The
pepper must be revolved in order to obtain an uniform drying. Those bunches axes that are
mixed with the product may be removed with a small wooden scraper. The care should be taken
to avoid the pepper to become wet by the rain or condensation.
Transport - The transportation from the field to the plant must be as fastest as possible in order
to minimizing the losses due to deterioration caused by high temperatures, such as excessive
water loss and increased metabolic activity. The transportation from the field to the plant must
be as fastest as possible in order to minimizing the losses due to deterioration caused by high
temperatures, such as excessive water loss and increased metabolic activity.

7
 2. Primary processing

Cleaning and Grading -The cleaning and selection of the pepper grains concomitantly occur
in the same equipment. The cleaning consists of removing wood chips, leaves, rotten fruits and
other impurities that might prejudice the quality of the product, and mainly stones and metal
pieces that could damage the equipment. This is a very important procedure that will guarantee
the quality of the product. As higher is the purity degree level of the grains as higher will be
their selling value. When selecting the raw material, however, the objective is to discard those
grains that are inappropriate for processing and consumption. Besides, it is possible to separate
the grains with adequate size and shape in order to be sold in whole. The defective grains, can
be consumed under the triturated form. The removal of the impurities, inappropriate and
defective grains are possible due to the differences in mass, shapes, size and colors. The
cleaning and selection of the pepper grains concomitantly occur in the same equipment. The
cleaning consists of removing wood chips, leaves, rotten fruits and other impurities that might
prejudice the quality of the product, and mainly stones and metal pieces that could damage the
equipment. This is a very important procedure that will guarantee the quality of the product.
As higher is the purity degree level of the grains as higher will be their selling value. The
cleaning and selection can be accomplished by equipments consisting of vibratory sieves,
ventilation systems and color-based classification.

3. Secondary processing
Processing - The process that will transform the raw material into product happens at this stage.
In other words, the raw material will be transformed into dehydrated fingers or curcuma
powder. See in Intact Black Pepper or Ground Black Pepper.
Packaging - The black pepper (in whole or ground) should be packed into polypropylene
packaging (bags or flasks) or glass. All packaging must be hermetically sealed to avoid loss in
the mass or modifications in the moisture content. Some care should be taken when removing
the air from within the packaging before sealing. The vacuum packaging improves the
conservation of the quality of the dehydrated pepper.
Storage - The dehydrated pepper must be stored in fresh places that are protected from the
light and moisture. The light alters the color, whereas the heat reduces the life time of the
product.

8
 8. BIOLOGICAL AND PHARMACOLOGICAL ACTIVITIES

A. Anti-microbial Activity of Piperine

Piperine in pepper has antimicrobial properties due to the phenolic compounds which help in
inhibiting the growth of S. aureus, Salmonella typhimurium, Bacillus, and E. coli2. The
accumulation of pyruvic acid and the reduction of ATP proved that chloroform extracts of
black pepper can change cell membrane permeability, destroy bacterial respiratory metabolism,
and ultimately lead to pyknosis and death. Although the antibacterial mechanism of pepper is
unknown, there are several experimental results which provide an approach for utilizing pepper
as a safe natural antimicrobial agent with applications in the food industry
B. Antioxidant Activity of Piperine
Essential Oils or extract of black pepper displays various pharmacological activities.
Essential oils are made up of different organic compounds that have conjugated carbon
double bonds and hydroxyl groups, which can give hydrogen to stop free radicals and reduce
oxidative stress it was found that flavonoids, phenols and piperine are important for the
antioxidant properties in black pepper. The antioxidant activities of pepper were mainly due
to catechin, rutin, epicatechin, and resveratrol. However, other compounds like ascorbic acid
could also contribute to the antioxidant activity.
C. Tobacco Withdrawal
Small clinical studies suggest that the essential oil of black pepper may help in treating
nicotine withdrawal and cravings. The exact reason how it acts, is not known. Researchers
proved that inhaling combusted black pepper may have helped in tobacco withdrawal and
cravings by reducing the automatic motor desire to smoke, calming the anxiety that comes
with withdrawal, and giving the same sensorimotor experience as smoking tobacco cigarettes.
The vaporized black pepper essential oil may be an effective way to help individuals quit
smoking even though black pepper that has been burned is probably not appealing outside
D. Hepatic Biotransformation
Te effect of black pepper on the hepatic biotransformation system has been studied in mice
for 10 and 20 days by giving 0.5, 1 and 2% dosages of black pepper. It was identified that
glutathione S-transferase and sulydryl levels went up in a dose-dependent way in mice fed
black pepper-containing diets for 10 days, except for a 0.5% black pepper diet. Cytochrome
b5 and cytochrome P450 levels were also significantly and dose-dependently raised. As a
possible way to get the body’s detoxication system going, black pepper has been mentioned
as a possible way to stop chemical carcinogenesis. Several studies have looked at how black
pepper or piperine affects the digestive enzymes in the liver and intestines. is suggests that
there could be food-drug interactions with prescription drugs through changes in
biotransformation pathways

