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Aim To Enhance The Solubility of The Curcumin by Metal Complexation Method - 20250105 - 040344 - 0000

The document outlines a study aimed at enhancing the solubility of curcumin, a compound derived from turmeric, through metal complexation methods. The primary objectives include significantly increasing curcumin's aqueous solubility, maintaining its stability, and improving its bioavailability to enhance therapeutic effects. The rationale emphasizes that improved solubility can lead to better absorption, reduced side effects, and the potential for new drug delivery systems.

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0% found this document useful (0 votes)
34 views12 pages

Aim To Enhance The Solubility of The Curcumin by Metal Complexation Method - 20250105 - 040344 - 0000

The document outlines a study aimed at enhancing the solubility of curcumin, a compound derived from turmeric, through metal complexation methods. The primary objectives include significantly increasing curcumin's aqueous solubility, maintaining its stability, and improving its bioavailability to enhance therapeutic effects. The rationale emphasizes that improved solubility can lead to better absorption, reduced side effects, and the potential for new drug delivery systems.

Uploaded by

dnyanadamohod1
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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AIM: TO ENHANCE

THE SOLUBILITY OF
THE CURCUMIN BY
METAL
COMPLEXATION
METHOD

#Curcumin is a bright yellow


chemical produced by plants of the
Curcuma longa species.

#It is the principal curcuminoid of


turmeric (Curcuma longa), a member
of the ginger family, Zingiberaceae
CHALLENGES
IN USE OF CURCUMIN
USES
OBJECTIVE
:
* Significantly increase the aqueous solubility of curcumin: This is the core
objective. The study should aim to develop a method or formulation that
substantially improves curcumin's solubility in water.
* Maintain curcumin's stability: The chosen method should not significantly
degrade curcumin or reduce its therapeutic activity.
* Improve curcumin's bioavailability: The enhanced solubility should translate to
a significant increase in the amount of curcumin that is absorbed by the body.
ISSN 0974-3618 (Print) www.rjptonline.org
0974-360X (Online)
REVIEW ARTICLE
PHARMACOLOGICAL ACTIVITIES OF CURCUMIN: AN UPDATE
Aya Yaseen Mahmood Alabdali1
, Sasikala Chinnappan2*,
Basma M. Abd Razik3
, Mogana R4
, Shaik Ibrahim Khalivulla5
, Rahman H6
1The University of Mashreq, Collage of Pharmacy, Iraq, Baghdad.
2,4,5Faculty of Pharmaceutical Sciences, UCSI University Kuala Lumpur (South
Wing),
No.1, Jalan Menara Gading, UCSI Heights 56000 Cheras, Kuala Lumpur, Malaysia.

LITERATURE
3Department of Pharmaceutical Chemistry, College of Pharmacy,
Mustansiriyah University, 10001, Baghdad, Iraq.
*Corresponding Author E-mail: [email protected]

REVIEW 1
ABSTRACT:
In the past few years, multiple drugs have been produced from traditional
materialand recent pandemic
disease COVID-19 once again research on this matter is being conducted to
determine potential therapeutic
purposes of different Ayurvedic Indian medicines and herbs. One such medicinal
herb is Curcuma longa.
Curcumin is strong antioxidant, anti-inflammatory, antispasmodic, antiangiogenic,
anti-carcinogenic, as shown
by multiple in vitro and in vivo studies. The action of the growth factor receptors is
inhibited by curcumin. The
anti-inflammatory effect of curcumin is obtained on the cytokines, proteolytic
enzymes, eicosanoids, and lipid
mediators. The superoxide radicals, nitric oxide and hydrogen peroxide, are sifted
by curcumin, while lipid
peroxidation is inhibited. Such properties of the compound thus form the
foundation for its various therapeutic
and pharmacological effects could also hold antiviral properties including COVID-
19. The aim of this research is
to summarize the updated pharmacological activities of curcumin
2.
Alsamydai and Jaber, IJP, 2018; Vol. 5(6): 313-326. E- ISSN: 2348-3962, P-ISSN: 2394-5583
International Journal of Pharmacognosy 313
IJP (2018), Vol. 5, Issue 6 (Review Article)
Received on 09 February, 2018; received in revised form, 21 March, 2018; accepted, 30 March, 2018; published 01
June, 2018

