Dendrite elongation inhibitor from Artocarpus altilis Parkinson

Rao, G. Gopala; Gopalakrishnan, M.; Madhavi, M.; Mukhopadhyay, T.; Thanusu, J.; Ezhilarasi, M.R.

doi:10.1016/j.jopr.2013.03.024

Cited by 2 publications

(3 citation statements)

References 11 publications

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“…Several compounds have been reported to modulate melanocyte dendricity, which, in part, explains their effects on the subsequent steps of melanogenesis. For example, a combination of natural Curcuma zedoaria and aloe vera extracts inhibited melanin synthesis and total dendrite length in mouse melanoma cells [ 7 ] and another study reported on another natural extract which inhibited melanin synthesis and total dendrite length in B16F10 cells [ 6 ]. Another plant-based compound, methylophiopogonanone B, was shown to induce dendrite retraction and inhibit melanosome transfer in primary human melanocytes [ 50 ].…”

Section: Discussionmentioning

confidence: 99%

“…For the efficient export of melanosomes by melanocytes, both the dendrite length and number of dendrites are critical components, as melanocytes can branch out by increasing their number of dendrites to contact multiple keratinocytes that are in close proximity and can also elongate their dendrites to export pigment to multiple keratinocytes surrounding them in the suprabasal layers of the epidermis. The inhibition of melanosome export is emerging as a novel target when designing inhibitors of excessive pigmentation and a large number of reports [ 6 , 7 , 8 , 9 ], including our previous studies [ 10 , 11 , 12 ], have described compounds which can inhibit dendricity and thus have the potential to suppress export of melanosomes.…”

Section: Introductionmentioning

confidence: 99%

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Novel Chemically Modified Curcumin (CMC) Analogs Exhibit Anti-Melanogenic Activity in Primary Human Melanocytes

Goenka

Simon

2021

IJMS

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Hyperpigmentation is a dermatological condition characterized by the overaccumulation and/or oversecretion of melanin pigment. The efficacy of curcumin as an anti-melanogenic therapeutic has been recognized, but the poor stability and solubility that have limited its use have inspired the synthesis of novel curcumin analogs. We have previously reported on comparisons of the anti-melanogenic activity of four novel chemically modified curcumin (CMC) analogs, CMC2.14, CMC2.5, CMC2.23 and CMC2.24, with that of parent curcumin (PC), using a B16F10 mouse melanoma cell model, and we have investigated mechanisms of inhibition. In the current study, we have extended our findings using normal human melanocytes from a darkly pigmented donor (HEMn-DP) and we have begun to study aspects of melanosome export to human keratinocytes. Our results showed that all the CMCs downregulated the protein levels of melanogenic paracrine mediators, endothelin-1 (ET-1) and adrenomedullin (ADM) in HaCaT cells and suppressed the phagocytosis of FluoSphere beads that are considered to be melanosome mimics. All the three CMCs were similarly potent (except CMC2.14, which was highly cytotoxic) in inhibiting melanin production; furthermore, they suppressed dendricity in HEMn-DP cells. CMC2.24 and CMC2.23 robustly suppressed cellular tyrosinase activity but did not alter tyrosinase protein levels, while CMC2.5 did not suppress tyrosinase activity but significantly downregulated tyrosinase protein levels, indicative of a distinctive mode of action for the two structurally related CMCs. Moreover, HEMn-DP cells treated with CMC2.24 or CMC2.23 partially recovered their suppressed tyrosinase activity after cessation of the treatment. All the three CMCs were nontoxic to human dermal fibroblasts while PC was highly cytotoxic. Our results provide a proof-of-principle for the novel use of the CMCs for skin depigmentation, since at low concentrations, ranging from 5 to 25 µM, the CMCs (CMC2.24, CMC2.23 and CMC2.5) were more potent anti-melanogenic agents than PC and tetrahydrocurcumin (THC), both of which were ineffective at melanogenesis at similar doses, as tested in HEMn-DP cells (with PC being highly toxic in dermal fibroblasts and keratinocytes). Further studies to evaluate the efficacy of CMCs in human skin tissue and in vivo studies are warranted.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Novel Chemically Modified Curcumin (CMC) Analogs Exhibit Anti-Melanogenic Activity in Primary Human Melanocytes

Goenka

Simon

2021

IJMS

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“…Pencerah kulit merupakan salah satu komponen penting dalam perawatan kulit yang dapat dilakukan dengan menghilangkan dendrisitas melanosit untuk mengendalikan warna kulit. Ekstrak metanol daun sukun, fraksi etil asetatnya, dan juga senyawa 2-geranil-2',3,4,4'tetrahidroksi dihidrokalkon menujukkan aktivitas penghambatan terhadap dendrisitas melanosit yang baik pada konsentrasi 50 μg/mL (Rao et al, 2013).…”

