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Intraduction

Hibiscus sabdariffa (roselle) is a species belonging to the Malvaceae family. In English-


speaking places, the name of the plant is also known as rozelle, and in the Arabian peninsula it
is also known as Karkade. In Turkey, it is known as "Hatmi çiçeği,Nar çiçeği". It grows in
tropical regions such as India, Hawaii, the Caribbean and Australia
(Natural Product Radiance, n.d.; Riaz & Chopra, 2018)
.

Hibiscus sabdariffa is a 0.15 to 1 m bushy annual that is branched from the base. The
stems are reddish, almost glabrous. The basal leaves are undivided and ovate; the cauline
leaves are 3-lobed and 7.5 to 10 cm wide. The lobes are 2.5 cm wide and crenate
(Medical Economics Company., 2000)
.

The flowers are solitary, axillary and almost sessile. The calyx is red, the corolla is
yellow, and the anthers are blood red. The fruit is a 2 cm long, ovoid, many seeded capsule
(Da-Costa-Rocha et al., 2014; Riaz & Chopra, 2018).

Almost all of the parts obtained after harvesting Hibiscus sabdariffa are used in the field of
health. Among the parts used, the main ones are seeds, leaves and calyces. After harvest,
roselle is used in many forms as spice, perfume, various salads and vegetable oils. One of the
most important factors in the quality of products is harvesting procedures.

Hibiscus tea contains high amounts of fruit acids in its structure. This fruit acid, which is
difficult to absorb, has a laxative effect on our body. Hibiscus tea contains high amounts of
fruit acids in its structure. This fruit acid, which is difficult to absorb, has a laxative effect on
our body. The aqueous extract of the leaves of our plant helps relax the uterine muscle.
Hibiscus also plays a role in lowering blood pressure (Medical Economics Company., 2000).

Hibiscus flowers have many uses; they are used to reduce appetite, for stomach colds and
respiratory tract colds, as an expectorant and diuretic, as a low-effective laxative, and for
circulatory disorders. later reviews are available: One on the effectiveness of Hs in the
treatment of hypertension and another on the treatment of hypertension and hyperlipidemia
(Da-Costa-Rocha et al., 2014).

In Chinese medicine, the purposes of using the plant's preparations are to prevent skin
swelling and Herpes (Medical Economics Company., 2000).

Taxonomy, Biological Activities and Distribution of Hibiscus sabdariffa


Figure 2.1. Roselle plant at flowering stage (Schoch et al., 2020).

Taxonomy (Schoch et al., 2020)

• Domain:Eukaryota
• Kingdom: Plantae
• Phylum: Tracheophyta
• Class: Magnoliopsida
• Order: Malvales

Family: Malvaceae

Genus: Hibiscus

Species: Hibiscus sabdariffa

Figure 2.2. Taxonomy of Hibiscus (Schoch et al., 2020).

Biological Activities
Fig. 1. Hibiscus sabdariffa L. plant and its biological potentials validated so far.

It was a fact that, Hs has been used to treat cardiac and nerve conditions, induce diuresis, and
induce lactation, among other conditions in folklore. Logical examinations have additionally
exhibited the antihypertensive, antidiabetic, against weight and hostile to hyperlipidaemic
properties of Hs. These organic exercises are believed to be because of the battery of
phytochemicals in Hs that have solid cell reinforcement movement and that hinder α-amylase,
α-glucosidase, angiotensin changing over catalyst, calcium channel blockage and direct
vasorelaxant impacts. A portion of the phytochemicals that are believed to be liable for these
natural impacts incorporate anthocyanins, flavonoids and natural acids. There is anyway the
requirement for more hearty investigates including controlled clinical preliminaries to
approve these organic exercises with the end goal of carrying the advantages nearer to the
bedside.