PHARMACOLOGICAL ASPECTS OF CURCUMIN: REVIEW ARTICLE


Ali Alsamydai *
and Nisrein Jaber
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Jordan,
Amman, Jordan.
ABSTRACT: Turmeric (Curcuma longa) is widely used popular
Indian medicinal plant which belongs to the family of
Zingiberaceae. Curcumin, an important constituent of turmeric, is
known for various biological activities, primarily due to its
antioxidant mechanism. Epidemiological observations are
suggestive that turmeric consumption may reduce the risk of some
form of cancers and render other protective biological effects in
humans like antidiabetic, anti-inflammatory, anti-angiogenic, anti�oxidant, wound healing and anti-cancer effects.
This review
summarizes the most interesting biological effects of curcumin.
3. CURCUMIN AND ITS DERIVATIVES AS POTENTIAL THERAPEUTIC
AGENTS IN PROSTATE, COLON AND BREAST CANCERS
Zintle Mbese, Vuyolwethu Khwaza and Blessing Atim Aderibigbe *
Department of Chemistry, University of Fort Hare, Alice Campus, Alice 5700, Eastern Cape, South Africa;
[email protected] (Z.M.); [email protected] (V.K.)
* Correspondence: [email protected] or [email protected]; Tel.: +27(0)-406-022-266;
Fax: +086-662-8802
Academic Editors: Erika Ferrari and Carol Imbriano
Received: 30 August 2019; Accepted: 3 October 2019; Published: 30 November 2019


Abstract: Cancer is a life-threatening disease and is the second leading cause of death around the
world. The increasing threats of drug-resistant cancers indicate that there is an urgent need for the
improvement or development of more effective anticancer agents. Curcumin, a phenolic compound
originally derived from turmeric plant (Curcuma longa L. (Zingiberaceae family)) widely known as
a spice and a coloring agent for food have been reported to possess notable anticancer activity by
inhibiting the proliferation and metastasis, and enhancing cell cycle arrest or apoptosis in various
cancer cells. In spite of all these benefits, the therapeutic application of curcumin in clinical medicine
and its bioavailability are still limited due to its poor absorption and rapid metabolism. Structural
modification of curcumin through the synthesis of curcumin-based derivatives is a potential approach
to overcome the above limitations. Curcumin derivatives can overcome the disadvantages of curcumin
while enhancing the overall efficacy and hindering drug resistance. This article reports a review of
published curcumin derivatives and their enhanced anticancer activities.
Keywords: curcumin; anticancer activity; derivatives of curcumin; drug resistance; breast cancer;
prostate cancer; colon cancer
1.
4.
CURCUMIN ANALOGUES AND DERIVATIVES WITH ANTI-PROLIFERATIVE AND ANTI-INFLAMMATORY
ACTIVITY: STRUCTURAL CHARACTERISTICS AND MOLECULAR TARGETS
Eirini Chainoglou and Dimitra Hadjipavlou-Litina
Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, Thessaloniki, Greece
ABSTRACT
Introduction: Curcumin (Diferuloylmethane) is a natural phenolic compound, which belongs to the
curcuminoid family, presenting pleiotropic activity and low bioavailability. A lot of recent research is
focused on the design and synthesis of curcumin analogs as antiproliferative and anti-inflammatory
agents improving the bioavailability and target selectivity. Their structural characteristics and functional
groups seem to define the extent of the biological activity.
Areas covered: Publications (2008–2018), describing curcumin analogs and curcumin derivatives are
analyzed. Structural characteristics, functional groups, modelling studies, structure activity relationships,
biological evaluation in vitro/in vivo as antiproliferative and anti-inflammatory agents are included.
Furthermore, a wide range of biological results derived from different targets are also summarized.
Expert opinion: Several curcumin analogs and derivatives appear to have a high biological impact as
well as promising antiproliferative and anti-inflammatory activities. Their clinical evaluation will be
critical to assess therapeutic utility. Compounds for which the mechanism of action is well defined
can serve as lead compounds for the design of new more potent molecules.
ARTICLE HISTORY
Received 27 February 2019
Accepted 30 April 2019
KEYWORDS
Antiproliferative; anti�inflammatory; curcumin
analogs; modelling studies;
structure activity
relationship
5. A REVIEW OF CURCUMIN AND ITS DERIVATIVESIN ANTICANCER
AGENTS
Mhd Anas Tomeh 1
, Roja Hadianamrei 1 and Xiubo Zhao 1,2,*
1 Department of Chemical and Biological Engineering, University of Sheffield, Sheffield S1 3JD, UK;
[email protected] (M.A.T.); [email protected] (R.H.)
2 School of Pharmaceutical Engineering and Life Science, Changzhou University, Changzhou 213164, China
* Correspondence: [email protected]; Tel.: +44-(0)-0114-222-8256
Received: 6 February 2019; Accepted: 21 February 2019; Published: 27 February 2019