Section: Pelindung Radiasi Uvunclassified

KAJIAN ETNOBOTANI, FITOKIMIA, FARMAKOLOGI DAN TOKSIKOLOGI SUKUN (Artocarpus altilis (Park.) Fosberg)

Yumni¹,

Widyarini²,

Fakhrudin

2021

J. Tumbuhan Obat Indonesia

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ABSTRACT Indonesia is a country with large plant biodiversity with medicinal properties, such as “sukun” (Artocarpus altilis) or known as “breadfruit”. Breadfruit is a woody evergreen plant that has been used traditionally for various purposes, including medication. The fruit is rich in carbohydrates and fibers as a food source. The leaf and cortex are the most widely used for treating various diseases and other health benefits. This article aimed to present a comprehensive review on the potency of breadfruit from the perspective of ethnobotany, phytochemistry, pharmacology, and toxicology. The data in this narrative review was obtained from the scientific journals in the databases of Google Scholar, PubMed, Scopus, and ScienceDirect. Other credible sources, such as textbooks, student thesis, and patents were also used to support the main data. Based on the literature study, breadfruit has been used empirically in Indonesia as a medicinal herb. The scientific data of breadfruit showed antiinflammatory, antiplatelet, antioxidant, antiatherosclerosis, antihyperlipidemic, antimalaria, antidiabetic, cardioprotective, and anticancer activities. Breadfruit contains terpenoids, flavonoids, alkaloids, and phenolics as bioactive compounds. However, the unique compounds are geranylated and prenylated flavonoids such as cycloartenol, artonin V, and cyclomulberin. These compounds are distributed in the leaf, cortex, wood, and fruit. Limited data is available regarding the toxicology profile of breadfruit. Breadfruit leaves ethanol extract did not show any significant toxic effects in the animal experiments. However, the toxicity of the water extract is unclear, and thus, needs to be investigated to ensure its safety. Keywords: Artocarpus communis, bioactivity, chemical constituents, ethnopharmacology ABSTRAK Indonesia dikenal sebagai negara yang kaya akan keragaman tumbuhan berpotensi obat, diantaranya sukun (Artocarpus altilis). Sukun merupakan tanaman berkayu yang secara tradisional dimanfaatkan untuk berbagai keperluan termasuk pengobatan. Buah sukun mengandung karbohidrat dan serat sebagai sumber pangan. Daun dan batang sukun merupakan bagian yang paling banyak dimanfaatkan dalam pengobatan dan kesehatan. Reviu artikel ini bertujuan untuk mengkaji secara komprehensif potensi sukun dari sudut pandang etnobotani, fitokimia, farmakologi, dan toksikologi. Artikel narrative review ini ditulis berdasarkan data yang diperoleh dari kajian literatur hasil penelitian yang ada di basis data Google Scholar, PubMed, Scopus, dan ScienceDirect. Beberapa sumber pustaka lain seperti buku, naskah tugas akhir dan paten juga digunakan untuk memperkaya penulisan. Hasil kajian literatur sukun menunjukkan bahwa tanaman ini memiliki riwayat empiris digunakan sebagai obat tradisional di Indonesia. Hasil penelitian ilmiah menunjukkan sukun memiliki aktivitas antiinflamasi, antiplatelet, antioksidan, antiatherosklerosis, antihiperlipi-demia, antimalaria, antidiabetes, kardioprotektif, dan antikanker. Sukun mengandung senyawa terpenoid, flavonoid, alkaloid, dan senyawa fenolik. Senyawa khas dari tumbuhan genus Artocarpus ini adalah flavonoid dengan gugus geranil atau prenil, misalnya sikloartenol, artonin V, dan siklomulberin. Senyawa tersebut tersebar dalam daun, kulit kayu, batang, dan buah. Data terkait profil toksikologi sukun masih terbatas. Ekstrak etanol daun sukun tidak menunjukkan efek toksik pada hewan uji. Namun, ekstrak airnya belum memiliki profil toksikologi yang jelas sehingga perlu dilakukan pengujian untuk memastikan keamanannya. Kata kunci: Artocarpus communis, bioaktivitas, kandungan kimia, etnofarmakologi

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Dendrite elongation inhibitor from Artocarpus altilis Parkinson

Cited by 2 publications

References 11 publications

Novel Chemically Modified Curcumin (CMC) Analogs Exhibit Anti-Melanogenic Activity in Primary Human Melanocytes

Novel Chemically Modified Curcumin (CMC) Analogs Exhibit Anti-Melanogenic Activity in Primary Human Melanocytes

KAJIAN ETNOBOTANI, FITOKIMIA, FARMAKOLOGI DAN TOKSIKOLOGI SUKUN (Artocarpus altilis (Park.) Fosberg)

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