Cardiovascular effects of new water-soluble derivatives of forskolin

Khandelwal, Y.; Rajeshwari, K.; Rajagopalan, Rukkumani; Swamy, L. Lakshmi; Dohadwalla, A. N.; Souza, N. J. De; Rupp, R. H.

doi:10.1021/jm00118a002

Cited by 29 publications

(7 citation statements)

References 4 publications

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“…Further synthetic and structure-activity studies, such as the introduction of water-soluble substituents onto forskolin, were carried out, and of the active analogues produced, the 6-(3-dimethylaminopropionyl) forskolin hydrochloride (NKH477) (79) (see Fig. 7 in part 1) was found to be one of the more potent water-soluble forskolin derivatives [213,214,216,217]. NKH477, like forskolin, was also found to stimulate adenylyl cyclase directly and produce various cAMP-dependent pharmacological effects, for example, on cardiovascular, respiratory, renal, and immune systems [92,[218][219][220][221][222][223].…”

Section: Second Generation Forskolin Derivativesmentioning

confidence: 99%

Plectranthus barbatus: A Review of Phytochemistry, Ethnobotanical Uses and Pharmacology – Part 2

Alasbahi

Melzig²

2010

Planta Med

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Pharmacology ! Plectranthus barbatusStudies on several extracts with various polarities obtained from different parts of P. barbatus revealed a number of pharmacological properties that may justify most of the traditional uses of P. barbatus, for example, organic extracts were reported to possess anti-inflammatory, antimicrobial [1, 2], antioxidant [3], cytotoxic [4], hypotensive [5,6], spasmolytic [7], hepatoprotective [8] and antifeedant [9] activities as well as activity against Ehrlichʼs ascites tumor in mice [10]. An alcoholic extract of the P. barbatus roots was shown to exhibit marked inhibitory action against Escherichia coli toxin-induced secretory response in rabbits and guinea pig ileal loops [11]. It has been shown that a hydroalcoholic extract of P. barbatus (880 mg/kg/day) exerted a variety of toxic effects on the different periods of pregnancy in rats; for example, in the period before embryo implantation, it caused a delay in fetal development and anti-implantation and, after embryo implantation, a delay in the development associated with maternal toxicity [12]. The water extract of P. barbatus leaves was found to exert hypoglycemic, hypotensive and antispasmodic activities [13]. It has been demonstrated that the water extract (WE) of the stems and leaves, at a dose of 1 g/kg p. o., shortened the sleeping time induced by pentobarbital by 37 %, and at a dose of 2 g/kg p. o. enhanced the intestinal transit of charcoal by 30% in mice. The WE (2 g/kg/intraduodenal) also reduced the gastric secretions (3.9 ± 1.0 to 0.5 ± 0.2 mL/4 h), and total acid secretion (34.4 ± 11.0 to 2.7 ± 0.5 mEq/L) and raised gastric pH (2.2 ± 0.3 to 6.5 ± 0.8) in rats. The treatment with WE (2 g/ kg p. o.) was also found to protect against lesions induced by ethanol or cold-restraint stress, in pylorus-ligated rats [14]. Similar results were obtained by Schultz et al. [15] who reported that the WE of the leaves (0.5-0.1 g/kg) injected into the duodenal lumen decreased the volume (62 and 76 %) and total acidity (23 and 50%) of gastric Abstract ! Plectranthus barbatus Andr. is one of the most important species of the genus Plectranthus L′ Herit. (Lamiaceae), with a wide variety of traditional medicinal uses in Hindu and Ayurvedic traditional medicine as well as in the folk medicine of Brazil, tropical Africa and China. The plant has therefore been an attractive target for intensive chemical and pharmacological studies up to now. This review presents data about the phytochemistry, ethnobotanical uses and pharmacology of Plectranthus barbatus as well as the pharmacology of its constituents. In addition to essential oil, abietane diterpenoids and 8,13-epoxy-labd-14-en-11-one diterpenoids are the main constituents found in Plectranthus barbatus. The major ethnobotanical uses are for intestinal disturbance and liver fatigue, respiratory disorders, heart diseases and certain nervous system disorders. Forskolin as one of the major constituents with its unique adenylyl cyclase activation that underlies the wide range of pharmacologic...

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Section: Second Generation Forskolin Derivativesmentioning

confidence: 99%

Plectranthus barbatus: A Review of Phytochemistry, Ethnobotanical Uses and Pharmacology – Part 2

Alasbahi

Melzig²

2010

Planta Med

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“…The reaction of 1a-tert-butyldimethylsilyl-7b-deacetyl-forskolin [6] with 3-chloro-propanoyl chloride in pyridine gave 7b-(2-chloroacetyloxy-1a-tert-butyldimethylsilyl-7b-deacetylforskolin. The crude material was subjected to the treatment of 1N NaOH and K 2 CO 3 in acetonitrile-water, leading to acyl group migration at the 6b-position to giving 6 as major product.…”

Section: Resultsmentioning

confidence: 99%

A Novel Chemo‐selective Epoxidation across Acrylate Ester: Synthesis of New Water‐Soluble Forskolin Analogues

Gangopadhyay

Lal

2006

Synthetic Communications

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While removing the TBDMS group from OH protection, a novel epoxidation reaction occurred across acrylate ester attached to a forskolin fragment. Besides spectroscopic data, the epoxide formation was confirmed by ring opening with a secondary amine. This unique epoxidation reaction, to our knowledge, is not known in the literature. This reaction led us to discover a simple deblocking protocol. The epoxide and the desired Michael substrates were used to introduce imidazole into forskolin.

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“…It is illustrated (Figure 30.19) by soluble esters of forskolin [80], of allopurinol [81], and of metronidazole [82]. It is illustrated (Figure 30.19) by soluble esters of forskolin [80], of allopurinol [81], and of metronidazole [82].…”

Section: Attachment Of the Solubilizing Moiety To An Alcoholic Hydmentioning

confidence: 99%

Preparation of Water-Soluble Compounds by Covalent Attachment of Solubilizing Moieties

Wermuth¹,

Lesuisse²

2015

The Practice of Medicinal Chemistry

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Cardiovascular effects of new water-soluble derivatives of forskolin

Cited by 29 publications

References 4 publications

Plectranthus barbatus: A Review of Phytochemistry, Ethnobotanical Uses and Pharmacology – Part 2

Plectranthus barbatus: A Review of Phytochemistry, Ethnobotanical Uses and Pharmacology – Part 2

A Novel Chemo‐selective Epoxidation across Acrylate Ester: Synthesis of New Water‐Soluble Forskolin Analogues

Preparation of Water-Soluble Compounds by Covalent Attachment of Solubilizing Moieties

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