Abstract: Cancer is the second leading cause of death in the world and one of the major public
health problems. Despite the great advances in cancer therapy, the incidence and mortality rates of
cancer remain high. Therefore, the quest for more efficient and less toxic cancer treatment strategies
is still at the forefront of current research. Curcumin, the active ingredient of the Curcuma longa
plant, has received great attention over the past two decades as an antioxidant, anti-inflammatory,
and anticancer agent. In this review, a summary of the medicinal chemistry and pharmacology
of curcumin and its derivatives in regard to anticancer activity, their main mechanisms of action,
and cellular targets has been provided based on the literature data from the experimental and clinical
evaluation of curcumin in cancer cell lines, animal models, and human subjects. In addition, the recent
advances in the drug delivery systems for curcumin delivery to cancer cells have been highlighted.
Keywords: curcumin; anticancer; structure activity relationship; cellular pathway; mechanism of
action; delivery system
6.
Synthesis and characterization of dual function vanadyl, gallium
and indium curcumin complexes for medicinal applications
Khosro Mohammadi a,1, Katherine H. Thompson a,*, Brian O. Patrick a
, Tim Storr a
,
Candice Martins a
, Elena Polishchuk a
, Violet G. Yuen b
, John H. McNeill b
,
Chris Orvig a,*
a Medicinal Inorganic Chemistry Group, Chemistry Department, University of British Columbia, Vancouver, BC, Canada V6T 1Z1 b Faculty of Pharmaceutical
Sciences, University of British Columbia, Vancouver, BC, Canada V6T 1Z3
Received 6 June 2005; received in revised form 19 July 2005; accepted 8 August 2005
Available online 19 September 2005
Abstracts
Novel bis[4-hydroxy-3-methoxyphenyl]-1,6-heptadiene-3,5-dione (curcumin) complexes with the formula, ML3, where M is
Ga(III) or In(III), or of the formula, ML2 where M is [VO]2+, have been synthesized and characterized by mass spectrometry, infra�red and absorption
spectroscopies, and elemental analysis. A new ligand, bis[4-acetyl-3-hydroxyphenyl]-1,6-heptadiene-3,5-dione
(diacetylbisdemethoxycurcumin, DABC) was similarly characterized; an X-ray structure analysis was performed. Vanadyl com�plexes tested in an acute i.p. testing
protocol in STZ-diabetic rats showed a lack of insulin enhancing potential. Vanadyl complexes
were, however, more cytotoxic than were the ligands alone in standard MTT (3-[4,5-dimethylthiazole-2-yl]ate, -2,5-diphenyl-tetra�zolium bromide) cytotoxicity
testing, using mouse lymphoma cells. With the exception of DABC, that was not different from
VO(DABC)2, the complexes were not significantly different from one another, with IC50 values in the 5–10 lM range. Gallium
and indium curcumin complexes had IC50 values in the same 5–10 lM range; whereas Ga(DAC)3 and In(DAC)3 (where
DAC = diacetylcurcumin) were much less cytotoxic (IC50 = 20–30 lM). Antioxidant capacity was decreased in VO(DAC)2,
Ga(DAC)3, and In(DAC)3, compared to vanadyl, gallium and indium curcumin, corroborating the importance of curcumins free
phenolic OH groups for scavenging oxidants, and correlated with reduced cytotoxic potential.
 2005 Elsevier Inc. All rights reserved.
rationale
* Curcumin's poor water solubility limits its absorption in the body. Increasing solubility leads to
better absorption in the gastrointestinal tract, resulting in higher levels of curcumin reaching target
tiss
* Higher bioavailability translates to increased therapeutic effects. This is crucial for reaping the full
benefits of curcumin's potential anti-inflammatory, antioxidant, and anti-cancer properties.
* With improved solubility, lower doses of curcumin may be needed to achieve the same therapeutic
outcome. This can reduce the potential for side effects and improve patient complianc
* Increased solubility expands the potential for developing new drug delivery systems and
formulations for curcumin. This could enable its use in various therapeutic areas, such as oral, topical,
and intravenous administratio
* Solubility enhancement allows for the creation of more stable and palatable formulations, such as
solutions, suspensions, and emulsions. This improves the ease of administration and patient
acceptance.
* In some cases, increasing solubility can also enhance the stability of curcumin, protecting it from
degradation and extending its shelf life.
* Solubility enhancement can facilitate the combination of curcumin with other drugs or
nutraceuticals. This could lead to synergistic effects and improved overall treatment
PLAN OF ACTION
01 02 03 04

Data analysis
Litrature review Synthesis of Evaluation
and
and background Curcumin
derivative
conclusion
understanding
THANK YOU

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