9
E. Anti-inflammatory and Anti-nociceptive
Balb/C mice exhibited pronounced anti-inflammatory and anti-nociceptive properties, the
administration of black pepper essential oil via intraperitoneal injection over a consecutive
period of five days. The extracts of P. nigrum exhibited inhibitory effects on the generation
of pro-inflammatory nuclear factor (NF-B)cyclooxygenase-1 (COX-1), and cyclooxygenase-
2 (COX-2), as well as the proliferation of tumour cells. The administration of P.nigrum
essential oil through inhalation for 15 minutes was found to exhibit analgesic properties8.
Ethanolic extract of Piper nigrum novels amide alkaloids such as pipernigramides,
pipernigrester, and seven other compounds are extracted, which shows anti-inflammatory
properties in the carrageenan-induced paw oedema test
F. Nutritional and Biomedical Properties
Piperine essential oils of black pepper and ginger in combination have extensively been
reported for their nutritional and biomedical properties. Bacillus cereus, Salmonella
typhimurium, S. aureus and E. coli growth were strongly suppressed by piperine and they
also act as promising substitutes for food packaging materials and bandages
G. Cholesterol-lowering Activity
Piperine has been utilized to potentially mediate these effects due to its observed ability to
decrease blood lipids in living organisms and inhibit cholesterol absorption in laboratory
settings. The experiment revealed that the uptake of cholesterol into CaCo-2 cells exhibited a
reduction that was dependent on the dosage of piperine and black pepper extract. Notably,
both substances contained an equivalent amount of piperine. The study utilized differentiated
CaCo-2 cells to investigate the impact of black pepper extract and piperine on the absorption
of cholesterol in the intestinal lumen. This ending demonstrates that piperine exerts an
influence on the process of cholesterol metabolism.
H. Anti-tumour Activity
Extracts of black pepper having a high mitotic index, high rate of metastasis, poor prognosis,
and triple-negative breast cancer have gained attention, and essential oils of black pepper
show good Anti-cancer activity. Due to its poor stability, nanoparticles containing black
pepper essential oil were created using nanoprecipitation, employing Eudragit L100 as the
carrier, which inhibited the expression of cancer cell lines
I. Osteosarcoma (Bone Cancer)
Survival of patients with metastasis has been stabilized, with a broad-spectrum medication
doxorubicin, which shows a restricted therapeutic window because of its cardiotoxicity.
Piperine can cause the death of some cancer cells, and it increases the chemosensitivity of
doxorubicin. Combined therapy of piperine and doxorubicin has reduced tumour growth and
cell proliferation which is proved by in vivo and in vitro studies
J. Mesothelioma Cancer
A combination of curcumin-C3 complex and bioperine (A bioactive form of piperine) has
shown significant effects in in vitro studies as it inhibits the mesothelioma cells forming
tumour growth by limiting cell motility, proliferative cell rate, and self-renewal, and also
slows tumour growth in a xenogram mice model by decreasing
10
K. Stomach Carcinogen
Helicobacter pylori is designated as a stomach carcinogen. The effects of piperine on H.
pylori adhesion and growth were studied by using the broth macro dilution method and the
urease assay to conrm adherence to gastric cancer cells, it was possible to measure the
amount of H. pylori growth inhibition. The motility test by motility agar beside piperine
administration was evaluated by RT-PCR and immunoblotting. Piperine on administration in
dose dependant has reduced adhesion to gastric adenocarcinoma cells and inhibition was
statistically significant by student T-test

ANTI -
MICROBIAL
STOMACH
ANTIOXIDANT
CARCINOGE
N

TOBACCO
OSTEOSARCO WITHDRAWAL
MA

BIOLOGICAL AND
ANTI -
PHARMACOLOGICAL HEPATIC
EFFECTS BIOTRANSFOR
TUMOUR
MATION

ANTI –
CHOLESTEROL INFLAMMATO
LOWERING RY
NUTRITION
AND
BIOMEDICAL

11
 9. CONCLUSION
Piper nigrum (L.) has many favourable chemical properties and beneficial effects. Besides,
this review presents a summary of the data on the chemical composition of black pepper,
including minerals, vitamins, carotenoids and flavonoids, and various therapeutic benefits. Up
to date existing information, > 80 metabolites have been isolated from P. nigrum. Among them,
biologically active alkaloid piperine and the main essential oils constituents including β-
caryophyllene, limonene, sabinene, α-pinene, β-bisabolene and α-copaene can serve as a new
natural source for use in food, aroma, cosmetics and pharmaceutical industries. Piperine also
has a broad spectrum of therapeutic potential and potential for improving the bioavailability of
therapeutic drugs and nutrients. BPEO and piperine have many biological effects such as
hepatoprotective, antioxidant, anticancer, antibacterial, anti-inflammatory, antifungal,
antimicrobial, antihypertensive, antiasthma, antithyroid, wound healing and insecticidal
activities. Black pepper has extensive biological effects and has been utilized in preclinical,
clinical and therapeutics trials examining novel and new treatments of diseases. Furthermore,
piperine and BPEO have been widely explored for their therapeutic potential (Table 4).
However, gaps exist in the previous investigations on P. nigrum, and we have given
suggestions on a few topics that should have priority for detailed examinations.
First, the essential oil of black pepper loses its flavour quickly upon storing under a normal
room temperature. However, limited studies have been accompanied on maintaining the shelf
life of BPEO. Hence, future research is required to evaluate the storage quality of BPEO.
Second, insufficient biological and pharmacological investigations have been conducted on
piperine and BPEO. A few pharmacological assessments were performed utilizing
exceptionally high dosage concentrations, some were inadequate in examination with
controls, and others lacked determination of MIC values, perhaps prompting false positive
outcomes. Third, even though P. nigrum possesses several potential pharmacological effects
on antioxidant, antimicrobial, anticancer, and cytotoxic effects, these studies were employed
only in cell lines and animal models, scientific studies in humans have rarely been executed.
Hence, the future investigation could focus on the pharmacological properties of piperine,
BPEO and active constituents in various clinical studies with humans. Fourth, black pepper-
based drugs may be industrialized in future. Future research also needs to conduct clinical
trials to investigate the excessive consumption of black pepper in humans and animal models.
This review supports the expanded use of black pepper in culinary applications. Regular
consumption of black pepper could protect humans from various chronic diseases as a
nutraceutical as well as functional food.

12
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