Distribution of Hibiscus sabdariffa

Since the beginning, the main source of Roselle amongst different scientist is a controversial
issue. Cobley who is a known scholar, claimed that Roselle is a local plant of West Africa and
the spread is started from there to other continents(America and Asia). However there is also
another opinion on the issue that suggest Rosell originated from India and Saudi Arabia.
Roselle is also a tropical crop as well as a home garden crop in Africa, Brazil, Hawai, Florida
and Philippinnes. Because of the fact that it is widely grown in different geograpichs it makes
it a contrversial crop.
Figure 2.3. Distribution of Hibiscus (Hibiscus Sabdariffa - Roselle -- Discover Life, n.d.)
.

PHYTOCHEMISTRY of HIBISCUS SABDARIFFA


Proximate constituents and nutrient composition of Hibiscus sabdariffa

Despite the fact that, the purposes of various pieces of Roselle are numerous and changed
both in food and in conventional medication, all pieces of Roselle including seeds, leaves,
products of the soil are utilized as a food in various regions of the planet. Meaty red calyxes
of Roselle are generally utilized for the creation of soda pops and tonic without liquor like
wine, juice, jam, jam, syrupand additionally dried and blended into tea and zest. The young
leaves and tender stems of Roselle are eaten raw as a green vegetable and are high in vitamin
C, riboflavin, anthocyanins, ascorbic acid, niacin, calcium, and iron. The Roselle seeds are
great wellspring of protein, fat, absolute sugars and are generally utilized in the eating
regimen in numerous African nations
PHYTOCHEMICALS OF HIBISCUS SABDARIFFA

Bioactive components
In terms of it’s therapeutic value, roselle's main components are a polysaccharide, organic acid, and
flavonoids, particularly anthocyanins. One of the think about the extracts of dried calyces are to
include chemical compenent. Forinstance organic acids ( citric acid, tartaric acid, oxalic acid, maleic
acid, hibsicic acid, asborbic acid) besides, phtosterols, polyphenols, anthocyanins and other water-
soluble antioxidants. There if bioactive components with organic acids are all together, they have free
radical scavenging activity. In that case the biactive molecules immsenly effect health of a person in a
good way. Also indicate the polyphenolic part present in the concentrates of Hibiscus sabdariffa as
announced by various examination gatherings.

(alt başlık) Organic acid


One of the research indicates that high concentration of organic acids like oxalic acid, succinic acid,
tartaric acid; malic acid, citric acid. These are the last of predominant ones. Also Jabuer et al stated
oxalic acid, shikimic and fumaric acids as the main orgamic acid with malic acid (9.10 g/100 g) to be
the the most abundant

acid in the calyces of roselle.

(alt başlık) Polyphenols and flavonoids


The roots of many therapeutic maerials is because of the secondary metobolisms in the plants.
Roselle calyces are an intriguing source of potential vioactive molecules with antioxidant,
hypocholesterolemic antihypertensive, antimicrobial, anti-inflammatory, antidiabetic and
anticarcinogenic activities. Researches bring the light of the fact that the calyces of roselle are
intensive in polyphenols and flavonoids that improve the nutritious worth of roselle as these these
mixtures are connected with their antioxidant property The phenolic content in the plant comprises
for the most part of anthocyanins like delphinidin-3-glucoside, sambubioside, and cyanidine-3-
sambubioside and other flavonoids like gossypetine, hibiscetin and their respective glycosides;
protocatechuic acid, eugenol, and sterol like β-sitoesterol and ergoesterol. The colourful anthocyanins
are the members of the flavonoids group of phytochemicals. Anthocyanins molecules are responsive
to deteriation. The stability of it comes from the pH, temperature, the presence of enzyme, light, and
structure, the presence of other flavonoids, phenolic acids and metals

(alt başlık) Anthocyanins of Hibiscus sabdariffa

The reports of Ali et al. and Gradinaru et al. consisting 2 major athocynanins compounds.
(delphinidine-3-sambubioside and cyanidine-3-sambubioside)and 2 minor compounds(delphinidine-
3-glucoside and cyanidine-3-glucoside) It’s in the roselle’s calyces. Also paralel findings have reported
by Pouget et al. and Bridle and Timberlake. Therefore the studies of Tsai et al. notified that 85% of
anthocyanins is delphinidine-3- sambubioside those are one of the crucial source of antioxidant
antioxidant capacity of roselle extract. The other study by aurelio et al. concluded that the extracts of
roselle calyce are powerful in anthocyanins like delphinidine-3-glucpside sambubioside and cyanidin-
3-sambubioside Contributes to antioxidant properties . Scientest mostly used an aqueous or organic
solvent to extract the polyphenols and anthocyanins from the roselle calyces. Dissimilar extraction
methods and different varieties of Hibiscus sabdariffa used in various resarches is making the
comparing part harder. Another scientest Luvongo et al. claimed total phenolic content to be 6.06
mg/g in roselle extract. Dried roselle contained total anthocyanins as cyanidine 3-glucoside 622.91
mg/100 g and 37.42 mg/g total phenolic content in dry weight sample Recently Jabeur et al. in their
study defiened delphinedine-3-o-sambubioside, delphinidine-3-o glucoside and cyanidine-3-o
sambubioside in the concentration of (7.03 mg/g), (1.54 mg/g) and (4.40 mg/g) in order of.

4.PHARMACOLOGICAL EFFECTS

Anti-oxidant effect
Antioxidative activity is the protective ability of a substance to scavenge reactive oxygen and free
radicals, thereby inhibiting the oxidative mechanisms. It lessens aging and shields lining organelles
from early cell damage. Numerous in vitro and in vivo investigations have demonstrated the strong
antioxidant content of Roselle calyxes. Both the entire aqueous and anthocyanin-rich extracts of
Roselle are potent antioxidants, according to Augustine. Research has also demonstrated the
powerful antioxidant properties of polyphenolic acid, flavonoids, and anthocyanins present in roselle.

Antihyperlipidemic effect
Many investigations have demonstrated the hypolipidemic effectiveness of Hibiscus sabdariffa extract
(HSE), indicating that roselle may have potential as an antiobesity medication. The hallmark of obesity
is weight increase brought on by an excessive buildup of bodily fat. A high-fat diet combined with an
unbalanced energy intake leads to obesity, which is linked to a number of metabolic syndromes,
including insulin resistance, fatty liver, and cardiovascular risk factors (hyperlipidemia and
hypertension) Early cellular processes and disturbance of normal cellular homeostasis are
characteristics of these metabolic diseases. Due to their multi-targeted effects on obesity and its
effects on human health, polyphenols derived from Hibiscus sabdariffa have the potential to be
auxiliary in this pathology due to their pleiotropic character. These effects include the regulation of
energy metabolism, oxidative stress and inflammatory pathways, transcription factors, hormones and
peptides, digestive enzymes, and epigenetic modifications. Clinical investigations involving humans
and animals have provided proof that HSE lowers hyperlipidemia. According to a study, feeding
hypercholesterolemic rats a dose of 5–10% HSE for nine weeks decreased the lipid fraction in the
liver, kidney, heart, and plasma. In a related study, it was found that after receiving cholesterol for ten
weeks, rabbits treated with 0.5 or 1% HSE had lower serum levels of triglycerides, total cholesterol,
and low-density lipoprotein (LDL).

Antidiabetic effect
Evidence is increasingly emerging regarding the potential of H. sabdariffa to control diabetes. Peng et
al. studied the composition of H. sabdariffa polyphenolic extract in a technical way and used a rat
model of type 2 diabetes to test its protective effect. Treatment with phenolic-rich extract reduced
hyperglycemia and hyperinsulinemia, which increased with maximum efficacy at 200 mg/kg. The
extract reduced serum triacylglycerol, cholesterol, and low-density lipoprotein/high-density
lipoprotein ratio. The extract significantly reduced the abnormal elevation in plasma advanced
glycation end (AGE) formation by inhibiting the expression of receptors. Adisakwattana et al. [25]
investigated plants, including H. sabdariffa, for intestinal -glucosidase and pancreatic -amylase
inhibition. When combined with chrysanthemum, butterfly pea, and mulberry extract, it provided
additional maltase inhibition in the gut. On the other hand, its combination with chrysanthemum and
mulberry caused synergistic inhibition of pancreatic amylase. Ademiluyi and Oboh [26] also
investigated the inhibitory effect of aqueous extracts of two varieties (red and white) of H. sabdariffa
calyces on -amylase and -glucosidase. The red variety exhibited higher -glucosidase inhibitory activity,
while the white variety exhibited higher -amylase inhibitory activity. -glucosidase inhibitory activities
of both calyces were higher than those of -amylases. The red variety had strong antioxidant capacity
due to its high phenolic content. Wisetmuen et al. [27] investigated the mechanism underlying the
antihyperglycemic activity of its ethanolic extract in diabetic rats. When administered at a dose of 1
g/kg per day for 6 weeks, the extract significantly reduced blood sugar levels and increased basal
insulin levels. Histological examination showed that the extract increased the number of islets of
Langerhans in diabetic rats. Collectively, the inhibition of intestinal -glucosidase and pancreatic -
amylase activities, combined with its abundance of antioxidants, establish H. sabdariffa as a
promising adjunctive therapy for diabetes.

Antihypertensive effect
A persistent medical disorder affecting the heart that raises arterial blood pressure is called
hypertension. This health issue is prevalent in both developed and underdeveloped nations. Hibiscus
sabdariffa (HS) has historically been used as an antihypertensive medication. Cardiovascular disorders
are associated with the historical usage of HS. In both animal and human models, Hibiscus sabdariffa
extract (HSE) has been shown in numerous scientific research papers to considerably lower blood
pressure.Haji Tarkhani and Haji Faraji assessed how HS tea affected hypertension. When the
treatment was stopped after three days, the systolic and diastolic blood pressure increased by 5.6%
and 6.2%, respectively. The first single trial involved 54 patients with moderate hypertension and
showed a reduction in blood pressure (systolic by 11.2% and diastolic by 10.7%) in 12 days. Herrera-
Arellano et al. demonstrated that HS aqueous extract safely and successfully decreased blood
pressure by over 10% in a randomized experiment including 75 patients. The extract was also found
to be superior to 25 mg of captopril. Herrera-Arellano et al. conducted a study whereby they
examined the impact of standardized Hibiscus sabdariffa extract in a 4-week clinical trial that was
double-blind, randomized, and controlled with lisinopril for 171 individuals with hypertension. Blood
pressure (BP) was dropped by HS extract, but the effect was not as great as it was for the patient
receiving 10 mg of lisinopril. This suggests that HS extract had a significant antihypertensive effect
with a broad margin of safety and tolerance.

hepatoprotective effect

A strong protective effect of dried flower extracts against the imbalance between free
radicals and antioxidants has been demonstrated in rat primary liver cells (hepatocytes).
Protocatechuic acid, a simple phenolic compound from H. sabdariffa, showed protective
effects against t-BHP-induced hepatocyte cell malfunction and DNA mutation. One
mechanism may be linked to its ability to scavenge free radicals. An extract of its leaves
protected rats against cadmium-induced liver, prostate and testicular fat oxidation. The
extract provides liver protection by affecting the levels of ammonia excess lipid peroxidation
products and liver marker enzymes in the experimental blood, which is largely attributed to
the free radical scavenging properties of the natural antioxidants present in the plant.
Protective effects of the aqueous extract and anthocyanins on paracetamol-induced liver
damage in rats were also observed. Aqueous ethanol (1:1) extract of calyx was observed to
show a significant reduction in lipid peroxidation level in carbon tetrachloride-induced
Hepatotoxicity. However, another study also observed that long and frequent use of aqueous
methanol extract of calyces may cause hepatotoxicity.
antibacterial effect
The bacterial growth inhibiting activity of the methanol extract of H. sabdariffa calyces was
evaluated by the method of discs impregnated with certain doses of antibiotics as reported
in Abdallah and Al-Harbi; 100 μl of each working bacterial culture was shaken, spun, firmed,
and mixed thoroughly with 20 ml of warm autoclaved Mueller-Hinton agar (Watin-Biolife,
KSA) in 50-ml glass vials and then directly onto 90-mm sterile disposable plastic plates (Jalil
Medicals) was shed. ) and left to solidify (dry) at 20 to 24°C. 6 mm disks were previously
prepared using Whatman No.1 filter paper, all microbes were accurately killed and saturated
with 300 mg/ml methanol extract of H. sabdariffa calyx, preliminary experimental testing
showed that the empty disk (6 mm) had a capacity of 20 μl. . extract at a concentration of
500 mg/ml, which is equivalent to 10 mg/disc. Wet, saturated discs were then loaded
directly onto a Mueller-Hinton Agar plate, where the microorganisms were cultured into a
protected area. 6 mm antibiotic discs on the same plate; Penicillin G 10 units and gentamicin
10 μg (Oxoid), which served as positive controls, were also loaded. Cultured plates containing
extract and antibiotic disks were incubated at 37°C for approximately 1 day. The common
denominator junction area of two disks copied on the same plate was taken in millimeters
(mm) using a ruler; At 6 mm zone diameter, inhibition was observed.

immunomodulation effect

This concept of immune responses being developed to reduce and weaken disease is found
in many alternative medicine beliefs; Plants were used to improve health in times when our
immunity was low and to strengthen the immune system and protect the body's resistance
against microbes entering the body. Some of these herbs are specifically stimulatory or
suppressive and normalize or modulate disease processes and are therefore called
'immunomodulators'. extracts to some extent and to a large extent the two subheadings of
the plant have the ability to stimulate the immune system in vivo. The activity provides a
final insight into the interaction between interleukin 10 production, inhibition of tumor
necrosis factor-alpha, and the action of B cells responsible for meeting the immunoglobulin
requirement. For the sake of thought, it has made great strides in being developed into a
drug entity that can be used to stimulate the immune system, aiding in the treatment of the
immunocompromised when the immune system is weakened or collapsed. However, in
humans, the extract taken as a beverage may play a major role in activating the immune
system. More qualified and detailed research is needed to fully evaluate the mechanism of
action of hibiscus.
diuretic effect

Adrenaloctomized rats were administered hibiscus extract, and fractions were extracted
using solvents of varying polarity. The diuretic effect was examined together with
deoxycorticosterone acetate, an aldosterone analogue. Finally, the effect of diuretic active
extracts on the gene expression of the alpha subunit from the transporter of renal epithelial
cells (αENaC) was observed and the effect as an intermediary was evaluated. On renal
filtration in an in situ kidney model. According to the observed results, the chemical structure
of Hibiscus sabdariffa aqueous extract was as follows: 32.4 mg/g delphinidin-3-O-
sambubioside, 11.5 mg/g cyanidin-3-O sambubioside, 11.5 mg/g quercetin and 2.7 mg/g
quercetin. mg/g chlorogenic acid. While the ratio of flavonoids and chlorogenic acid
increased rapidly during the extraction process, the presence of anthocyanins decreased
over time as a result of the gradual decrease in the polarity of the solvents and remained
very low at the end of the process. Adrenalectomy-induced diuresis in rats was balanced by
deoxycorticosterone acetate activity. However, spironolactone, Hibiscus sabdariffa aqueous
extract and oral acetonitrile:methanol 5:5 combination extract all abolished the effect
achieved by deoxycorticosterone acetate. A comparable effect was noted on renal filtration
derived from the isolated kidney model. Another reason why Hibiscus sabdariffa has such
nice effects as diuretic, natriuretic, and potassium-sparing is that there are chemicals in the
plant's extract that are potentially responsible for modulating aldosterone activity. Quercetin,
a chemical found in Hibiscus sabdariffa, releases the nice-for-us oxide nitric oxide in the
vascular endothelium, which increases renal vasorelaxation by increasing kidney filtration.
The main function of nitric oxide is revealed, causing the diuretic property of Hibiscus
sabdariffa.

Treatment of anemia
Hibiscus sabdariffa (Hs) is very rich in iron and ascorbic acid. For this reason, it has become
the type frequently mentioned against anemia. This ascorbic acid contributes to the
absorption of non-existent iron, which also largely justifies its anti-anemic status in
alternative medicine. Pharmacologically, Hibiscus sabdariffa (HS) extract is effective in
mammalian It has been tested in animals and humans and has shown high hematocrit and
hemoglobin results. Adıgün et al. observed the effect of the aqueous extract of Hibiscus
sabdariffa on hematological parameters such as hemoglobin, the ratio of the volume formed
by red blood cells to the total blood volume, and total and differential white blood cell count,
and recommended a dosage of 200-400 mg/kg to be beneficial. Rats were given oral doses of
200-1000 mg/kg body weight for up to 14 days. After 14 days, a significant increase in the
ratio of the volume formed by red blood cells to the total blood volume and hemoglobin was
observed in the animal group given a dose of 200-400 mg per kg. However, higher doses
showed a significant decrease in the ratio of the volume of red blood cells to the total blood
volume, but this decrease was not observed in hemoglobin. It suggests that application of
the aqueous extract of Hibiscus sabdariffa is beneficial for blood cells. Anemia is an iron
deficiency disease in which there is less presence of red blood cells (RBCs) in the blood. RBC's
main function is to carry oxygen to body cells. It is thought that the anti-anemic activity of
Roselle extract, its minimal pH, and its high ascorbic acid concentration, which increases
mineral bioavailability, are responsible for this. Studies on the anti-anemic activity of Roselle
extract are insufficient yet, and more qualified studies and knowledge are needed to
investigate the great potential and mechanism of action of Roselle in the treatment of
anemia.

anticancer effect
Anthocyanins can cause programmed cell death in cancer cells, especially in HL-60 cells. The
antioxidative activity of anthocyanins was evaluated by their effects on LDL oxidation in the cell-free
system and their ability to inhibit programmed cell death in RAW264.7 cells. showed that
anthocyanins of this plant can be used to inhibit LDL oxidation and oxLDL-mediated macrophage
programmed cell death, acting as an agent that inhibits cancer development. The inhibitory effect of
protocatechuic acid on tumor progression in mouse skin has demonstrated in studies that
protocatechuic acid has great potential as an anticancer agent against tumor progression.

The dosage of the extract


It is difficult to elucidate dosing recommendation because of the heterogeneity in the studies
related to the bioactivity of the poly phenolic contents of Hibiscus sabdariffa. The extraction
methods and products used in other studies are different. The doses that are used in each of
the positive studies are gives.

Doses of the extract of Hibiscus sabdariffa with biological activity.


TOKSIK
In the past, hibiscus extract has been the subject of many authors' studies on the reproduction and
development of rats. Hibiscus extract was added to the daily drinking water of female rats in certain
doses. As a result, a decrease in the daily food intake of female rats was observed. In baby rats, this
effect delayed puberty and dose-dependent weight gain. As mentioned by the authors, the resulting
effects are due to the decrease in food intake. One of the major factors in the decrease in food intake
may be the fact that mice do not like the taste of hibiscus, rather than the direct toxic properties of
hibiscus (Iyare & Adegoke, 2008a,b; Iyare et al., 2010).
In the researched articles, extracts of hibiscus are associated with small amounts of toxicity. The
LD50 of hibiscus extract in rats was found to be over 5000 mg/kg (Onyenekwe et al., 1999) as a result,
hibiscus extract has almost no toxic properties. In rats that are already hypertensive, 500-1000 mg/kg
was found. Hibiscus extract in kg doses reduced blood pressure, accordingly, it also reduced serum,
creatinine, cholesterol and glucose values to a high extent, but it also increased uric acid properties to
the same extent.

Kidney function, serum creatinine and uric acid levels of hypertensive and normal-tensive mice were
measured. The serum creatinine level of mice in the hypertensive group was significantly higher than
that of mice in the normatensive group.

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